heterocyclic bicyclo compounds

Summary

Summary: A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)

Top Publications

  1. ncbi Pharmacologic activation of p53 elicits Bax-dependent apoptosis in the absence of transcription
    Jerry E Chipuk
    Division of Cellular Immunology, La Jolla Institute for Allergy and Immunology, San Diego, CA 92121, USA
    Cancer Cell 4:371-81. 2003
  2. ncbi Latrunculin B-induced plant dwarfism: Plant cell elongation is F-actin-dependent
    F Baluska
    Zellbiologie der Pflanzen, Botanisches Institut, Rheinisch Friedrich Wilhems Universität Bonn, D 53115, Germany
    Dev Biol 231:113-24. 2001
  3. ncbi Functional interactions between the p35 subunit of the Arp2/3 complex and calmodulin in yeast
    C Schaerer-Brodbeck
    Biozentrum of the University of Basel, CH 4056 Basel, Switzerland
    Mol Biol Cell 11:1113-27. 2000
  4. ncbi Restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound
    Vladimir J N Bykov
    Karolinska Institutet, Department of Oncology Pathology, Cancer Center Karolinska, Karolinska Hospital, Stockholm, Sweden
    Nat Med 8:282-8. 2002
  5. ncbi Role of actin in anchoring postsynaptic receptors in cultured hippocampal neurons: differential attachment of NMDA versus AMPA receptors
    D W Allison
    Department of Cell and Structural Biology, University of Illinois, Urbana, Illinois 61801, USA
    J Neurosci 18:2423-36. 1998
  6. ncbi Effects of cytochalasin D and latrunculin B on mechanical properties of cells
    T Wakatsuki
    Department of Biochemistry and Molecular Biophysics, Washington University School of Medicine, St. Louis, MO 63110, USA
    J Cell Sci 114:1025-36. 2001
  7. ncbi Differential organelle movement on the actin cytoskeleton in lily pollen tubes
    Alenka Lovy Wheeler
    Department of Biology and Plant Biology Graduate Program, Morrill Science Center III, University of Massachusetts, Amherst, Massachusetts 01003, USA
    Cell Motil Cytoskeleton 64:217-32. 2007
  8. ncbi Intracellular gonadotropin-releasing hormone receptors in breast cancer and gonadotrope lineage cells
    Kathleen R Sedgley
    Laboratories for Integrative Neuroscience and Endocrinology, University of Bristol, Dorothy Hodgkin Building, Whitson Street, Bristol BS1 3NY, UK
    J Endocrinol 191:625-36. 2006
  9. ncbi Phencyclidine-induced cognitive deficits in mice are improved by subsequent subchronic administration of the novel selective alpha7 nicotinic receptor agonist SSR180711
    Kenji Hashimoto
    Division of Clinical Neuroscience, Chiba University Center for Forensic Mental Health, Chiba, Japan
    Biol Psychiatry 63:92-7. 2008
  10. ncbi Dementia rating and nicotinic receptor expression in the prefrontal cortex in schizophrenia
    Carmen M Martin-Ruiz
    Institute for Ageing and Health, Newcastle General Hospital, Newcastle upon Tyne, United Kingdom
    Biol Psychiatry 54:1222-33. 2003

Research Grants

  1. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 2007
  2. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2006
  3. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2003
  4. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 1991
  5. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2007
  6. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2001
  7. NOVEL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    Frank Carroll; Fiscal Year: 2001
  8. Development of Pharmacotherapies for Nicotine Addiction
    Frank Carroll; Fiscal Year: 2005
  9. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2009
  10. Design and Development of Pharmacotherapies for Treating Stimulant Abuse
    Frank Ivy Carroll; Fiscal Year: 2010

