Genomes and Genes
Publications253 found, 100 shown here
- Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATMIan Hickson
KuDOS Pharmaceuticals Ltd, Cambridge Science Park, Milton Road, Cambridge, UK
Cancer Res 64:9152-9. 2004..We conclude that KU-55933 is a novel, specific, and potent inhibitor of the ATM kinase...
- Pyrones as bacterial signaling moleculesAlexander O Brachmann
1 Merck Stiftungsprofessur für Molekulare Biotechnologie, Goethe Universitat Frankfurt, Frankfurt, Germany 2
Nat Chem Biol 9:573-8. 2013..the insect pathogen Photorhabdus luminescens the orphan LuxR-type receptor PluR detects endogenously produced α-pyrones that serve as signaling molecules at low nanomolar concentrations...
- From miso, saké and shoyu to cosmetics: a century of science for kojic acidRonald Bentley
Department of Biological Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA
Nat Prod Rep 23:1046-62. 2006..It was one of the first secondary metabolites to have its biosynthetic pathway studied by the isotope tracer technique, and, more recently, has been of interest as a skin lightening agent. There are 112 references...
- In vitro activity of API-1252, a novel FabI inhibitor, against clinical isolates of Staphylococcus aureus and Staphylococcus epidermidisJames A Karlowsky
Antimicrob Agents Chemother 51:1580-1. 2007
- Arzanol, an anti-inflammatory and anti-HIV-1 phloroglucinol alpha-Pyrone from Helichrysum italicum ssp. microphyllumGiovanni Appendino
Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Universita del Piemonte Orientale, Via Bovio 6, 28100 Novara, Italy
J Nat Prod 70:608-12. 2007..Arzanol inhibited HIV-1 replication in T cells and the release of pro-inflammatory cytokines in LPS-stimulated primary monocytes, qualifying as a novel plant-derived anti-inflammatory and antiviral chemotype worth further investigation...
- Cytotoxic activity of (S)-goniothalamin and analogues against human cancer cellsAngelo de Fátima
Instituto de Quimica, UNICAMP, CP 6154, 13084 971, Campinas, Sao Paulo, Brazil
Bioorg Med Chem 14:622-31. 2006..adr)...
- Melasma: a comprehensive update: part IIVaneeta M Sheth
Department of Dermatology at Brigham and Women s Hospital, Harvard Medical School, Boston, Massachusetts, USA
J Am Acad Dermatol 65:699-714; quiz 715. 2011..A thorough understanding of the risks and benefits of various therapeutic options is crucial in selecting the best treatment...
- Α-pyrones and diketopiperazine derivatives from the marine-derived actinomycete Nocardiopsis dassonvillei HR10-5Peng Fu
Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, and Affiliated Hospital of Medical College of Qingdao University, Qingdao 266003, People s Republic of China
J Nat Prod 74:2219-23. 2011Three new α-pyrones, nocapyrones E-G (1-3), and three new diketopiperazine derivatives, nocazines A-C (4-6), together with a new oxazoline compound, nocazoline A (7), were isolated from the marine-derived actinomycete Nocardiopsis ..
- Identification, cloning, expression, and purification of three novel human calcium-independent phospholipase A2 family members possessing triacylglycerol lipase and acylglycerol transacylase activitiesChristopher M Jenkins
Division of Bioorganic Chemistry and Molecular Pharmacology, Department of Medicine, Washington University School of Medicine, St Louis, Missouri 63110, USA
J Biol Chem 279:48968-75. 2004....
- Suppression of HIV-1 infection by a small molecule inhibitor of the ATM kinaseAlan Lau
KuDOS Pharmaceuticals Limited, 327 Cambridge Science Park, Milton Road, Cambridge CB4 0WG, UK
Nat Cell Biol 7:493-500. 2005..Consistent with these observations, we demonstrate that a novel and specific small molecule inhibitor of ATM kinase activity, KU-55933, is capable of suppressing the replication of both wild-type and drug-resistant HIV-1...
- Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndromeBarbara Cool
Department of Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
Cell Metab 3:403-16. 2006..These results demonstrate that small molecule-mediated activation of AMPK in vivo is feasible and represents a promising approach for the treatment of type 2 diabetes and the metabolic syndrome...
- Mode of action, in vitro activity, and in vivo efficacy of AFN-1252, a selective antistaphylococcal FabI inhibitorNachum Kaplan
Affinium Pharmaceuticals, Inc, Toronto, ON, Canada
Antimicrob Agents Chemother 56:5865-74. 2012..These studies, demonstrating a selective mode of action, potent in vitro activity, and in vivo efficacy, support the continued investigation of AFN-1252 as a targeted therapeutic for staphylococcal infections...
- Apoptosis of insulin-secreting cells induced by endoplasmic reticulum stress is amplified by overexpression of group VIA calcium-independent phospholipase A2 (iPLA2 beta) and suppressed by inhibition of iPLA2 betaSasanka Ramanadham
Mass Spectrometry Resource, Division of Endocrinology, Diabetes, and Metabolism, Department of Medicine, Washington University School of Medicine, Box 8127, 660 South Euclid Avenue, St Louis, Missouri 63110, USA
Biochemistry 43:918-30. 2004..These findings indicate that iPLA(2)beta participates in ER stress-induced apoptosis, a pathway that promotes beta-cell death in diabetes...
- Beyond AICA riboside: in search of new specific AMP-activated protein kinase activatorsBruno Guigas
Hormone and Metabolic Research Unit, Université catholique de Louvain and de Duve Institute, Brussels, Belgium
IUBMB Life 61:18-26. 2009..We conclude that A-769662 could be one of the new promising chemical agents to activate AMPK with limited AMPK-independent side effects...
- An assessment of the genotoxicity and human health risk of topical use of kojic acid [5-hydroxy-2-(hydroxymethyl)-4H-pyran-4-one]Gerhard J Nohynek
L Oreal Recherche, Corporate Safety, 25 29, quai Aulagnier, 92600 Asnières, France
Food Chem Toxicol 42:93-105. 2004..In conclusion, the topical use of KA as a skin lightening agent results in minimal exposure that poses no or negligible risk of genotoxicity or toxicity to the consumer...
- Evaluation of the antioxidant and cytotoxic activity of arzanol, a prenylated alpha-pyrone-phloroglucinol etherodimer from Helichrysum italicum subsp.microphyllumAntonella Rosa
Dipartimento di Biologia Sperimentale, Sez Patologia Sperimentale, Universita degli Studi di Cagliari, Cittadella Universitaria, SS 554, Km 4 5, 09042 Monserrato, Cagliari, Italy
Chem Biol Interact 165:117-26. 2007..The results of the present work suggest that the natural compound arzanol exerts useful antioxidant properties in different in vitro systems of lipid peroxidation...
- Nocapyrones H-J, 3,6-disubstituted α-pyrones from the marine actinomycete Nocardiopsis sp. KMF-001Min Cheol Kim
Natural Medicine Center, Korea Institute of Science and Technology KIST, Gangneung, Gangwon do 210 340, Republic of Korea
Chem Pharm Bull (Tokyo) 61:511-5. 2013Three new 3,6-disubstituted α-pyrones, nocapyrones H-J (1-3), were isolated from the marine actinomycete Nocardiopsis sp. KMF-001...
