spiro compounds

Summary

Summary: A group of compounds consisting in part of two rings sharing one carbon atom in common.

Top Publications

  1. pmc Effect of elatol, isolated from red seaweed Laurencia dendroidea, on Leishmania amazonensis
    Adriana Oliveira dos Santos
    Programa de Pós Graduação em Microbiologia, Universidade Estadual de Londrina, Rodovia Celso Garcia Cid, PR 445, Km 380, CEP 86051 990, Campus Universitario, Londrina, Parana, Brazil
    Mar Drugs 8:2733-43. 2010
  2. ncbi Spliceostatin A targets SF3b and inhibits both splicing and nuclear retention of pre-mRNA
    Daisuke Kaida
    Chemical Genetics Laboratory, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Nat Chem Biol 3:576-83. 2007
  3. pmc Reduced fidelity of branch point recognition and alternative splicing induced by the anti-tumor drug spliceostatin A
    Anna Corrionero
    Centre de Regulacio Genomica, 08003 Barcelona, Spain
    Genes Dev 25:445-59. 2011
  4. ncbi Chemical defense of Mediterranean sponges Aplysina cavernicola and Aplysina aerophoba
    Carsten Thoms
    Institut fur Pharmazeutische Biologie, Universitat Dusseldorf, Universitatsstrasse 1, Geb 26 23, D 40225 Dusseldorf, Germany
    Z Naturforsch C 59:113-22. 2004
  5. pmc An MDM2 antagonist (MI-319) restores p53 functions and increases the life span of orally treated follicular lymphoma bearing animals
    Ramzi M Mohammad
    Division of Hematology and Oncology, Department of Internal Medicine, Karmanos Cancer Institute, Wayne State University School of Medicine, 732 HWCRC, 4100 John R Street, Detroit, Michigan 48201, USA
    Mol Cancer 8:115. 2009
  6. ncbi In vitro anti-trypanosomal activity of elatol isolated from red seaweed Laurencia dendroidea
    P Veiga-Santos
    Programa de Pós Graduação em Ciências Farmacêuticas, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B 08, Universidade Estadual de Maringa, Av Colombo 5790, CEP 87020 900 Maringa, Parana, Brazil
    Parasitology 137:1661-70. 2010
  7. ncbi Identification, characterization, and biological activity of specific receptors for natural (ghrelin) and synthetic growth hormone secretagogues and analogs in human breast carcinomas and cell lines
    P Cassoni
    Department of Biomedical Sciences and Oncology, University of Turin, 10126 Turin, Italy
    J Clin Endocrinol Metab 86:1738-45. 2001
  8. ncbi In vitro and in vivo interaction of synthetic peroxide RBx11160 (OZ277) with piperaquine in Plasmodium models
    Christopher Snyder
    Swiss Tropical Institute, Socinstrasse 57, CH 4002 Basel, Switzerland
    Exp Parasitol 115:296-300. 2007
  9. ncbi A receptor in pituitary and hypothalamus that functions in growth hormone release
    A D Howard
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Science 273:974-7. 1996
  10. pmc MDM2 inhibitor MI-319 in combination with cisplatin is an effective treatment for pancreatic cancer independent of p53 function
    Asfar S Azmi
    Department of Pathology, Karmanos Cancer Institute, Wayne State University, School of Medicine, Detroit, MI, United States
    Eur J Cancer 46:1122-31. 2010

Research Grants

  1. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
  2. TOTAL SYNTHESIS OF AZASPIRACIDS
    K Nicolaou; Fiscal Year: 2006
  3. SYNTHESIS OF ANTIBIOTICS
    K C Nicolaou; Fiscal Year: 2010
  4. TOTAL SYNTHESIS OF KINAMYCINS AND LOMAIVITICINS
    K Nicolaou; Fiscal Year: 2007
  5. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2002
  6. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 1999
  7. SYNTHESIS OF ANTIBIOTICS
    K Nicolaou; Fiscal Year: 2009
  8. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2004
  9. Synthesis of Marine Neurotoxins
    K C Nicolaou; Fiscal Year: 2010
  10. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2003

Detail Information

Publications236 found, 100 shown here

  1. pmc Effect of elatol, isolated from red seaweed Laurencia dendroidea, on Leishmania amazonensis
    Adriana Oliveira dos Santos
    Programa de Pós Graduação em Microbiologia, Universidade Estadual de Londrina, Rodovia Celso Garcia Cid, PR 445, Km 380, CEP 86051 990, Campus Universitario, Londrina, Parana, Brazil
    Mar Drugs 8:2733-43. 2010
    ..Our studies indicated that elatol is a potent antiproliferative agent against promastigote and intracellular amastigote forms, and may have important advantages for the development of new anti-leishamanial chemotherapies...
  2. ncbi Spliceostatin A targets SF3b and inhibits both splicing and nuclear retention of pre-mRNA
    Daisuke Kaida
    Chemical Genetics Laboratory, RIKEN, 2 1 Hirosawa, Wako, Saitama 351 0198, Japan
    Nat Chem Biol 3:576-83. 2007
    ..Thus, the inhibition of pre-mRNA splicing during early steps involving SF3b allows unspliced mRNA leakage and translation...
  3. pmc Reduced fidelity of branch point recognition and alternative splicing induced by the anti-tumor drug spliceostatin A
    Anna Corrionero
    Centre de Regulacio Genomica, 08003 Barcelona, Spain
    Genes Dev 25:445-59. 2011
    ..Our results reveal a mechanism that prevents nonproductive base-pairing interactions in the spliceosome, and highlight the regulatory and cancer therapeutic potential of perturbing the fidelity of splice site recognition...
  4. ncbi Chemical defense of Mediterranean sponges Aplysina cavernicola and Aplysina aerophoba
    Carsten Thoms
    Institut fur Pharmazeutische Biologie, Universitat Dusseldorf, Universitatsstrasse 1, Geb 26 23, D 40225 Dusseldorf, Germany
    Z Naturforsch C 59:113-22. 2004
    ..sphinx and possibly also against other predators while the antibiotically active bioconversion products aeroplysinin-1 (5) and dienone (6) may protect sponges from invasion of bacterial pathogens...
  5. pmc An MDM2 antagonist (MI-319) restores p53 functions and increases the life span of orally treated follicular lymphoma bearing animals
    Ramzi M Mohammad
    Division of Hematology and Oncology, Department of Internal Medicine, Karmanos Cancer Institute, Wayne State University School of Medicine, 732 HWCRC, 4100 John R Street, Detroit, Michigan 48201, USA
    Mol Cancer 8:115. 2009
    ..For comparison purpose, MI-319, MI-219 and Nutlin-3 were assessed side by side against FSCCL and three other B-cell hematological tumor cell lines in growth inhibition and gene expression profiling experiments...
  6. ncbi In vitro anti-trypanosomal activity of elatol isolated from red seaweed Laurencia dendroidea
    P Veiga-Santos
    Programa de Pós Graduação em Ciências Farmacêuticas, Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Bloco B 08, Universidade Estadual de Maringa, Av Colombo 5790, CEP 87020 900 Maringa, Parana, Brazil
    Parasitology 137:1661-70. 2010
    ..This is the first report of the anti-trypanosomal effect of the sesquiterpene elatol...
  7. ncbi Identification, characterization, and biological activity of specific receptors for natural (ghrelin) and synthetic growth hormone secretagogues and analogs in human breast carcinomas and cell lines
    P Cassoni
    Department of Biomedical Sciences and Oncology, University of Turin, 10126 Turin, Italy
    J Clin Endocrinol Metab 86:1738-45. 2001
    ..In conclusion, this study provides the first demonstration of specific GHS binding sites, other than GHS-R1, in breast cancer. These receptors probably mediate growth inhibitory effects on breast carcinoma cells in vitro...