- Identity between the Ca2+-independent phospholipase A2 enzymes from P388D1 macrophages and Chinese hamster ovary cellsM A Balboa
Department of Chemistry and Biochemistry, University of California at San Diego, La Jolla, California 92093 0601, USA
J Biol Chem 272:8576-80. 1997..Additionally, covalent modification of the CHO enzyme by [3H]bromoenol lactone is dependent on active enzyme as is the P388D1 iPLA2. Finally, both enzymes have the same specific activities under identical experimental conditions...
- A bromoenol lactone suicide substrate inactivates group VIA phospholipase A2 by generating a diffusible bromomethyl keto acid that alkylates cysteine thiolsHaowei Song
Medicine Department Mass Spectrometry Facility, Division of Endocrinology, Metabolism, and Lipid Research, Washington University School of Medicine, St Louis, Missouri 63110, USA
Biochemistry 45:1061-73. 2006....
- Nocapyrones A-D, gamma-pyrones from a Nocardiopsis strain isolated from the marine sponge Halichondria paniceaImke Schneemann
Kieler Wirkstoff Zentrum KiWiZ at the Leibniz Institute of Marine Sciences IFM GEOMAR, Am Kiel Kanal 44, 24106 Kiel, Germany
J Nat Prod 73:1444-7. 2010Four new gamma-pyrones, nocapyrones A-D (1-4), were isolated from an organic extract of the Nocardiopsis strain HB383, which was isolated from the marine sponge Halichondria panicea...
- Arzanol, a prenylated heterodimeric phloroglucinyl pyrone, inhibits eicosanoid biosynthesis and exhibits anti-inflammatory efficacy in vivoJulia Bauer
Department for Pharmaceutical Analytics, Pharmaceutical Institute, University of Tuebingen, Auf der Morgenstelle 8, D 72076 Tuebingen, Germany
Biochem Pharmacol 81:259-68. 2011..italicum, and a rationale for further pre-clinical evaluation of this novel anti-inflammatory lead...
- The ATM inhibitor KU-55933 suppresses cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated AktYan Li
Sanford Project and Cancer Biology Research Center, Sanford Research University of South Dakota, Sioux Falls, South Dakota 57104, USA
Mol Cancer Ther 9:113-25. 2010..Therefore, combining KU-55933 with rapamycin may provide a highly effective approach for improving mammalian target of rapamycin-targeted anticancer therapy that is currently hindered by rapamycin-induced feedback activation of Akt...
- Tyrosine phosphatase inhibition augments collateral blood flow in a rat model of peripheral vascular diseaseAndrew N Carr
Cardiovascular Research Division, Health Care Research Center, Procter and Gamble Pharmaceuticals, 8700 Mason Montgomery Rd, Box 1064, Mason, OH 45040, USA
Am J Physiol Heart Circ Physiol 287:H268-76. 2004....
- Group VIA phospholipase A2 (iPLA2beta) participates in angiotensin II-induced transcriptional up-regulation of regulator of g-protein signaling-2 in vascular smooth muscle cellsZhongwen Xie
Department of Physiology and the Graduate Center for Nutritional Sciences, University of Kentucky, Lexington, Kentucky 40536, USA
J Biol Chem 282:25278-89. 2007..Collectively, our results demonstrate that iPLA2beta participates in Ang II-induced transcriptional up-regulation of RGS2 in VSMC...
- AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activityJames A Karlowsky
Department of Medical Microbiology and Infectious Diseases, Faculty of Medicine, University of Manitoba, Winnipeg, Manitoba, Canada
Antimicrob Agents Chemother 53:3544-8. 2009..Enterobacteriaceae, nonfermentative gram-negative bacilli, and Moraxella catarrhalis. These data support the continued development of AFN-1252 for the treatment of patients with resistant staphylococcal infections...
- Potent, selective pyrone-based inhibitors of stromelysin-1David T Puerta
Department of Chemistry and Biochemistry, Howard Hughes Medical Institute, and Center for Theoretical Biological Physics, University of California San Diego, La Jolla, CA 92093, USA
J Am Chem Soc 127:14148-9. 2005..The inhibitors demonstrate nanomolar potency against MMP-3 and are selective for MMP-3 over MMP-2 and MMP-1. We postulate that the potency and unusual selectivity profile of these MPI is attributable to the pyrone chelating group...
- Identification of calcium-independent phospholipase A2 (iPLA2) beta, and not iPLA2gamma, as the mediator of arginine vasopressin-induced arachidonic acid release in A-10 smooth muscle cells. Enantioselective mechanism-based discrimination of mammalian iPLChristopher M Jenkins
Division of Bioorganic Chemistry and Molecular Pharmacology, Department of Medicine, Washington University School of Medicine, St Louis, Missouri 63110, USA
J Biol Chem 277:32807-14. 2002....
- Tipranavir-ritonavir genotypic resistance score in protease inhibitor-experienced patientsAnne Genevieve Marcelin
Department of Virology, Pitie Salpetriere Hospital, 83 Boulevard de l hopital, 75013 Paris, France
Antimicrob Agents Chemother 52:3237-43. 2008....
- Citromycetins and bilains A-C: new aromatic polyketides and diketopiperazines from Australian marine-derived and terrestrial Penicillium sppRobert J Capon
Centre for Molecular Biodiversity, Institute for Molecular Bioscience, University of Queensland, St Lucia, Queensland 4072, Australia
J Nat Prod 70:1746-52. 2007..The citromycin polyketides 2 and 4 and the diketopiperazine 15 were weakly cytotoxic...
- Ca2+-independent phospholipase A2 enhances store-operated Ca2+ entry in dystrophic skeletal muscle fibersFrançois Xavier Boittin
Laboratory of Pharmacology, Geneva Lausanne School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, 1211 Geneva 4, Switzerland
J Cell Sci 119:3733-42. 2006..The Ca2+-independent phospholipase A2 pathway therefore appears as an attractive target to reduce excessive Ca2+ influx and subsequent degeneration occurring in dystrophic fibers...
- Kojic acid, a secondary metabolite from Aspergillus sp., acts as an inducer of macrophage activationAna Paula D Rodrigues
Universidade Federal do Par, Instituto de Cincias Biolgicas, Laboratrio de Biologia Estrutural, Belm, Par, Brazil
Cell Biol Int 35:335-43. 2011..The study demonstrates a new role for KA as a macrophage activator...
- Male mice that do not express group VIA phospholipase A2 produce spermatozoa with impaired motility and have greatly reduced fertilityShunzhong Bao
Mass Spectrometry Resource, Division of Endocrinology, Departments of Medicine and of Obstetrics and Gynecology, Washington University School of Medicine, St Louis, Missouri 63110, USA
J Biol Chem 279:38194-200. 2004....
- Role of an endoplasmic reticulum Ca(2+)-independent phospholipase A(2) in oxidant-induced renal cell deathBrian S Cummings
Department of Pharmaceutical Sciences, Medical University of South Carolina, Charleston, South Carolina 29425, USA
Am J Physiol Renal Physiol 283:F492-8. 2002..These results are the first to demonstrate the expression and subcellular localization of an ER-iPLA(2). These results also suggest that ER-iPLA(2) functions to protect against oxidant-induced lipid peroxidation and oncosis...
- Calcium-independent phospholipase A2 modulates cytosolic oxidant activity and contractile function in murine skeletal muscle cellsMing C Gong
Dept of Physiology, Univ of Kentucky Medical Center, 800 Rose St, Lexington, KY 40536, USA
J Appl Physiol 100:399-405. 2006..These findings suggest that constitutively expressed iPLA2 modulates oxidant activity in skeletal muscle fibers by supporting ROS production, thereby influencing contractile properties and fatigue characteristics...
- Deoxyverrucosidin, a novel GRP78/BiP down-regulator, produced by Penicillium spSoo Jin Choo
Laboratory of Antioxidants, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305 333, Korea
J Antibiot (Tokyo) 58:210-3. 2005..and identified it as a down-regulator of the grp78 gene. The structure of 1 was determined by mainly ESI-mass and two-dimensional NMR spectra. 1 dose-dependently inhibited the expression of GRP78 promoter with an IC50 of 30 nM...
- 2-pyrones possessing antimicrobial and cytotoxic activitiesIan J S Fairlamb
Department of Chemistry, University of York, Heslington, York YO10 5DD, UK
Bioorg Med Chem 12:4285-99. 2004..In an effort to identify synthetic 2-pyrones with interesting biological effects, herein we report the synthesis and biological evaluation of 4-substituted-6-..
- Agonist-induced calcium entry correlates with STIM1 translocationKehinde Ross
Dermatological Sciences, Institute of Cellular Medicine, Medical School, Newcastle University, Newcastle upon Tyne, United Kingdom
J Cell Physiol 211:569-76. 2007..Thus by differentially regulating store-refilling after agonist-mediated depletion, LPA and UTP may exert distinct effects on the duration of STIM1 localization at the plasma membrane, and thus, on the magnitude and duration of ACE...
- Inhibition of calcium-independent phospholipase A2 activity in rat hippocampus impairs acquisition of short- and long-term memoryEvelin L Schaeffer
Laboratory of Neuroscience LIM 27, Department and Institute of Psychiatry, Faculty of Medicine, University of Sao Paulo, Brazil
Psychopharmacology (Berl) 181:392-400. 2005..In mice, intraperitoneal injections of a selective iPLA(2) inhibitor impaired spatial learning. Accordingly, reduced cPLA(2) and iPLA(2) activities were found in postmortem hippocampus of patients with Alzheimer's disease...
- Polyenylpyrroles and polyenylfurans from an Australian Isolate of the soil ascomycete Gymnoascus reessiiBenjamin R Clark
Institute for Molecular Biosciences, University of Queensland, QLD 4072, Australia
Org Lett 8:701-4. 2006..Structures were assigned with detailed spectroscopic analysis...
- Inhibition of protein tyrosin phosphatase improves vascular endothelial dysfunctionDhvanit I Shah
Department of Pharmaceutical Sciences and Drug Research, Faculty of Medicine, Punjabi University, Patiala 147002 Punjab, India
Vascul Pharmacol 44:177-82. 2006..Therefore, it may be concluded that BMOV induced inhibition of PTPase may activate eNOS due to opening of ATP sensitive K(+) channels and consequently reduce oxidative stress to improve vascular endothelial dysfunction...
- Cytotoxic flavonoids and alpha-pyrones from Cryptocarya obovataVincent Dumontet
Institut de Chimie des Substances Naturelles, CNRS, 1, Avenue de la Terrasse, 91198 Gif sur Yvette Cedex, France
J Nat Prod 67:858-62. 2004..Obolactone (1) and obochalcolactone (3) display significant activity in in vitro cytotoxic assays against the KB cell line. Biosynthetic pathways for oboflavanones and obochalcolactone are suggested...
- 6-[omega-arylalkenyl]-5,6-dihydro-alpha-pyrones from Cryptocarya moschata (Lauraceae)A J Cavalheiro
Instituto de Quimica, Universidade Estadual Paulista, Araraquara, SP, Brazil
Phytochemistry 53:811-9. 2000Eleven 6-[omega-arylalkenyl]-5,6-dihydro-alpha-pyrones, cryptomoscatones D2, E1, E2, E3 and F1 and cryptopyranmoscatones A1, A2, A3, B1, B2 and B4, in addition to goniothalamin and cryptofolione, were isolated from branch and stem bark ..
- In vitro antiproliferative and cytotoxic activities of novel kojic acid derivatives: 5-benzyloxy-2-selenocyanatomethyl- and 5-methoxy-2-selenocyanatomethyl-4-pyranoneMaria Fickova
Institute of Experimental Endocrinology, Slovak Academy of Sciences, Vlarska 3, 833 07 Bratislava, Slovak Republic
J Appl Toxicol 28:554-9. 2008..Cell growth inhibitory activities of new selenium containing kojic acid derivatives are preferentially aimed at the intracellular compartment rather than the plasma membrane and enlarge the group of antiproliferative active compounds...
- Solanapyrone analogues from a Hawaiian fungicolous fungusLori E Schmidt
Department of Chemistry, University of Iowa, Iowa City, Iowa 52242, USA
J Nat Prod 70:1317-20. 2007..Solanapyrone J (1) showed antifungal activity against Aspergillus flavus and Fusarium verticillioides, while both 1 and 2 showed activity against Staphylococcus aureus and Candida albicans...
- Mixed-ligand copper(II) maltolate complexes: synthesis, characterization, DNA binding and cleavage, and cytotoxicityArchika Barve
Department of Chemistry, University of Pune, Pune 411007, India
Inorg Chem 48:9120-32. 2009..The cytotoxicity of the complexes against HeLa (cervical) cancer cell lines shows that synergy between the metal and ligands results in a significant enhancement in the cell death with IC(50) of approximately 150-270 microg mL(-1)...
- Oxyresveratrol and hydroxystilbene compounds. Inhibitory effect on tyrosinase and mechanism of actionYeon Mi Kim
College of Pharmacy and Research Center for Bioresource and Health, Chungbuk National University, Cheongju 361 763, Korea
J Biol Chem 277:16340-4. 2002..The number and position of hydroxy substituents seem to play an important role in the inhibitory effects of hydroxystilbene compounds on tyrosinase activity...
- Synthesis and anticonvulsant activity of new kojic acid derivativesMutlu Dilsiz Aytemir
Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey
Arzneimittelforschung 60:22-9. 2010....
- Protective role of arzanol against lipid peroxidation in biological systemsAntonella Rosa
Dip Biologia Sperimentale, Sez Patologia Sperimentale, Universita degli Studi di Cagliari, Cittadella Universitaria, SS 554, Km 4 5, 09042 Monserrato, Cagliari, Italy
Chem Phys Lipids 164:24-32. 2011..36×10(-5) and 2.20±0.004×10(-5)cm/s, respectively, suggesting a passive diffusion pathway. The results of the work qualify arzanol as a potent natural antioxidant with a protective effect against lipid oxidation in biological systems...