  8. ncbi In vitro and in vivo interaction of synthetic peroxide RBx11160 (OZ277) with piperaquine in Plasmodium models
    Christopher Snyder
    Swiss Tropical Institute, Socinstrasse 57, CH 4002 Basel, Switzerland
    Exp Parasitol 115:296-300. 2007
    ..1) was identified, suggesting that a RBx11160-piperaquine combination therapy in humans should allow each molecule to exert its full antimalarial effect...
  9. ncbi A receptor in pituitary and hypothalamus that functions in growth hormone release
    A D Howard
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Science 273:974-7. 1996
    ..On the basis of its pharmacological and molecular characterization, this GPC-R defines a neuroendocrine pathway for the control of pulsatile GH release and supports the notion that the GHSs mimic an undiscovered hormone...
  10. pmc MDM2 inhibitor MI-319 in combination with cisplatin is an effective treatment for pancreatic cancer independent of p53 function
    Asfar S Azmi
    Department of Pathology, Karmanos Cancer Institute, Wayne State University, School of Medicine, Detroit, MI, United States
    Eur J Cancer 46:1122-31. 2010
    ..In conclusion, this study highlights a new role of MDM2 inhibitors in combination with cisplatin, and thus warrants further clinical investigation in human pancreatic tumours containing both wt-p53 and mut-p53...
  11. doi Anti-tumour effects of elatol, a marine derivative compound obtained from red algae Laurencia microcladia
    Andreza Campos
    Department of Pharmacology Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Florianopolis, SC, Brazil
    J Pharm Pharmacol 64:1146-54. 2012
    ..This paper aims to evaluate the anti-tumour properties of elatol, a compound (sesquiterpene) isolated from algae Laurencia microcladia...
  12. pmc Structural determinants in phycotoxins and AChBP conferring high affinity binding and nicotinic AChR antagonism
    Yves Bourne
    Architecture et Fonction des Macromolecules Biologiques, Centre National de la Recherche Scientifique, Universite d Aix Marseille, Campus Luminy Case 932, F 13288 Marseille Cedex 9, France
    Proc Natl Acad Sci U S A 107:6076-81. 2010
    ....
  13. pmc Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals
    Matthias A Fügi
    Swiss Tropical Institute, Socinstrasse 57, CH 4002 Basel, Switzerland
    Antimicrob Agents Chemother 54:1042-6. 2010
    ..The latter had no effect on the antimalarial activities of the former. These data indicate that the antimalarial properties of peroxides do not derive from reversible interactions with parasite targets...
  14. pmc Co-transcriptional degradation of aberrant pre-mRNA by Xrn2
    Lee Davidson
    Wellcome Trust Centre for Cell Biology, University of Edinburgh, Edinburgh, UK
    EMBO J 31:2566-78. 2012
    ..Our data therefore establish a previously unknown function for Xrn2 and an important further aspect of pre-mRNA metabolism that occurs co-transcriptionally...
  15. pmc Spliceostatin A inhibits spliceosome assembly subsequent to prespliceosome formation
    Gabriel A Roybal
    Department of Molecular, Cell and Developmental Biology and Center for Molecular Biology of RNA, University of California, Santa Cruz, CA, USA
    Nucleic Acids Res 38:6664-72. 2010
    ..This work establishes SSA as a powerful tool for dissecting the dynamics of spliceosomes in cells. In addition our data will inform the design of synthetic splicing modulator compounds for targeted anti-tumor treatment...
  16. pmc Reactivation of p53 by novel MDM2 inhibitors: implications for pancreatic cancer therapy
    Asfar S Azmi
    Department of Pathology, Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, MI 48201, USA
    Curr Cancer Drug Targets 10:319-31. 2010
    ..No tumor inhibition was found in mut-p53 BxPC-3 xenografts. In light of our results, the inhibitors of MDM2 warrant clinical investigation as new agents for PC treatment...
  17. pmc Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis
    Vadim Makarov
    A N Bakh Institute of Biochemistry, Russian Academy of Science, 119071 Moscow, Russia
    Science 324:801-4. 2009
    ..The most advanced compound, BTZ043, is a candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant TB...
  18. pmc Temporal activation of p53 by a specific MDM2 inhibitor is selectively toxic to tumors and leads to complete tumor growth inhibition
    Sanjeev Shangary
    Comprehensive Cancer Center and Department of Internal Medicine, University of Michigan, 1500 East Medical Center Drive, Ann Arbor, MI 48109, USA
    Proc Natl Acad Sci U S A 105:3933-8. 2008
    ..MI-219 activates p53 in normal tissues with minimal p53 accumulation and is not toxic to animals. MI-219 warrants clinical investigation as a new agent for cancer treatment...
  19. pmc The catalytic asymmetric total synthesis of elatol
    David E White
    Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, California 91125, USA
    J Am Chem Soc 130:810-1. 2008
    ..This strategy represents a general platform for accessing the chamigrene natural product family, as demonstrated by the synthesis of (+)-laurencenone B as an intermediate in our route...
  20. pmc Exploring the links between natural products and bacterial assemblages in the sponge Aplysina aerophoba
    Oriol Sacristán-Soriano
    Centro de Estudios Avanzados de Blanes CSIC, Accés a la Cala St Francesc 14, 17300 Blanes, Girona, Spain
    Appl Environ Microbiol 77:862-70. 2011
    ..Further investigating these associations will shed light on the organization and functioning of host-endobiont systems such as Aplysina aerophoba...
  21. doi First identification of azaspiracid and spirolides in Mesodesma donacium and Mulinia edulis from Northern Chile
    Gonzalo Alvarez
    Centro de Investigacións Mariñas Xunta de Galicia, Apto 13, 36620 Vilanova de Arousa, Pontevedra, Spain
    Toxicon 55:638-41. 2010
    ..This is the first report of the occurrence of these groups of toxins in Chile and suggests that it is necessary to monitor routinely these substances to warrant public health and shellfish exportations...
  22. ncbi Sanglifehrin a blocks key dendritic cell functions in vivo and promotes long-term allograft survival together with low-dose CsA
    H Hackstein
    Institute for Clinical Immunology and Transfusion Medicine, Justus Liebig University, Giessen, Germany
    Am J Transplant 7:789-98. 2007
    ..We propose that SFA represents a novel class of immunophilin-binding immunosuppressants with high activity against DCs and the development of graft vasculopathy in CsA-treated recipients...
  23. pmc Quantitation of four guanine oxidation products from reaction of DNA with varying doses of peroxynitrite
    Hongbin Yu
    Biological Engineering Division, Massachusetts Institute of Technology, 77 Massachusetts Avenue, Room 56 731A, Cambridge, Massachusetts 02139, USA
    Chem Res Toxicol 18:1849-57. 2005
    ..The complexity of these dose-response relationships is likely due to the dual role of peroxynitrite as both an oxidant and a nucleophile in competition with water...
  24. ncbi Human muscarinic acetylcholine receptors are a target of the marine toxin 13-desmethyl C spirolide
    Carolina B Wandscheer
    Departamento de Farmacología, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus Universitario, Lugo, Spain
    Chem Res Toxicol 23:1753-61. 2010
    ..The 13-desmethyl C spirolide targets mAChRs causing a reduction of function, a decrease of specific antagonist binding to mAChRs, and alteration of membrane-bound receptors that might have important toxicological implications...
  25. pmc Meayamycin inhibits pre-messenger RNA splicing and exhibits picomolar activity against multidrug-resistant cells
    Brian J Albert
    Departments of 1Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, USA
    Mol Cancer Ther 8:2308-18. 2009
    ..These data suggest that meayamycin is a useful chemical probe to study pre-mRNA splicing in live cells and is a promising lead as an anticancer agent...
  26. doi The preparation of certified calibration solutions for azaspiracid-1, -2, and -3, potent marine biotoxins found in shellfish
    Ruth A Perez
    National Research Council of Canada, Institute for Marine Biosciences, 1411 Oxford Street, Halifax, Nova Scotia B3H 3Z1, Canada
    Anal Bioanal Chem 398:2243-52. 2010
    ..The calibration solutions are suitable for method development, method validation, calibration of liquid chromatography or mass spectrometry instrumentation and quality control of shellfish monitoring programs...
  27. ncbi Identification of an antimalarial synthetic trioxolane drug development candidate
    Jonathan L Vennerstrom
    College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, Nebraska 68198 6025, USA
    Nature 430:900-4. 2004
    ..Here we describe how a synthetic peroxide antimalarial drug development candidate was identified in a collaborative drug discovery project...
  28. doi Improved isolation procedure for azaspiracids from shellfish, structural elucidation of azaspiracid-6, and stability studies
    Jane Kilcoyne
    Marine Institute, Renville, Oranmore, County Galway, Ireland
    J Agric Food Chem 60:2447-55. 2012
    ..The stability of 6 relative to 1 was also assessed in three solvents in a short-term study that demonstrated the greatest stability in aqueous acetonitrile...
  29. ncbi Spiroiminodihydantoin is the major product of the 8-oxo-7,8-dihydroguanosine reaction with peroxynitrite in the presence of thiols and guanosine photooxidation by methylene blue
    J C Niles
    Division of Bioengineering, Massachusetts Institute of Technology, 77 Massachusetts Avenue, Room 56-731A, Cambridge, Massachusetts 02139, USA
    Org Lett 3:963-6. 2001
    ..Additionally, we have found that the spiroiminodihydantoin, and not the previously reported 4-hydroxy-8-oxo-4,8-dihydroguanosine, is the major final product formed during the methylene blue-mediated photooxidation of guanosine...
  30. ncbi Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes
    Yuxiang Dong
    College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, Nebraska 68198 6025, USA
    J Med Chem 48:4953-61. 2005
    ..In pharmacokinetic experiments, four trioxolanes had high plasma clearance values, suggesting a potential metabolic instability. The toxicological profiles of two trioxolanes were comparable to that of artesunate...
  31. ncbi LC-MS-MS aboard ship: tandem mass spectrometry in the search for phycotoxins and novel toxigenic plankton from the North Sea
    Bernd Krock
    Alfred Wegener Institut fur Polar und Meeresforschung, Am Handelshafen 12, 27570, Bremerhaven, Germany
    Anal Bioanal Chem 392:797-803. 2008
    ..On-board LC-MS-MS is a valuable method for near real-time analysis of phycotoxins in plankton for studies on bloom dynamics and the fate of toxins in the food web, and for characterization and isolation of putatively toxigenic organisms...
  32. ncbi Spiroiminodihydantoin and guanidinohydantoin are the dominant products of 8-oxoguanosine oxidation at low fluxes of peroxynitrite: mechanistic studies with 18O
    Jacquin C Niles
    Biological Engineering Division and Department of Chemistry, Massachusetts Institute of Technology, 77 Massachusetts Avenue, Room 56 738A, Cambridge, Massachusetts 02139, USA
    Chem Res Toxicol 17:1510-9. 2004
    ..To explain the pH-dependent Gh and Sp yields, we propose that 5 has a pKa approximately 5.8 and that the differential reactivity of the protonated and deprotonated form of 5 leads to its partitioning into Gh and Sp, respectively...
  33. doi A unique approach to the concise synthesis of highly optically active spirooxazolines and the discovery of a more potent oxindole-type phytoalexin analogue
    Xianxing Jiang
    Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of Biochemistry and Molecular Biology, Lanzhou University, Lanzhou, China
    J Am Chem Soc 132:15328-33. 2010
    ..Preliminary biological evaluation of several of the spirooxazolines using a model of acute neuroinflammation revealed promising antipyretic activity and provided an opportunity to discover new antipyretic agents...
  34. doi Discovery of XEN907, a spirooxindole blocker of NaV1.7 for the treatment of pain
    Sultan Chowdhury
    Department of Medicinal Chemistry, Xenon Pharmaceuticals Inc, Burnaby, British Columbia, Canada
    Bioorg Med Chem Lett 21:3676-81. 2011
    ..7 blocker. This lead compound, which in turn showed a further 10-fold increase in potency, represents a promising structure for further optimization efforts...
  35. ncbi Isolation, structural determination and acute toxicity of pinnatoxins E, F and G
    Andrew I Selwood
    Cawthron Institute, Private Bag 2, Nelson, New Zealand
    J Agric Food Chem 58:6532-42. 2010
    ....
  36. ncbi Preparation and synthetic applications of 2-halotryptophan methyl esters: synthesis of spirotryprostatin B
    Fumiko Y Miyake
    Department of Chemistry, Oregon State University, Corvallis, OR 97331, USA
    Angew Chem Int Ed Engl 43:5357-60. 2004
  37. ncbi Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity
    Yasuhiro Goto
    Banyu Tsukuba Research Institute, Banyu Pharmaceutical Co Ltd, Okubo 3, Tsukuba 300 2611, Japan
    J Med Chem 49:847-9. 2006
    ..A novel D-proline amide class was identified in this library and was found to possess potent ORL1 antagonistic activity...
  38. ncbi Characterization of a Dispiroketal Spirolide Subclass from Alexandrium ostenfeldii
    Joy S Roach
    Institute for Marine Biosciences, National Research Council of Canada, Halifax, Nova Scotia, Canada B3H 3Z1
    J Nat Prod 72:1237-40. 2009
    ..Spirolide H contains this cyclic imine moiety but does not show toxicity in the mouse assay, suggesting that the presence of the cyclic imine moiety is not the only structural requirement for toxicity...
  39. ncbi Novel, one-pot, three-component route to indol-3-yl substituted spirooxindole derivatives
    Tao Chen
    Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215123, China
    J Comb Chem 12:659-63. 2010
    ....
  40. ncbi Evaluation of various pH and temperature conditions on the stability of azaspiracids and their importance in preparative isolation and toxicological studies
    Carmen Alfonso
    Departamento de Farmacologia, Facultad de Veterinaria, Universidad de Santiago de Compostela, 27002 Lugo, Spain
    Anal Chem 80:9672-80. 2008
    ..Finally, the toxic potential of acid degradation products of AZAs was found to be dramatically reduced compared to the parent compounds, as assessed through cytotoxicity...
  41. doi Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide
    Claudio Trapella
    Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Bioorg Med Chem 17:5080-95. 2009
    ..However compound 35 was found inactive when challenged against N/OFQ in vivo in the mouse tail withdrawal assay. Thus, the usefulness of the novel NOP ligand compound 35 is limited to in vitro investigations...
  42. doi Organocatalytic synthesis of spiro[pyrrolidin-3,3'-oxindoles] with high enantiopurity and structural diversity
    Xiao Hua Chen
    Hefei National Laboratory for Physical Sciences at the Microscale and Department of Chemistry, University of Science and Technology of China, Hefei, 230026, China
    J Am Chem Soc 131:13819-25. 2009
    ....
  43. doi Quantitative analysis of azaspiracids in Azadinium spinosum cultures
    Thierry Jauffrais
    IFREMER, Laboratoire EMP PHYC, Rue de l Ile d Yeu, 44311, Nantes, France
    Anal Bioanal Chem 403:833-46. 2012
    ..5 × 10(9) μm(3). Moreover, experiments carried out to clarify the formation and structure of methylated AZA analogues led to the description of two AZA methyl esters and to the correction of the chemical structures of AZAs29-32...