- Kojic acid-amino acid conjugates as tyrosinase inhibitorsJin Mi Noh
School of Chemical and Biological Engineering, Seoul National University, Seoul 151 744, Republic of Korea
Bioorg Med Chem Lett 19:5586-9. 2009..It also exhibited dopachrome reducing activity. We also propose a new tyrosinase inhibition mechanism based on the docking simulation data...
- One-pot regio- and stereoselective synthesis of α'-methoxy-γ-pyrones: biological evaluation as mitochondrial respiratory complex inhibitorsHelena Rosso
Laboratoire des Fonctions Azotées et Oxygénées Complexes de l IRCOF, CNRS UMR 6014 and FR 3038, Universite de Rouen, Mont Saint Aignan, France
J Org Chem 76:9429-37. 2011The one-pot construction of functionalized α'-methoxy-γ-pyrones is detailed...
- Relative antiviral efficacy of ritonavir-boosted darunavir and ritonavir-boosted tipranavir vs. control protease inhibitor in the POWER and RESIST trialsA Hill
Department of Pharmacology, University of Liverpool, Liverpool, UK
HIV Med 8:259-64. 2007....
- Cytotoxic and antimicrobial metabolites from marine lignicolous fungi, Diaporthe spXin Lin
The Key Laboratory of Ministry of Education of Cell Biology and Tumor Engineering, School of Life Science, Xiamen University, Xiamen 361005, PR China
FEMS Microbiol Lett 251:53-8. 2005..Two known compounds, 7-methoxy-4,6-dimethyl-3H-isobenzofuran-1-one (2) and mycoepoxydiene (3), were also demonstrated to exhibit cytotoxic activities for the first time. All three compounds were assessed for antimicrobial activity...
- Emerging HIV-1 resistance to tipranavir and darunavir in patients with virological failure to first-generation protease inhibitors in TaiwanS M Hsieh
Department of Internal Medicine, National Taiwan University Hospital and National Taiwan UniversityCollege of Medicine, Taipei, Taiwan
Int J STD AIDS 22:617-20. 2011..Our data revealed a significant increase in the levels of genotypic resistance to TPV and DRV over the past two years in patients with virological failure to first-generation PIs...
- Effects of 3-isobutyl-1-methylxanthine and kojic acid on cocultures and skin equivalents composed of HaCaT cells and human melanocytesMarco Springer
BioTeSys GmbH, Schelztorstrasse 54 56, 73728 Esslingen, Germany
Arch Dermatol Res 295:88-91. 2003
- Marinactinones A-C, new γ-pyrones from marine actinomycete Marinactinospora thermotolerans SCSIO 00606Fazuo Wang
Key Laboratory of Marine Bio resources Sustainable Utilization, Research Center for Marine Microbes, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, PR China
J Antibiot (Tokyo) 64:189-92. 2011Three new γ-pyrones named marinactinones A-C (1-3) were isolated from marine-derived actinomycete Marinactinospora thermotolerans SCSIO 00606. These structures were elucidated by extensive spectroscopic methods...
- Efficient synthesis of 5-amido-3-hydroxy-4-pyrones as inhibitors of matrix metalloproteinasesYi Long Yan
Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, California 92093 0358, USA
Org Lett 9:2517-20. 20073-hydroxy-4-pyrones are a class of important metal chelators with versatile medicinal applications. An efficient pathway for the preparation of new 5-amido-3-hydroxy-4-pyrone derivatives has been developed...
- Phaeochromycins A-E, anti-inflammatory polyketides isolated from the soil actinomycete Streptomyces phaeochromogenes LL-P018Edmund I Graziani
Department of Chemical and Screening Sciences, Wyeth Research, 401 N Middletown Road, Pearl River, New York 10965, USA
J Nat Prod 68:1262-5. 2005..Phaeochromycin D (4) is an unusual partially cyclized degraded octaketide intermediate...
- Three dimeric naphtho-γ-pyrones from the mangrove endophytic fungus Aspergillus tubingensis isolated from Pongamia pinnataHong Bo Huang
School of Chemistry and Chemical Engineering, Sun Yat Sen University, Guangzhou, P R China
Planta Med 76:1888-91. 2010Three new dimeric naphtho-γ-pyrones, named rubasperone A (1), rubasperone B (2), and rubasperone C (3), together with two known compounds, rubrofusarin (4) and rubrofusarin B (5), were isolated from the mangrove endophytic fungus ..
- Bromoenol lactone promotes cell death by a mechanism involving phosphatidate phosphohydrolase-1 rather than calcium-independent phospholipase A2Lucia Fuentes
Institute of Molecular Biology and Genetics, University of Valladolid School of Medicine, E 47005 Valladolid, Spain
J Biol Chem 278:44683-90. 2003....
- Isolation, Structure elucidation, and antimycobacterial properties of dimeric naphtho-gamma-pyrones from the marine-derived fungus Aspergillus carbonariusYapeng Zhang
Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, PR China
Chem Biodivers 5:93-100. 2008Two new dimeric naphtho-gamma-pyrones, compounds 1 and 2, were isolated from the AcOEt extract of the fungal strain WZ-4-11 of Aspergillus carbonarius, together with eight known analogues, including 10,10'-bifonsecin B (3), 6'-O-..
- Mycoepoxydiene, a fungal polyketide, induces cell cycle arrest at the G2/M phase and apoptosis in HeLa cellsJifeng Wang
Key Laboratory of the Ministry of Education for Cell Biology and Tumor Cell Engineering, School of Life Sciences, Xiamen University, Xiamen, Fujian, China
Bioorg Med Chem Lett 20:7054-8. 2010..This study is the first report demonstrating the action mechanism of MED against tumor cell growth. These results provide the potential of MED as a novel low toxic antitumor agent...
- Peritoneal dialysis solutions low in glucose degradation products--evidence for clinical benefitsTadashi Tomo
Faculty of Medicine, Second Department of Internal Medicine, Oita University, Yufu, Japan
Perit Dial Int 28:S123-7. 2008....
- Inhibition of the Rho GTPase, Rac1, decreases estrogen receptor levels and is a novel therapeutic strategy in breast cancerADENA E ROSENBLATT
Department of Molecular and Cellular Pharmacology, University of Miami Miller School of Medicine, 1600 Northwest 10th Avenue R 189, Miami, Florida 33136, USA
Endocr Relat Cancer 18:207-19. 2011....
- A nonspecific phosphotyrosine phosphatase inhibitor, bis(maltolato)oxovanadium(IV), improves glucose tolerance and prevents diabetes in Zucker diabetic fatty ratsCarol L Winter
Department of Metabolism Biology, Procter and Gamble Pharmaceuticals, 8700 Mason Montgomery Road, Box 1070, Mason, Ohio, 45040
Exp Biol Med (Maywood) 230:207-16. 2005..These data demonstrate that phosphatase inhibition offers a new approach to diabetes prevention, one that may have advantages over current approaches...