  44. ncbi Lihouidine, a novel spiro polycyclic aromatic alkaloid from the marine sponge Suberea n. sp. (Aplysinellidae, Verongida)
    Bruce F Bowden
    Department of Chemistry, School of Pharmacy and Molecular Sciences, James Cook University, Townsville, Qld 4811, Australia
    J Org Chem 69:7791-3. 2004
    ..The structure of the alkaloid, which was racemic, was determined by a combination of 1D and 2D NMR techniques and single-crystal X-ray structural analysis...
  45. ncbi Cutting edge: sanglifehrin A, a novel cyclophilin-binding immunosuppressant blocks bioactive IL-12 production by human dendritic cells
    Christoph Steinschulte
    Institute for Clinical Immunology and Transfusion Medicine, Justus Liebig University, Giessen, Germany
    J Immunol 171:542-6. 2003
    ..Real-time RT-PCR reveals 84-94% suppression of IL-12p40, IL-12p35, and IL-23-specific p19 transcription. These novel insights into the immunosuppressive action of SFA are likely to impact on the clinical use of this agent...
  46. ncbi Structure of human cyclophilin A in complex with the novel immunosuppressant sanglifehrin A at 1.6 A resolution
    Joerg Kallen
    Protein Structure Unit, Novartis Institutes for BioMedical Research, CH 4002 Basel, Switzerland
    J Biol Chem 280:21965-71. 2005
    ..This observation raises the possibility that the dimer of CypA.SFA complexes is the molecular species mediating the immunosuppressive effect...
  47. ncbi The novel cyclophilin binding compound, sanglifehrin A, disassociates G1 cell cycle arrest from tolerance induction
    Amy Allen
    Division of Immunology and Hematopoeisis, Department of Oncology, The Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University School of Medicine, Baltimore, MD 21231, USA
    J Immunol 172:4797-803. 2004
    ..Based on these data, we propose that the decision as to whether TCR engagement will lead to productive activation or tolerance is dictated by a rapamycin -inhibitable pathway, independent of the G(1)-->S phase cell cycle progression...
  48. ncbi MDM2 inhibitors for cancer therapy
    Lyubomir T Vassilev
    Discovery Oncology, Roche Research Center, Hoffmann La Roche Inc, Nutley, NJ 07110, USA
    Trends Mol Med 13:23-31. 2007
    ..Here, the new developments in the quest for pharmacological p53 activators are reviewed with an emphasis on small-molecule inhibitors of the p53-MDM2 interaction...
  49. ncbi Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction
    Ke Ding
    Department of Internal Medicine, Comprehensive Cancer Center, Life Sciences Institute, University of Michigan, 1500 E Medical Center Drive, Ann Arbor, 48109, USA
    J Med Chem 49:3432-5. 2006
    ..MI-63 has excellent specificity over cancer cells with deleted p53 and shows a minimal toxicity to normal cells...
  50. ncbi First report on azaspiracid and yessotoxin groups detection in French shellfish
    Zouher Amzil
    IFREMER, Microbiology and Phycotoxins Department, BP 21105, 44311 Nantes, France
    Toxicon 52:39-48. 2008
    ..This paper reports for the first time on AZA and YTX-groups detection in French shellfish...
  51. ncbi New paralytic alkaloids, asperparalines A, B and C, from Aspergillus japonicus JV-23
    H Hayashi
    Department of Applied Biological Chemistry, College of Agriculture, Osaka Prefecture University, Japan
    Biosci Biotechnol Biochem 64:111-5. 2000
    ..Their structures were elucidated by spectroscopic methods and X-ray crystallography. These asperparalines showed paralytic activity against silk worms...
  52. ncbi Effective tumor cell death by sigma-2 receptor ligand siramesine involves lysosomal leakage and oxidative stress
    Marie Stampe Ostenfeld
    Apoptosis Department, Institute for Cancer Biology, Danish Cancer Society, Copenhagen, Denmark
    Cancer Res 65:8975-83. 2005
    ..c. fibrosarcoma models in mice. These results present siramesine as a promising new drug for the treatment of tumors resistant to traditional therapies...
  53. ncbi The novel cyclophilin-binding drug sanglifehrin A specifically affects antigen uptake receptor expression and endocytic capacity of human dendritic cells
    Andrea M Woltman
    Department of Nephrology, Leiden University Medical Center, Leiden, The Netherlands
    J Immunol 172:6482-9. 2004
    ..In contrast, FcalphaRI (CD89) and FcgammaRII (CD32) were increased by SFA. The explicit effect of SFA on the expression of Ag uptake receptors and Ag capture by DCs makes SFA unique among immunophilin-binding immunosuppressive drugs...
  54. ncbi Cyclophilin sensitivity to sanglifehrin A can be correlated to the same specific tryptophan residue as cyclosporin A
    Trevor J Pemberton
    The School of Life Sciences, University of Sussex and The Brighton and Sussex Medical School, Falmer, Brighton East Sussex BN1 9QG, UK
    FEBS Lett 555:335-40. 2003
    ....
  55. doi Discovery of new analogs of the marine biotoxin azaspiracid in blue mussels (Mytilus edulis) by ultra-performance liquid chromatography/tandem mass spectrometry
    Nils Rehmann
    Marine Institute, Rinville, Oranmore, Co Galway, Ireland
    Rapid Commun Mass Spectrom 22:549-58. 2008
    ..All the new AZA analogs were present at low concentrations in the shellfish and it is probably safe to assume that they do not pose a risk for the shellfish consumer...
  56. ncbi Paraherquamides, brevianamides, and asperparalines: laboratory synthesis and biosynthesis. An interim report
    Robert M Williams
    Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA
    Acc Chem Res 36:127-39. 2003
    ..Key biosynthetic studies are described, along with classical synthetic approaches as well as those inspired by Nature for the synthesis of these interesting molecules...
  57. ncbi Tissue distribution, effects of cooking and parameters affecting the extraction of azaspiracids from mussels, Mytilus edulis, prior to analysis by liquid chromatography coupled to mass spectrometry
    Philipp Hess
    Marine Environment and Food Safety Services, Marine Institute, Biotoxins, Galway Technology Park, Parkmore, Galway, Ireland
    Toxicon 46:62-71. 2005
    ..Duplicate extraction using 100% methanol was found to be the best combination of parameters...
  58. ncbi Long-term effects of ranirestat (AS-3201) on peripheral nerve function in patients with diabetic sensorimotor polyneuropathy
    Vera Bril
    Department of Medicine, University of Toronto, Canada
    Diabetes Care 29:68-72. 2006
    ..We aimed to determine whether ranirestat, an aldose reductase inhibitor, maintains the improved nerve function observed in patients with diabetic sensorimotor polyneuropathy (DSP) after completing a 12-week nerve biopsy study...
  59. ncbi Irreversible cytoskeletal disarrangement is independent of caspase activation during in vitro azaspiracid toxicity in human neuroblastoma cells
    Natalia Vilariño
    Departamento de Farmacologia, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus Universitario, 27002 Lugo, Spain
    Biochem Pharmacol 74:327-35. 2007
    ....
  60. ncbi Structural confirmation and occurrence of azaspiracids in Scandinavian brown crabs (Cancer pagurus)
    Trine Torgersen
    Department of Feed and Food Hygiene, National Veterinary Institute, P O Box 8156 Dep, NO 0033 Oslo, Norway
    Toxicon 51:93-101. 2008
    ..Very little azaspiracids were detected in mussels from the same locations at the same time, and no proposed microalgal source of azaspiracids was reported in the water previous to or at the time of collection of the toxic crabs...