- Virologic and immunologic effectiveness of tipranavir/ritonavir (TPV/r)- versus darunavir/ritonavir (DRV/r)-based regimens in clinical practiceTony Antoniou
University of Toronto, Toronto, Ontario, Canada, Maple Leaf Medical Clinical, Toronto, Ontario, Canada
J Int Assoc Physicians AIDS Care (Chic) 9:382-9. 2010....
- Food and Drug Administration analysis of tipranavir clinical resistance in HIV-1-infected treatment-experienced patientsLisa K Naeger
Division of Antiviral Products, Center for New Drug Evaluation, Food and Drug Administration, Silver Spring, Maryland, USA
AIDS 21:179-85. 2007..To assess the resistance profile of tipranavir...
- Regioselective synthesis of kojic acid esters by Bacillus subtilis proteaseTakao Raku
New Energy and Industrial Technology Development Organization, Tsukuba Central 6, 1 1 1 Higashi, Tsukuba, Ibaraki, 305 8566, Japan
Biotechnol Lett 25:969-74. 2003..The kojic acid esters had radical scavenging activities, inhibited tyrosinase activity and was biodegradable...
- Antinociceptive properties of coumarins, steroid and dihydrostyryl-2-pyrones from Polygala sabulosa (Polygalaceae) in miceFlavia Carla Meotti
Departamento de Quimica, Universidade Federal de Santa Maria, 97110 000, Santa Maria, RS Brazil
J Pharm Pharmacol 58:107-12. 2006..The isolated compounds dihydrostyryl-2-pyrones (1, 2, 3), styryl-2-pyrone (7), alpha-spinasterol (9), scopoletin (10) and two esters of the coumarin (scopoletin)..
- Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPasesAdam Shutes
Lineberger Comprehensive Cancer Center, University of North Carolina, Chapel Hill, North Carolina 27599, USA
J Biol Chem 282:35666-78. 2007..Taken together, our results suggest that EHT 1864 selectively inhibits Rac downstream signaling and transformation by a novel mechanism involving guanine nucleotide displacement...
- Tyrosinase inhibition by extracts and constituents of Sideroxylon inerme L. stem bark, used in South Africa for skin lighteningS Momtaz
Department of Plant Science, University of Pretoria, Pretoria 0002, South Africa
J Ethnopharmacol 119:507-12. 2008..To investigate the stem bark of Sideroxylon inerme L. and its compounds for tyrosinase-inhibition activity and to evaluate the mechanism involved of the most potent compounds in tyrosinase inhibition...
- Identification of a small molecule inhibitor of Sir2pA Bedalov
Divisions of Clinical Research, Basic Sciences, and Human Biology, Fred Hutchinson Cancer Research Center, 1100 Fairview Avenue North, Seattle, WA 98109, USA
Proc Natl Acad Sci U S A 98:15113-8. 2001..By using splitomicin as a chemical genetic probe, we demonstrate that continuous HDA of Sir2p is required for maintaining a silenced state in nondividing cells...
- Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasionSarah E Golding
Department of Radiation Oncology, Virginia Commonwealth University, Richmond, VA 23298 0058, USA
Mol Cancer Ther 8:2894-902. 2009..Altogether, KU-60019 inhibits the DNA damage response, reduces AKT phosphorylation and prosurvival signaling, inhibits migration and invasion, and effectively radiosensitizes human glioma cells...
- Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinaseOlga Göransson
Division for Diabetes, Metabolism and Endocrinology, Department of Experimental Medical Science, Lund University, Lund, Sweden
J Biol Chem 282:32549-60. 2007..We propose that this direct and specific AMPK activator will be a valuable experimental tool to understand the physiological roles of AMPK...
- Steady-state disposition of the nonpeptidic protease inhibitor tipranavir when coadministered with ritonavirLinzhi Chen
Departments of Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc, Ridgefield, Connecticut 06877, USA
Antimicrob Agents Chemother 51:2436-44. 2007..In conclusion, after the coadministration of TPV and RTV, unchanged TPV represented the primary form of circulating and excreted TPV and the primary extraction route was via the feces...
- 3-O-methylfunicone, a secondary metabolite produced by Penicillium pinophilum, induces growth arrest and apoptosis in HeLa cellsE Buommino
Department of Experimental Medicine, Section of Microbiology and Clinical Microbiology, Second University of Naples, Italy
Cell Prolif 37:413-26. 2004..The capacity of the compound to affect the cell cycle and to modulate apoptosis is indicative of a potential for the development of a new agent for cancer chemotherapy...
- Drug toxicity, HIV progression, or comorbidity of aging: does tipranavir use increase the risk of intracranial hemorrhage?Amy C Justice
Veterans Affairs Connecticut Healthcare System, West Haven, Connecticut 06516, USA
Clin Infect Dis 47:1226-30. 2008..We studied 2 large cohorts to estimate the background rate of intracranial hemorrhage and compared it with rates reported among persons who had been exposed to tipranavir...
- Detailed reaction mechanism of macrophomate synthase. Extraordinary enzyme catalyzing five-step transformation from 2-pyrones to benzoatesK Watanabe
Department of Applied Bioscience, Graduate School of Agriculture, Hokkaido University, Sapporo 060 8589, Japan
J Biol Chem 275:38393-401. 2000..Incubation of the stereospecifically deuterium-labeled malate with 2-pyrones in the presence of malate dehydrogenase provided information for the stereochemical course of the reaction ..
- Total synthesis of alpha-pyrone meroterpenoids, novel bioactive microbial metabolitesToshiaki Sunazuka
Kitasato Institute for Life Sciences, Kitasato University, and The Kitasato Institute, Shirokane, Minato ku, Japan
Chem Rev 105:4559-80. 2005
- A role for phospholipase A2 activity in membrane tubule formation and TGN traffickingJohn A Schmidt
Department of Molecular Biology and Genetics, Cornell University, Ithaca, NY 14853, USA
Traffic 11:1530-6. 2010..Thus, PLA(2) enzymes appear to have an important role in the earliest steps of membrane tubule formation at the TGN, which are utilized for membrane trafficking...
- Group VIA calcium-independent phospholipase A2 mediates endothelial cell S phase progressionShane P Herbert
Faculty of Biological Sciences, Institute of Molecular and Cellular Biology, University of Leeds, Leeds LS2 9JT, United Kingdom
J Biol Chem 281:35709-16. 2006..Consequently, iPLA2-VIA is a novel regulator of endothelial cell S phase progression, cell cycle residence, and angiogenesis...
- 2-Pyrone natural products and mimetics: isolation, characterisation and biological activityGerard P McGlacken
Department of Chemistry, University of York, Heslington, York, UK YO10 5DD
Nat Prod Rep 22:369-85. 2005..An emphasis has been placed upon the biological activity associated with 2-pyrones, particularly with respect to potential therapeutic or anti-microbial agents...
- Pharmacokinetics, safety, and efficacy of tipranavir boosted with ritonavir alone or in combination with other boosted protease inhibitors as part of optimized combination antiretroviral therapy in highly treatment-experienced patients (BI Study 1182.51)Sharon L Walmsley
Division of Clinical Investigation and Human Physiology, University of Toronto, Toronto, ON, Canada
J Acquir Immune Defic Syndr 47:429-40. 2008..Given the limited treatment options for patients with high-level resistance, antiretroviral (ARV) regimens based on concomitant use of 2 ritonavir (RTV)-boosted protease inhibitors (PIs) were considered a therapeutic option...
- Methoxy poly(ethylene glycol)-block-poly(delta-valerolactone) copolymer micelles for formulation of hydrophobic drugsHelen Lee
Leslie Dan Faculty of Pharmacy, Department of Pharmaceutical Sciences, and Faculty of Applied Science and Engineering, Division of Engineering Science, University of Toronto, 19 Russell St, Toronto, Ontario, Canada M5S 2S2
Biomacromolecules 6:3119-28. 2005..The present study indicates that the MePEG-b-PVL copolymers are suitable biomaterials for hydrophobic drug formulation and delivery...
- New beginnings for matrix metalloproteinase inhibitors: identification of high-affinity zinc-binding groupsDavid T Puerta
Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, California 92093, USA
J Am Chem Soc 126:8388-9. 2004..These results demonstrate that MPIs based on new ZBGs are feasible and may indeed improve the overall performance of inhibitors designed against these important medicinal targets...
- Significant effects of tipranavir on platelet aggregation and thromboxane B2 formation in vitro and in vivoJochen Graff
Pharmazentrum Frankfurt, Institute of Clinical Pharmacology at the Johann Wolfgang Goethe University Frankfurt, Germany
J Antimicrob Chemother 61:394-9. 2008..Recently, the FDA published a warning concerning intracranial haemorrhage in patients taking the HIV-1 protease inhibitor tipranavir co-administered with ritonavir...
- Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone familyMatthew J Sanders
Cellular Stress Group, Medical Research Council Clinical Sciences Centre, Hammersmith Hospital, Imperial College, DuCane Road, London, United Kingdom
J Biol Chem 282:32539-48. 2007..Importantly, this model may provide clues for understanding the mechanism by which AMP leads to activation of AMPK, which in turn may help in the identification of other AMPK activators...
- Inhibition of phospholipase A2 reduces neurite outgrowth and neuronal viabilityOrestes V Forlenza
Laboratory of Neuroscience LIM 27, Department and Institute of Psychiatry, Faculty of Medicine, University of Sao Paulo, Rua Dr Ovidio Pires de Campos s n, 05403 010 Sao Paulo, Brazil
Prostaglandins Leukot Essent Fatty Acids 76:47-55. 2007..We conclude that the functional integrity of both calcium-dependent and calcium-independent cytosolic PLA2 is necessary for the in vitro development of cortical and hippocampal neurons...
- Tipranavir: a ritonavir-boosted protease inhibitorKatherine F Croom
Adis International Limited, Auckland, New Zealand
Drugs 65:1669-77; discussion 1678-9. 2005..The most common adverse events in clinical trials of tipranavir were gastrointestinal. The incidence of treatment discontinuation because of adverse events in the RESIST trials was 8% (pooled data)...
- Tipranavir: the first nonpeptidic protease inhibitor for the treatment of protease resistanceBeatriz Luna
Wingate University School of Pharmacy, Wingate, North Carolina, USA
Clin Ther 29:2309-18. 2007..TPV exhibits a resistance profile distinct from that of other currently available PIs, making it a potential option for treatment experienced patients with resistance to multiple Pls...
- Metal complexes of maltol and close analogues in medicinal inorganic chemistryKatherine H Thompson
Medicinal Inorganic Chemistry Group, Chemistry Department, University of British Columbia, Vancouver, BC, Canada V6T 1Z1
Chem Soc Rev 35:545-56. 2006..The most widely investigated for medicinal applications are the 3-hydroxy-4-pyrones and the 1,2- 3,2- and 3,4-hydroxypyridinones...
- Loss of mitochondrial transmembrane potential and caspase-9 activation during apoptosis induced by the novel styryl-lactone goniothalamin in HL-60 leukemia cellsS H Inayat-Hussain
Department of Biomedical Science, Faculty of Allied Health Sciences, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz 50300, Kuala Lumpur, Malaysia
Toxicol In Vitro 17:433-9. 2003..FMK) abrogated apoptosis as assessed by all of the apoptotic features in this study. In summary, our results demonstrate that goniothalamin-induced apoptosis occurs via the mitochondrial pathway in a caspase dependent manner...
- A novel tricyclic pyrone compound ameliorates cell death associated with intracellular amyloid-beta oligomeric complexesIzumi Maezawa
MIND Institute and Department of Pathology, University of California Davis, Sacramento, California, USA
J Neurochem 98:57-67. 2006..CP2 analogs represent a new class of promising compounds for the amelioration of Abeta toxicities within both intracellular and extracellular sites...
- Novel tricyclic pyrone compounds prevent intracellular APP C99-induced cell deathLee Way Jin
Department of Pathology, University of Washington, Seattle 98195 7470, USA
J Mol Neurosci 19:57-61. 2002..Lead compounds will now be selected for their abilities to ameliorate A beta/CTF-mediated pathology in transgenic mice. Our hope is that these compounds may eventually prove beneficial for the prevention and treatment of AD...
- Novel alpha-pyrones produced by a marine Pseudomonas sp. F92S91: taxonomy and biological activitiesMaya P Singh
Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA
J Antibiot (Tokyo) 56:1033-44. 2003..Culture F92S91, later identified as a Pseudomonas sp. based on 16S profiling, was found to produce two alpha-pyrones (I and II) and three high molecular weight peptides...
- Goniothalamin induces apoptosis in vascular smooth muscle cellsK M Chan
Department of Biomedical Science, Faculty of Allied Health Sciences, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia
Chem Biol Interact 159:129-40. 2006..Moreover, GN effects were comparable to rapamycin. In conclusion, our data show that GN initially induces DNA damage which subsequently leads to cytotoxicity primarily via apoptosis in VSMCs...
- The clinical development of new mitotic inhibitors that stabilize the microtubuleSridhar Mani
Departments of Medicine and Oncology, Albert Einstein College of Medicine, Montefiore and Jacobi Medical Center, Bronx, NY, USA
Anticancer Drugs 15:553-8. 2004..There is now considerable data regarding the efficacy of the epothilones in human beings and discodermolide holds such promise, as well...
- The structure activity relationship of discodermolide analoguesSimon J Shaw
Kosan Biosciences, Inc 3832 Bay Center Place, Hayward, CA 94545, USA
Mini Rev Med Chem 8:276-84. 2008..The majority of analogues have been generated via modification of the lactone region. This suggests that significant simplifications can be made in this region provided that the lactone moiety is maintained...
- Goniothalamin induces cell cycle-specific apoptosis by modulating the redox status in MDA-MB-231 cellsWen Ying Chen
Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung City, Taiwan
Eur J Pharmacol 522:20-9. 2005....
- Synergistic suppression of microtubule dynamics by discodermolide and paclitaxel in non-small cell lung carcinoma cellsStephane Honore
FRE CNRS 2737, Universite de la Mediterranee, Marseille, France
Cancer Res 64:4957-64. 2004....