  61. ncbi Antibodies with broad specificity to azaspiracids by use of synthetic haptens
    Craig J Forsyth
    Department of Chemistry, University of Minnesota, USA
    J Am Chem Soc 128:15114-6. 2006
    ..This result suggests that the antibodies also have a similar affinity for AZA2, AZA3, and AZA6 as they do for AZA1 and that such antibodies are suitable for analysis of AZAs in shellfish samples...
  62. ncbi Total synthesis and structural elucidation of azaspiracid-1. Final assignment and total synthesis of the correct structure of azaspiracid-1
    K C Nicolaou
    Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    J Am Chem Soc 128:2859-72. 2006
    ..In addition to the total synthesis of azaspiracid-1 (1), the syntheses of its C(1)-C(20) epimer (2) and of several truncated analogues for biological investigations are described...
  63. ncbi Azaspiracid-1 inhibits bioelectrical activity of spinal cord neuronal networks
    Nadezhda V Kulagina
    Center for Bio Molecular Science and Engineering, Naval Research Laboratory, 4555 Overlook Avenue SW, Code 6900, Washington, DC 20375, USA
    Toxicon 47:766-73. 2006
    ....
  64. ncbi Cell growth inhibition and actin cytoskeleton disorganization induced by azaspiracid-1 structure-activity studies
    Natalia Vilariño
    Departamento de Farmacologia, Facultad de Veterinaria, Universidad de Santiago de Compostela, 27002 Lugo, Spain
    Chem Res Toxicol 19:1459-66. 2006
    ..AZA-1-induced reorganization of the actin cytoskeleton concurred with detachment and growth inhibition, three events that are probably related...
  65. ncbi Feasibility of gamma irradiation as a stabilisation technique in the preparation of tissue reference materials for a range of shellfish toxins
    Pearse McCarron
    Marine Institute, Marine Environment and Food Safety Services, Rinville, Oranmore, County, Galway, Ireland
    Anal Bioanal Chem 387:2487-93. 2007
    ..It does, however, merit further investigation as a stabilisation procedure for preparation of shellfish tissue materials for some lipophilic toxins, in particular azaspiracids. Chemical structures of the toxins investigated in the study...
  66. ncbi Azaspiracids modulate intracellular pH levels in human lymphocytes
    Amparo Alfonso
    Departamento de Farmacologia, Facultad de Veterinaria, USC, Campus Universitario s n, 27002 Lugo, Spain
    Biochem Biophys Res Commun 346:1091-9. 2006
    ..These results point to a structure-activity relationship in AZAs pH effect that affects the modulation and the coupling of intracellular pH and Ca2+...
  67. doi Transcriptional profiling and inhibition of cholesterol biosynthesis in human T lymphocyte cells by the marine toxin azaspiracid
    Michael J Twiner
    Marine Biotoxins Program, Center for Coastal Environmental Health and Biomolecular Research, NOAA National Ocean Service, 219 Fort Johnson Road, Charleston, SC 29412, USA
    Genomics 91:289-300. 2008
    ..These data collectively detail the inhibition of de novo cholesterol synthesis, which is the likely cause of cytotoxicity and potentially a target pathway of the toxin...
  68. ncbi Effects of azaspiracid-1, a potent cytotoxic agent, on primary neuronal cultures. A structure-activity relationship study
    Carmen Vale
    Departamento de Farmacologia, USC, Lugo, Spain
    J Med Chem 50:356-63. 2007
    ..Therefore, the effect of AZA-1 on [Ca2+]c depends on the presence of the ABCD or the ABCDE-ring structure, but the complete chemical structure is needed to produce neurotoxic effects...
  69. ncbi Vincristine induces dramatic lysosomal changes and sensitizes cancer cells to lysosome-destabilizing siramesine
    Line Groth-Pedersen
    Apoptosis Department and Centre for Genotoxic Stress Research, Institute of Cancer Biology, Danish Cancer Society, Strandboulevarden 49, DK 2100 Copenhagen, Denmark
    Cancer Res 67:2217-25. 2007
    ..These data strongly suggest that combination therapies consisting of microtubule-disturbing and lysosome-destabilizing drugs may prove useful in the treatment of otherwise therapy-resistant human cancers...
  70. ncbi Freeze-drying for the stabilisation of shellfish toxins in mussel tissue (Mytilus edulis) reference materials
    Pearse McCarron
    Marine Institute, Marine Environment and Food Safety Service, Rinville, Oranmore, Galway, Ireland
    Anal Bioanal Chem 387:2475-86. 2007
    ..Figure Aliquots of freeze-dried and wet mussel tissue reference materials containing the various shellfish toxins examined in the study...
  71. ncbi The total synthesis of spirotenuipesines A and B
    Mingji Dai
    Department of Chemistry, Columbia University, Havemeyer Hall, 3000 Broadway, New York, New York 10027, USA
    J Am Chem Soc 129:3498-9. 2007
  72. ncbi Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation
    Marie Stampe Ostenfeld
    Apoptosis Department and Centre for Genotoxic Stress Response, Institute for Cancer Biology, Danish Cancer Society, Copenhagen, Denmark
    Autophagy 4:487-99. 2008
    ..Threrefore, the combination of siramesine with inhibitors of autophagosome formation appears as a promising approach for future cancer therapy...
  73. ncbi Azaspiracid-1 alters the E-cadherin pool in epithelial cells
    Giuseppe Ronzitti
    Dipartimento di Scienze Biomediche, Universita di Modena e Reggio Emilia, I 41100 Modena, Italy
    Toxicol Sci 95:427-35. 2007
    ..The possibility that azaspiracids and YTXs might share their molecular mechanism(s) of action in defined biological settings should be considered...
  74. ncbi A cytotoxicity assay for the detection and differentiation of two families of shellfish toxins
    A F Flanagan
    National Diagnostic Centre, BioResearch Ireland, National University of Ireland, Galway, Ireland
    Toxicon 39:1021-7. 2001
    ..This assay should play an important role in shellfish monitoring in the future...
  75. ncbi Total synthesis of the proposed azaspiracid-1 structure, part 2: coupling of the C1-C20, C21-C27, and C28-C40 fragments and completion of the synthesis
    K C Nicolaou
    Department of Chemistry, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Angew Chem Int Ed Engl 42:3649-53. 2003
  76. ncbi Total synthesis of the proposed azaspiracid-1 structure, part 1: construction of the enantiomerically pure C1-C20, C21-C27, and C28-C40 fragments
    K C Nicolaou
    Department of Chemistry, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Angew Chem Int Ed Engl 42:3643-8. 2003
  77. ncbi Geographical, temporal, and species variation of the polyether toxins, azaspiracids, in shellfish
    Ambrose Furey
    PROTEOBIO, Mass Spectrometry Center for Proteomics and Biotoxin Research, Department of Chemistry, Cork Institute of Technology, Bishopstown, Cork, Ireland
    Environ Sci Technol 37:3078-84. 2003
    ..Although human intoxications have so far only been associated with mussel consumption, the discovery of significant azaspiracid accumulation in other bivalve mollusks could pose a threat to human health...
  78. ncbi The first identification of azaspiracids in shellfish from France and Spain
    Ana Braña Magdalena
    PROTEOBIO, Mass Spectrometry Centre for Proteomics and Biotoxin Research, Department of Chemistry, Cork Institute of Technology, Bishopstown, Cork, Ireland
    Toxicon 42:105-8. 2003
    ..24 microg/g, from Galicia, Spain, and scallops (Pecten maximus), 0.32 microg/g, from Brittany, France. Toxin profiles were similar to those found in the equivalent shellfish in Ireland in which AZA1 was the predominant toxin...
  79. ncbi Sanglifehrin-cyclophilin interaction: degradation work, synthetic macrocyclic analogues, X-ray crystal structure, and binding data
    Richard Sedrani
    Transplantation Research, Novartis Pharma AG, S 507 312, CH 4002 Basel, Switzerland
    J Am Chem Soc 125:3849-59. 2003
    ....
  80. ncbi Food safety implications of the distribution of azaspiracids in the tissue compartments of scallops (Pecten maximus)
    A Braña Magdalena
    PROTEOBIO, Mass Spectrometry Centre for Proteomics and Biotoxin Research, Department of Chemistry, Cork Institute of Technology, Bishopstown, Cork, Ireland
    Food Addit Contam 20:154-60. 2003
    ..It was concluded that to improve food safety, only the adductor muscle and gonad of scallops should be permitted for sale to the public...
  81. ncbi Lu 28-179 labels a sigma(2)-site in rat and human brain
    Karina Krøyer Søby
    Department of Molecular Pharmacology, H Lundbeck A S, Biological Research, DK 2500, Valby, Denmark
    Neuropharmacology 43:95-100. 2002
    ..Overall, these data are consistent with [(3)H]Lu 28-179 labelling a sigma(2)-like binding site...
  82. ncbi First evidence of an extensive northern European distribution of azaspiracid poisoning (AZP) toxins in shellfish
    Kevin J James
    Department of Chemistry, Ecotoxicology Research Unit, Cork Institute of Technology, Ireland
    Toxicon 40:909-15. 2002
    ..This is the first report of the occurrence of these azaspiracids outside Ireland with the significant implications that these toxins may occur in shellfish throughout northern Europe...
  83. ncbi Azaspiracid shellfish poisoning: unusual toxin dynamics in shellfish and the increased risk of acute human intoxications
    K J James
    Ecotoxicology Research Unit, Chemistry Department, Cork Institute of Technology, Bishopstown, Cork, Ireland
    Food Addit Contam 19:555-61. 2002
    ..It was also observed that the toxin profiles differed significantly in various mussel tissues with AZA1 as the predominant toxin in the digestive glands and AZA3 predominant in the remaining tissues...
  84. ncbi Azaspiracid-1, a potent, nonapoptotic new phycotoxin with several cell targets
    Yolanda Roman
    Departamento de Farmacologia, Facultad de Veterinaria, USC, 27002 Lugo, Spain
    Cell Signal 14:703-16. 2002
    ..The effect of AZ-1 in cAMP is not extracellularly Ca(2+) dependent and insensitive to okadaic acid (OA)...
  85. ncbi Siramesine H Lundbeck
    C Heading
    Curr Opin Investig Drugs 2:266-70. 2001
    ..Phase III trials are expected to take place in 2002 [387270]. A series of compounds have been synthesized by Lundbeck, the most potent of which may serve as a backup compound [179036]...
  86. ncbi Chronic effects in mice caused by oral administration of sublethal doses of azaspiracid, a new marine toxin isolated from mussels
    Emiko Ito
    Research Center for Pathogenic Fungi and Microbial Toxicoses, Chiba University, 1 8 1 Inohana, Chuo Ku, Chiba 260 8673, Japan
    Toxicon 40:193-203. 2002
    ..Tumors were not observed in 11 mice treated at lower doses and in 19 control mice. Hyperplasia of epithelial cells was also observed in the stomach of six mice out of ten administered at 20 microg/kg...
  87. ncbi Sanglifehrin A, a novel cyclophilin-binding compound showing immunosuppressive activity with a new mechanism of action
    G Zenke
    Transplantation Research, Core Technology, and Nervous System Research, Novartis Pharma, Basel, Switzerland
    J Immunol 166:7165-71. 2001
    ..In summary, we have identified a novel immunosuppressant, which represents, in addition to CsA, FK506 and rapamycin, a fourth class of immunophilin-binding metabolites with a new, yet undefined mechanism of action...
  88. ncbi Structures of azaspiracid analogs, azaspiracid-4 and azaspiracid-5, causative toxins of azaspiracid poisoning in Europe
    K Ofuji
    Graduate School of Agricultural Science, Tohoku University, Sendai, Japan
    Biosci Biotechnol Biochem 65:740-2. 2001
    ....
  89. ncbi Binding of 125I-labeled ghrelin to membranes from human hypothalamus and pituitary gland
    G Muccioli
    Department of Anatomy, Pharmacology and Forensic Medicine, University of Turin, Italy
    J Endocrinol Invest 24:RC7-9. 2001
    ..These receptors are the specific binding sites for GHS and their antagonists, as well as for SRIH analogs (vapreotide and cortistatin- 14), but not for native SRIH...
  90. ncbi Potent antibacterial activity of halogenated metabolites from Malaysian red algae, Laurencia majuscula (Rhodomelaceae, Ceramiales)
    Charles S Vairappan
    Borneo Marine Research Institute, Universiti Malaysia Sabah, Locked Beg 2073, 88999 Kota Kinabalu, Sabah, Malaysia
    Biomol Eng 20:255-9. 2003
    ..pneumonia and Salmonella sp. Further tests conducted using dilution method showed both compounds as having bacteriostatic mode of action against the tested bacteria...
  91. ncbi Detection of five new hydroxyl analogues of azaspiracids in shellfish using multiple tandem mass spectrometry
    Kevin J James
    PROTEOBIO, Department of Chemistry, Mass Spectrometry Centre for Proteomics and Biotoxin Research, Cork Institute of Technology, Bishopstown, Cork, Ireland
    Toxicon 41:277-83. 2003
    ....
  92. ncbi A novel pectenotoxin, PTX-12, in Dinophysis spp. and shellfish from Norway
    Christopher O Miles
    National Veterinary Institute, PB 8156 Dep, N 0033 Oslo, Norway
    Chem Res Toxicol 17:1423-33. 2004
    ..Our data also suggest that heterotrophic dinoflagellates may accumulate toxins from their prey...
  93. ncbi Azaspiracid poisoning, the food-borne illness associated with shellfish consumption
    K J James
    PROTEOBIO, Mass Spectrometry Centre for Proteomics and Biotoxin Research, Department of Chemistry, Cork Institute of Technology, Bishopstown, Cork, Ireland
    Food Addit Contam 21:879-92. 2004
    ..The strict regulatory control of azaspiracids in shellfish now requires frequent testing of shellfish using highly specific and sensitive methods involving liquid chromatography-mass spectrometry...
  94. ncbi Teratogenic effects of azaspiracid-1 identified by microinjection of Japanese medaka (Oryzias latipes) embryos
    Jamie R Colman
    Marine Biotoxins Program, Center for Coastal Environmental Health and Biomolecular Research, NOAA National Ocean Service, Charleston, SC 29412, USA
    Toxicon 45:881-90. 2005
    ..This work will complement future investigations on AZA-1 accumulation in marine food webs and provide a basis for understanding its toxicity at different trophic levels...
  95. ncbi Azaspiracid-4 inhibits Ca2+ entry by stored operated channels in human T lymphocytes
    Amparo Alfonso
    Departamento de Farmacologia, Facultad de Veterinaria, USC, 27002 Lugo, Spain
    Biochem Pharmacol 69:1627-36. 2005
    ..Thus, AZ-4 appeared to be a novel inhibitor of plasma membrane Ca2+ channels, affecting at least to store operated channels, showing an effect clearly different from other azaspiracid analogues...
  96. ncbi Is there a risk of human poisoning by azaspiracids from shellfish harvested at the Portuguese coast?
    Paulo Vale
    Instituto Nacional de Investigação Agrária e das Pescas IPIMAR, Av Brasilia, 1449 006 Lisboa, Portugal
    Toxicon 44:943-7. 2004
    ....