- Enantioselective synthesis of apoptolidinone: exploiting the versatility of thiazolidinethione chiral auxiliariesMichael T Crimmins
Department of Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599 3290, USA
J Am Chem Soc 127:13810-2. 2005..A cross-metathesis reaction is utilized to assemble the C1-C10 trieneoate fragment and the C11-C28 polypropionate region of the molecule...
- Ca2+-independent phospholipase A2 is a novel determinant of store-operated Ca2+ entryTarik Smani
Boston University School of Medicine, Boston, Massachusetts 02118, USA
J Biol Chem 278:11909-15. 2003..Thus, functional iPLA(2) is required for activation of store-operated channels and capacitative Ca(2+) influx in wide variety of cell types...
- Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout ScreeningRICHARD LAROCK; Fiscal Year: 2009..to prepare specially diverse libraries of indoles, benzofurans, benzopyrans, coumarins, isocoumarins, phthalides, pyrones, 2-quinolones, pyridines, isoquinolin-1-ones, isoindolin-1-ones, isoquinolines, carbolines, isoindolo[2,1-a]..
- Structural Facets of the Inhibition of Alzheimer's Amyloid-beta Oligomers by TricNathan A Oyler; Fiscal Year: 2012..A class of small organic compounds has been discovered, namely tricyclic pyrones (TP), such as CP2 (code name), that prevents the death of human neuroblastoma MC65 cells related to intracellular ..
- ASYMMETRIC SYNTHESIS OF PHYSIOLOGICALLY ACTIVE COMPOUNDSGary Posner; Fiscal Year: 1992..understanding of asymmetric inverse-electron-demand Diels-Alder cycloadditions between electron-deficient pyrones and pyridones and electron-rich dienophiles...
- Total Synthesis of Biologically Active Gamma-PyronesDirk Trauner; Fiscal Year: 2007..In a further contribution to synthetic methodology, new approaches towards gamma-pyrones are proposed...
- Transition Metal Mediated Routes to Heterocycles and CarbocyclesJanis Louie; Fiscal Year: 2009..involving nickel-based catalysts for mediating carbon dioxide/diyne and isocyanate/diyne annulations to produce 2-pyrones and 2-pyridones, respectively...
- Inhibition of Alzheimer's Beta-Amyloid Fibril FormationDuy Hua; Fiscal Year: 2009..In search of a compound that blocks this conformational change, we discovered that a class of tricyclic pyrones (TP), especially CP2 (code name), prevents the death of human neuroblastoma MC65 cells related to intracellular ..
- SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTSAMOS SMITH; Fiscal Year: 2007..abstract_text> ..
- NMR systems : 2 Bruker Avance 500 ConsolesAMOS 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]..
- SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORSAMOS SMITH; Fiscal Year: 2001..abstract_text> ..
- Design and Synthesis of HIV-1 Protease InhibitorsAMOS SMITH; Fiscal Year: 2004....
- ASYMMETRIC SYNTHESIS OF ANTITUMOR AGENTSMICHAEL CRIMMINS; Fiscal Year: 2005..Laulimalide stimulates tubulin polymerization more effectively than paclitaxel. Laulimalide is a representative of a new class of microtubule stabilizing agents with promise for therapeutic potential. ..
- Natural Product Leads for Drug DevelopmentKATHLYN PARKER; Fiscal Year: 2009..Molecular modeling will allow the design of candidates for more active drugs. Candidates will be evaluated in the squalene synthase assay. Collaborations for the medicinal chemistry components of the project have been arranged. ..
- STRATEGIES AND METHODS IN SYNTHESIS OF NATURAL PRODUCTSKATHLYN PARKER; Fiscal Year: 2003..During the period which corresponds to this proposal, we plan to apply our new methodology to the synthesis of deacetylravidomycin and kidamycin, representatives of the remaining two major classes. ..
- ASYMMETRIC SYNTHESIS OF NOVEL NATURAL PRODUCTSMICHAEL CRIMMINS; Fiscal Year: 2006..Synthesis of the biologically active agents guanacastepene, and SCH 351448 will also be pursued. ..
- Micromass LCT Mass SpectrometerMICHAEL CRIMMINS; Fiscal Year: 2004..The major users group is highly dependent on rapid turn around mass spectral data. Since there is currently no Departmental mass spectrometry facility, the research programs of the major users have been seriously hampered for some time. ..
- Synthesis of Tumor Inhibitory Marine Natural ProductsJames Marshall; Fiscal Year: 2004..The main chemical issues to be addressed include the control of stereochemistry by means of chiral organometal chemistry and the design of new and efficient routes to structurally novel natural products. ..
- Novel antibacterial agents for treatment of TularemiaNachum Kaplan; Fiscal Year: 2004..tularensis microbiological data and animal model data to warrant inclusion of the information on the product label as a narrow spectrum agent that could be used in the event of a F. tularensis release. ..
- SYNTHESIS OF ANNONACEOUS ACETOGENINS AND ANALOGUESJames Marshall; Fiscal Year: 2001..The synthetic approach will employ chiral allylic and allenic organometal reagents to introduce stereogenic centers with concurrent formation of carbon-carbon bonds. ..
- 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. ..
- Understanding and Altering the Virologic SetpointMartin Markowitz; Fiscal Year: 2006..abstract_text> ..
- Cellular Targets for Gallium Compounds in LymphomaChristopher Chitambar; Fiscal Year: 2008..Our studies will provide new information regarding: a) the impact of HFE mutations on the response of lymphoma to gallium, and, b) the mechanism of action of gallium at the mitochondrial level. ..
- FLUOROUS METHODS FOR TRADITIONAL AND PARALLEL SYNTHESISDENNIS CURRAN; Fiscal Year: 2003..In short, the work will help to move the very young field of fluorous chemistry from infancy into childhood. ..
- Purchase of a 600 MHz NMR Spectrometer with CryoprobeDENNIS CURRAN; Fiscal Year: 2007..This research often requires sophisticated NMR experiments on small samples, and the requested 600 MHz spectrometer will greatly expedite ongoing and planned work. [unreadable] [unreadable] [unreadable]..
- Molecular Target Focused Discovery of Anticancer DrugsGEORGE PETTIT; Fiscal Year: 2007..In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs direct at improving human cancer treatments. ..
- Molecular Target Focused Discovery of Anticancer DrugsGeorge R Pettit; Fiscal Year: 2010....
- RADICAL REACTIONS FOR NATURAL PRODUCTSDENNIS CURRAN; Fiscal Year: 2002....
- The Transmission and Fitness of Drug Resistant HIV-1MARTIN H MARKOWITZ; Fiscal Year: 2011..abstract_text> ..
- Host Polymorphisms and Uncomplicated MalariaSunil Parikh; Fiscal Year: 2008..Parikh will be able to utilize modern molecular epidemiology techniques to investigate human genetic factors underlying susceptibility to malaria and he will be well equipped for a career in academic research. ..
- STRATEGIES FOR CONTEXT SPECIFIC ANTICANCER THERAPIESJulian Simon; Fiscal Year: 2002..Together, the studies outlined in our Specific Aims, will constitute the first step in testing the hypothesis of context-specific toxicity in cancer chemotherapy. ..