  97. ncbi Effects of Azaspiracids 2 and 3 on intracellular cAMP, [Ca2+], and pH
    Yolanda Roman
    Departamentos de Farmacología and Departamento de Fisiología, Facultad de Veterinaria, Universidad de Santiago de Compostela, 27002 Lugo, Spain
    Chem Res Toxicol 17:1338-49. 2004
    ..Thus, both analogues seem to involve an AC pathway, although its effects on [Ca(2+)](i) and pH(i) are quite different...
  98. ncbi Elucidation of the fragmentation pathways of azaspiracids, using electrospray ionisation, hydrogen/deuterium exchange, and multiple-stage mass spectrometry
    Mónica Díaz Sierra
    PROTEOBIO, Mass Spectrometry Centre for Proteomics and Biotoxin Research, Department of Chemistry, Cork Institute of Technology, Bishopstown, Cork, Ireland
    J Mass Spectrom 38:1178-86. 2003
    ..The fragmentation of the A-ring was the most facile and was exploited in the development of LC/MS(n) methods for the analysis of azaspiracids...
  99. ncbi Aldose reductase inhibition by AS-3201 in sural nerve from patients with diabetic sensorimotor polyneuropathy
    Vera Bril
    Department of Medicine, University of Toronto, Ontario, Canada
    Diabetes Care 27:2369-75. 2004
    ..An additional aim was to determine whether any changes in nerve function would manifest with AS-3201 therapy...
  100. ncbi Cytotoxic and cytoskeletal effects of azaspiracid-1 on mammalian cell lines
    Michael J Twiner
    Marine Biotoxins Program, Center for Coastal Environmental Health and Biomolecular Research, NOAA National Ocean Service, Charleston SC 29412, USA
    Toxicon 45:891-900. 2005
    ..Although these phycotoxin-specific effects of AZA-1 suggest a possible site of action, further work using cell-based approaches is needed to determine the precise mode of action of AZA-1...
  101. ncbi Novel spirocyclic trichothecanes, spirotenuipesine A and B, isolated from entomopathogenic fungus, Paecilomyces tenuipes
    Haruhisa Kikuchi
    Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba yama, Aoba ku, Sendai 980 8578, Japan
    J Org Chem 69:352-6. 2004
    ..It is noteworthy that trichothecane mycotoxins are present in Paecilomyces tenuipes, which is typically used in medicinal health food...

Research Grants125 found, 100 shown here

  1. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  2. TOTAL SYNTHESIS OF AZASPIRACIDS
    K Nicolaou; Fiscal Year: 2006
    ..g. lung, liver, spleen and lymphocyte damage as well as cancer) health hazards. The project is also expected to advance our knowledge in chemical synthesis and impact favorably the drug discovery and development process. ..
  3. SYNTHESIS OF ANTIBIOTICS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  4. TOTAL SYNTHESIS OF KINAMYCINS AND LOMAIVITICINS
    K Nicolaou; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  5. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2002
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  6. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 1999
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  7. SYNTHESIS OF ANTIBIOTICS
    K Nicolaou; Fiscal Year: 2009
    ..abstract_text> ..
  8. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  9. Synthesis of Marine Neurotoxins
    K C Nicolaou; Fiscal Year: 2010
    ..The project is also expected to significantly advance our knowledge in chemical synthesis, chemical biology, and medicine ..
  10. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2003
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  11. Synthesis of Marine Neurotoxins
    K Nicolaou; Fiscal Year: 2007
    ..The project is also expected to significantly advance our knowledge in chemical synthesis, chemical biology, and medicine ..
  12. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2000
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  13. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  14. SYNTHESIS OF ANTICANCER AGENTS
    K Nicolaou; Fiscal Year: 2006
    ..unreadable] [unreadable] [unreadable]..
  15. SYNTHESIS OF ANTIBIOTICS
    K Nicolaou; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  16. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  17. Synthesis of Marine Neurotoxins
    K Nicolaou; Fiscal Year: 2008
    ..The project is also expected to significantly advance our knowledge in chemical synthesis, chemical biology, and medicine ..
  18. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2003
    ..abstract_text> ..
  19. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  20. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2006
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  21. Synthesis of Marine Neurotoxins
    K Nicolaou; Fiscal Year: 2009
    ..The project is also expected to significantly advance our knowledge in chemical synthesis, chemical biology, and medicine ..
  22. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2001
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  23. SYNTHESIS OF ANTICANCER AGENTS
    K Nicolaou; Fiscal Year: 2009
    ..abstract_text> ..
  24. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2005
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  25. TOTAL SYNTHESIS OF THIOSTREPTON
    K Nicolaou; Fiscal Year: 2003
    ..The disease areas likely to benefit most from the proposed investigations are bacterial-caused diseases and malaria. ..
  26. SYNTHESIS OF ANTIBIOTICS
    K Nicolaou; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  27. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2001
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  28. TOTAL SYNTHESIS OF AZASPIRACIDS
    K Nicolaou; Fiscal Year: 2005
    ..g. lung, liver, spleen and lymphocyte damage as well as cancer) health hazards. The project is also expected to advance our knowledge in chemical synthesis and impact favorably the drug discovery and development process. ..
  29. SYNTHESIS OF ANTIBIOTICS
    K Nicolaou; Fiscal Year: 2008
    ..abstract_text> ..
  30. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  31. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2002
    ..abstract_text> ..
  32. TOTAL SYNTHESIS OF THIOSTREPTON
    K Nicolaou; Fiscal Year: 2005
    ..The disease areas likely to benefit most from the proposed investigations are bacterial-caused diseases and malaria. ..
  33. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2004
    ..abstract_text> ..
  34. TOTAL SYNTHESIS OF THIOSTREPTON
    K Nicolaou; Fiscal Year: 2004
    ..The disease areas likely to benefit most from the proposed investigations are bacterial-caused diseases and malaria. ..
  35. TOTAL SYNTHESIS OF THIOSTREPTON
    K Nicolaou; Fiscal Year: 2002
    ..The disease areas likely to benefit most from the proposed investigations are bacterial-caused diseases and malaria. ..
  36. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2007
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  37. SYNTHESIS OF ANTICANCER AGENTS
    K Nicolaou; Fiscal Year: 2008
    ..abstract_text> ..
  38. SYNTHESIS OF MACROCYCLES STEROIDS CYCLOPENTANOIDS ETC
    BARRY TROST; Fiscal Year: 2001
    ..Ring expansion methods may convert these cores into the taxoid skeleton with appropriate functionality at key points for analog development. ..
  39. Synthesis of Macrolides. Steroids, Cyclopentanoids, etc
    BARRY TROST; Fiscal Year: 2005
    ..This new concept sets the stage for solutions to a long standing problem, the ion channel blockers, the grayanotoxins. as well as the more recently discovered rameswaralide, a potent antiinflamatory. ..
  40. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 2003
    ..By accessing a very diverse range of structural types, the best opportunities to discover new therapeutic agents arise. ..
  41. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 2001
    ..By accessing a very diverse range of structural types, the best opportunities to discover new therapeutic agents arise. ..
  42. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 2002
    ..By accessing a very diverse range of structural types, the best opportunities to discover new therapeutic agents arise. ..
  43. Synthesis of Macrolides. Steroids, Cyclopentanoids, etc
    BARRY TROST; Fiscal Year: 2002
    ..This new concept sets the stage for solutions to a long standing problem, the ion channel blockers, the grayanotoxins. as well as the more recently discovered rameswaralide, a potent antiinflamatory. ..
  44. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 2000
    ..Equally important, new avenues to vary structure around these cores in order to establish structure-activity relationships with the aim to create better therapeutic agents become available. ..
  45. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 1993
    ..The diversity of the challenges posed by antiviral and antitumor agents represent highly meaningful tests of their use...
  46. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 2004
    ..By accessing a very diverse range of structural types, the best opportunities to discover new therapeutic agents arise. ..
  47. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2008
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  48. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  49. Novel Approaches for Antitumor and Antiviral Agents
    BARRY TROST; Fiscal Year: 2009
    ..This proposal helps to address this key challenge by developing the underlying initial technology within classes of compounds having demonstrably antitumor or antiviral activities. ..
  50. NOVEL SYNTHETIC APPROACHES TO ANTITUMOR COMPOUNDS
    BARRY TROST; Fiscal Year: 1990
    ..A strategy to one family of tumor promoters represented by teleocidin explores the concept of chemical chameleons. In most cases, the strategy also considers the problem of absolute stereochemistry...
  51. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 2005
    ..By expediting access to very diverse arrays of structural types, the best opportunities to discover new therapeutic agents arise. ..
  52. SYNTHESIS OF MACROCYCLES STEROIDS CYCLOPENTANOIDS ETC
    BARRY TROST; Fiscal Year: 2000
    ..Ring expansion methods may convert these cores into the taxoid skeleton with appropriate functionality at key points for analog development. ..
  53. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 1999
    ..Equally important, new avenues to vary structure around these cores in order to establish structure-activity relationships with the aim to create better therapeutic agents become available. ..
  54. SYNTHESIS OF MACROCYCLES STEROIDS CYCLOPENTANOIDS ETC
    BARRY TROST; Fiscal Year: 1999
    ..Ring expansion methods may convert these cores into the taxoid skeleton with appropriate functionality at key points for analog development. ..
  55. NOVEL APPROACHES TO ANTITUMOR AND ANTIVIRAL AGENTS
    BARRY TROST; Fiscal Year: 2007
    ..By expediting access to very diverse arrays of structural types, the best opportunities to discover new therapeutic agents arise. ..
  56. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2007
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  57. NOVEL SYNTHETIC APPROACHES TO ANTITUMOR COMPOUNDS
    BARRY TROST; Fiscal Year: 1991
    ..A strategy to one family of tumor promoters represented by teleocidin explores the concept of chemical chameleons. In most cases, the strategy also considers the problem of absolute stereochemistry...
  58. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2006
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. [unreadable] [unreadable] [unreadable]..
  59. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2007
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  60. Evaluation in Primates of Cocaine Esterase for the Treatment of Cocaine Toxicity
    Mei Chuan Ko; Fiscal Year: 2008
    ..Dose-response functions for each enzyme will be obtained repeatedly and blood samples analyzed for titer development so that tolerance to the effects of CocE can be monitored. ..
  61. Evaluation in Primates of Cocaine Esterase for the Treatment of Cocaine Toxicity
    Mei Chuan Ko; Fiscal Year: 2009
    ..Dose-response functions for each enzyme will be obtained repeatedly and blood samples analyzed for titer development so that tolerance to the effects of CocE can be monitored. ..
  62. Intrathecal Opioid-Induced Pruritus
    Mei Chuan Ko; Fiscal Year: 2002
    ..These studies would provide a systematic understanding of the pharmacology of intrathecal morphine-induced pruritus in primates and establish the basis for identifying potential therapeutically effective antipruritics. ..
  63. NOVEL SYNTHETIC APPROACHES TO ANTITUMOR COMPOUNDS
    BARRY TROST; Fiscal Year: 1992
    ..A strategy to one family of tumor promoters represented by teleocidin explores the concept of chemical chameleons. In most cases, the strategy also considers the problem of absolute stereochemistry...
  64. Intrathecal Opioid-Induced Pruritus
    Mei Chuan Ko; Fiscal Year: 2001
    ..These studies would provide a systematic understanding of the pharmacology of intrathecal morphine-induced pruritus in primates and establish the basis for identifying potential therapeutically effective antipruritics. ..
  65. Synthesis of Macrolides. Steroids, Cyclopentanoids, etc
    BARRY TROST; Fiscal Year: 2003
    ..This new concept sets the stage for solutions to a long standing problem, the ion channel blockers, the grayanotoxins. as well as the more recently discovered rameswaralide, a potent antiinflamatory. ..
  66. Novel Approaches for Antitumor and Antiviral Agents
    Barry M Trost; Fiscal Year: 2010
    ..This proposal helps to address this key challenge by developing the underlying initial technology within classes of compounds having demonstrably antitumor or antiviral activities. ..
  67. Intrathecal Opioid-Induced Pruritus
    Mei Chuan Ko; Fiscal Year: 2003
    ..These studies would provide a systematic understanding of the pharmacology of intrathecal morphine-induced pruritus in primates and establish the basis for identifying potential therapeutically effective antipruritics. ..
  68. Synthesis and Study of Complex Natural Products
    Mohammad Movassaghi; Fiscal Year: 2009
    ....
  69. SYNTHESIS OF BIOACTIVE NATURAL PRODUCTS
    AMOS SMITH; Fiscal Year: 1992
    ..We believe that this philosophy of "unified synthetic strategies" will be further developed by this proposal...
  70. SYNTHESIS OF BIOACTIVE NATURAL PRODUCTS
    AMOS SMITH; Fiscal Year: 1991
    ..FK506 is therefore an important target for total synthesis, not only for its intrinsic synthetic challenge, but also due to its extrinsic worth to the field of medicine...
  71. UCLA AIDS Prevention and Treatment Clinical Trials Unit
    Judith Currier; Fiscal Year: 2008
    ..10. Stimulate community involvement and encourage participation of women and racial/ethnic minorities in ACTG, HPTN and VTN clinical trials at the UCLA-APT-CTU. ..
  72. Pilot-Scale Libraries for High-throughput Screening
    AMOS SMITH; Fiscal Year: 2007
    ....
  73. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun Ghosh; Fiscal Year: 2009
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  74. ASYMMETRIC SYNTHESIS OF IONOPHORE & MACROLIDE ANTIBIOTIC
    David Evans; Fiscal Year: 1992
    ....
  75. ASYMMETRIC SYNTHESIS OF VANCOMYCIN ANTIBIOTICS
    David Evans; Fiscal Year: 1999
    ..During the course of this project we intend to confirm (correct) the absolute stereochemical assignments of the principal members of this family by total synthesis. ..
  76. MECHANISM OF RENAL CELL REPAIR FOLLOWING TOXICANT INJURY
    RICK SCHNELLMANN; Fiscal Year: 1999
    ..Completion of these aims will result in a better understanding of the mechanisms involved in renal cell regeneration and the repair of physiological functions following toxicant exposure. ..
  77. SYNTHESIS OF BIOACTIVE NATURAL PRODUCTS
    AMOS SMITH; Fiscal Year: 2009
    ..Our experience with discodermolide gives us great confidence in this area. ..
  78. Alzhelmer's Disease Drug Development Program
    AMOS SMITH; Fiscal Year: 2008
    ....
  79. Pilot-Scale Libraries for High-throughput Screening
    AMOS SMITH; Fiscal Year: 2008
    ....
  80. NMR systems : 2 Bruker Avance 500 Consoles
    AMOS SMITH; Fiscal Year: 2006
    ..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. [unreadable] [unreadable] [unreadable]..
  81. SYNTHESIS OF BIOACTIVE NATURAL PRODUCTS
    AMOS SMITH; Fiscal Year: 2000
    ..This philosophy of "unified synthetic strategies" will be further developed in this proposal. ..
  82. ASYMMETRIC SYNTHESIS OF VANCOMYCIN ANTIBIOTICS
    David Evans; Fiscal Year: 2000
    ..During the course of this project we intend to confirm (correct) the absolute stereochemical assignments of the principal members of this family by total synthesis. ..
  83. SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORS
    AMOS SMITH; Fiscal Year: 2000
    ..abstract_text> ..