- SYNTHESIS OF NOVEL BIOLOGICALLY ACTIVE NATURAL PRODUCTSROBERT BOECKMAN; Fiscal Year: 2002..The hypothesis that an internal chelate of suitably disposed oxygen functions permits the modification of the ring conformation from half-chair to half-boat will be tested. ..
- Azinomycins - Total Synthesis and Mechanism of ActionRobert Coleman; Fiscal Year: 2007..abstract_text> ..
- Midcareer Investigator Award /Patient-Oriented ResearchCharles Hicks; Fiscal Year: 2008..unreadable] [unreadable]..
- Epothilone Analogs by Partial Chemical SynthesisDavid Myles; Fiscal Year: 2002..The proposed epothilone analogs with increased solubility will have a potentially competitive advantage for a $2 billion per year market for the treatment of breast, lung and ovarian cancers. ..
- NOVEL DOUBLE STRAND BREAK PRODUCING COMPOUNDSJulian Simon; Fiscal Year: 2001..The yeast experiments will involve both classical genetic approaches and genome-wide analyses based on DNA microarray technology. ..
- Theory of the Chemistry of NO, HNO, OONO-, and RSNOKENDALL HOUK; Fiscal Year: 2009..The success of the research described here can lead to new tools for study of physiological processes and drugs for hypertension, cardiac failure, and other biological processes involving NO metabolism. ..
- Synthetic Reactions Catalyzed by Transition MetalsEi ichi Negishi; Fiscal Year: 2010..Being considered for this purpose are discodermolide, hennoxazole A, zincophorin, roselipins, apoptolidin, nafuredin, caIlystatin A, milbemycin p3, calyculin A, and amphotericin B. ..
- Biosynthesis of Hypotensive Phosphonopeptide Natural ProductsBrian O Bachmann; Fiscal Year: 2010..Metalloproteinase inhibitors have potential to treat a large number of human illnesses including hypertension, cancer and osteoarthritis, among others. ..
- CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTSDavid Williams; Fiscal Year: 2009..Daphnicyclidin A. This recent discovery has revealed a new molecular architecture which exhibits significant antitumor activity. Our research will investigate strategies for chemical synthesis of these complex polycyclic systems. ..
- Inhibitors of Hedgehog Signaling For Brain Cancer ChemotherapyJEFFREY D contact WINKLER; Fiscal Year: 2010..The studies outlined herein therefore hold the promise of developing important new tools in cancer biology and new drug candidates for the treatment of brain cancers. ..
- Regulation of vascular smooth muscle calcium sensitivityPaul H Ratz; Fiscal Year: 2010..The Specific Aim of this study will be to test the hypothesis that ROK and PKCzeta both mediate KCI- induced Ca sensitization of FA, and that iPLA2 and PI3K are required as upstream activators of ROK and PKCzeta. ..
- Novel Ribostamycins and SAR Study of Ring III AminosugarCheng Wei Chang; Fiscal Year: 2008..unreadable] [unreadable]..
- Induction of Autophagy in Human Macrophages by LipopolysaccharideBeatrice Haimovich; Fiscal Year: 2008..To determine whether LPS-induced mitochondrial dysfunction results in HMDM autophagy. Aim 2. To determine whether autophagy enhances the resistance of LPS-treated HMDM to Gram-negative bacteria. ..
- Immunity in Early Syphillis: Pathway to HIV CoinfectionJuan Salazar; Fiscal Year: 2007..In Aim 2 we will study the effect of secondary syphilis on viral load (VL) in HIV co-infected individuals. In this aim we will compare VL between HIV patients with and without syphilis and determine the effect of penicillin on VL. ..
- Nociception in Diabetic Neuropathy: Role of EndothelinsLiliana Berti Mattera; Fiscal Year: 2004..abstract_text> ..
- BASIS FOR ALCOHOL AND COCAINE STROKES--ROLE OF MG2+Burton Altura; Fiscal Year: 2004..An understanding of how ethanol and cocaine induce strokes may ultimately suggest new targets for pharmacologic manipulation, and thus, improving the clinical outcome after "binge- drinking" or cocaine intoxication. ..
- Efficient synthesis of discodermolideGary Ashley; Fiscal Year: 2005..abstract_text> ..
- CaBP4, a Photoreceptor Specific Calcium-Binding ProteinFrancoise Haeseleer; Fiscal Year: 2005..The mechanism of interaction of CaBP4 with its target will also be examined using both in vitro and in vivo procedures. ..
- NEW DEVELOPMENTS IN ORGANOCOPPER CHEMISTRYR Dieter; Fiscal Year: 2004..The proposed synthetic routes to pyrrolidine aza sugars will develop the potential synthetic power of alpha-aminoalkylcuprate chemistry. ..
- MECHANISM OF PLATELET ACTIVATION ON MATRIX PROTEINSBeatrice Haimovich; Fiscal Year: 2004..phosphatase(s) and kinase(s) regulate the state of phosphorylation of a-actinin? Aim 3: What is the role of tyrosine phosphorylation of pplOl and vinculin, and which phosphatase(s) and kinase(s) regulate these phosphorylation events? ..
- New mitosis specific anticancer agentsJulian Simon; Fiscal Year: 2005..Through these convergent studies we hope to identify new mitosis-specific anticancer agents, their targets and the contexts in which these compounds are most effective. ..
- SYNTHETIC STUDIES RELATED TO CANCER RESEARCH/TREATMENTPaul Wender; Fiscal Year: 2005..Overall, this research program is expected to be of significant value in chemistry, biology, and medicine. ..
- Irreversible inhibitors of cholesterol esteraseLORRAINE DECK; Fiscal Year: 2005....
- Apoptosis and transport mechanisms in neurodegenerationDavid DeWitt; Fiscal Year: 2002..Cytoskeletal abnormalities including tau phosphorylation, neurofilament accumulation, and microtubule disruption will be examined to determine whether these changes. ..
- Motilin Receptor Agonists for Diabetic GastroperesisDavid Myles; Fiscal Year: 2005....
- Asymmetric Synthesis of Cytotoxic Natural ProductsRobert Coleman; Fiscal Year: 2005..abstract_text> ..
- INTERESTING BIOACTIVE SUBSTANCESDavid Williams; Fiscal Year: 2006..The selective synthesis of contiguous stereotriads will advance basic methodology for asymmetric conjugate additions. ..
- ANTIRETROVIRAL PHARMACOLOGY IN THE GENITAL TRACTAngela Kashuba; Fiscal Year: 2007..abstract_text> ..
- Vinylogous Amide Photochemistry in Organic SynthesisJeffrey Winkler; Fiscal Year: 2005..abstract_text> ..
- REGULATION OF DETRUSOR SMOOTH MUSCLE CONTRACTIONPAUL RATZ; Fiscal Year: 2005..Collectively, these studies will provide new insights into the cellular mechanisms regulating DSM contractions. ..
- ACYCLIC STEREOCONTROL IN RADICAL REACTIONSMUKUND SIBI; Fiscal Year: 2007..3. The conversion of readily available pyrones to chiral pyran building blocks, a common skeleton found in marine natural products with potent biological ..
- SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATESMichael Jung; Fiscal Year: 2003....