Detail Information

Publications204 found, 100 shown here

  1. ncbi Pharmacologic activation of p53 elicits Bax-dependent apoptosis in the absence of transcription
    Jerry E Chipuk
    Division of Cellular Immunology, La Jolla Institute for Allergy and Immunology, San Diego, CA 92121, USA
    Cancer Cell 4:371-81. 2003
    ..Hence, pharmacologic p53 modulators can activate a transcription-independent apoptotic program...
  2. ncbi Latrunculin B-induced plant dwarfism: Plant cell elongation is F-actin-dependent
    F Baluska
    Zellbiologie der Pflanzen, Botanisches Institut, Rheinisch Friedrich Wilhems Universität Bonn, D 53115, Germany
    Dev Biol 231:113-24. 2001
    ..In conclusion, F-actin is essential for the plant cell elongation, while this F-actin-dependent cell elongation is not an essential feature of plant-specific developmental programs...
  3. ncbi Functional interactions between the p35 subunit of the Arp2/3 complex and calmodulin in yeast
    C Schaerer-Brodbeck
    Biozentrum of the University of Basel, CH 4056 Basel, Switzerland
    Mol Biol Cell 11:1113-27. 2000
    ..This is the first report linking Arp2/3 complex function with calmodulin through which it exercises at least one of its endocytic functions...
  4. ncbi Restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound
    Vladimir J N Bykov
    Karolinska Institutet, Department of Oncology Pathology, Cancer Center Karolinska, Karolinska Hospital, Stockholm, Sweden
    Nat Med 8:282-8. 2002
    ..In vivo studies in mice revealed an antitumor effect with no apparent toxicity. This molecule may serve as a lead compound for the development of anticancer drugs targeting mutant p53...
  5. ncbi Role of actin in anchoring postsynaptic receptors in cultured hippocampal neurons: differential attachment of NMDA versus AMPA receptors
    D W Allison
    Department of Cell and Structural Biology, University of Illinois, Urbana, Illinois 61801, USA
    J Neurosci 18:2423-36. 1998
    ....
  6. ncbi Effects of cytochalasin D and latrunculin B on mechanical properties of cells
    T Wakatsuki
    Department of Biochemistry and Molecular Biophysics, Washington University School of Medicine, St. Louis, MO 63110, USA
    J Cell Sci 114:1025-36. 2001
    ..This study shows a strong dependence of the mechanical properties of cells and tissues on the organization and degree of polymerization of actin filaments...
  7. ncbi Differential organelle movement on the actin cytoskeleton in lily pollen tubes
    Alenka Lovy Wheeler
    Department of Biology and Plant Biology Graduate Program, Morrill Science Center III, University of Massachusetts, Amherst, Massachusetts 01003, USA
    Cell Motil Cytoskeleton 64:217-32. 2007
    ..We have not been able to decipher an oscillatory pattern in vacuole motion. Because this motion is dependent on actin and not tubulin, we think this is due to a different myosin from that which drives the ER and mitochondria...
  8. ncbi Intracellular gonadotropin-releasing hormone receptors in breast cancer and gonadotrope lineage cells
    Kathleen R Sedgley
    Laboratories for Integrative Neuroscience and Endocrinology, University of Bristol, Dorothy Hodgkin Building, Whitson Street, Bristol BS1 3NY, UK
    J Endocrinol 191:625-36. 2006
    ..Manipulations favoring such trafficking may facilitate selective targeting of extra-pituitary GnRHRs...
  9. ncbi Phencyclidine-induced cognitive deficits in mice are improved by subsequent subchronic administration of the novel selective alpha7 nicotinic receptor agonist SSR180711
    Kenji Hashimoto
    Division of Clinical Neuroscience, Chiba University Center for Forensic Mental Health, Chiba, Japan
    Biol Psychiatry 63:92-7. 2008
    ....
  10. ncbi Dementia rating and nicotinic receptor expression in the prefrontal cortex in schizophrenia
    Carmen M Martin-Ruiz
    Institute for Ageing and Health, Newcastle General Hospital, Newcastle upon Tyne, United Kingdom
    Biol Psychiatry 54:1222-33. 2003
    ..Further investigations are required to establish whether the reduction in alpha7 protein in the dorsal lateral prefrontal cortex is associated with clinical features other than dementia in schizophrenia...
  11. ncbi Potent and selective activation of the pancreatic beta-cell type K(ATP) channel by two novel diazoxide analogues
    M Dabrowski
    University Laboratory of Physiology, Parks Road, Oxford, UK
    Diabetologia 46:1375-82. 2003
    ..The high selectivity and efficacy of the compounds could prove useful for treatment of disease states where inhibition of insulin secretion is beneficial...
  12. ncbi Actin depolymerization is sufficient to induce programmed cell death in self-incompatible pollen
    Steven G Thomas
    School of Biosciences, University of Birmingham, Edgbaston, Birmingham B15 2TT, England, UK
    J Cell Biol 174:221-9. 2006
    ..This represents the first account of a specific causal link between actin polymerization status and initiation of PCD in a plant cell and significantly advances our understanding of the mechanisms involved in SI...
  13. ncbi Small molecules that reactivate mutant p53
    V J N Bykov
    Department of Oncology-Pathology, Cancer Center Karolinska, SE-171 76 Stockholm, Sweden
    Eur J Cancer 39:1828-34. 2003
    ..Various types of small molecules have been identified that can restore native conformation and wild-type function to mutant p53. Such molecules may serve as leads for the development of novel efficient anticancer drugs...
  14. ncbi Macrolactonization via Ti(IV)-mediated epoxy-acid coupling: a total synthesis of (-)-dactylolide [and zampanolide]
    Thomas R Hoye
    Department of Chemistry, University of Minnesota, Minneapolis, Minnesota 55455, USA
    J Am Chem Soc 125:9576-7. 2003
    ....
  15. ncbi Rho protein-mediated changes in the structure of the actin cytoskeleton regulate human inducible NO synthase gene expression
    Andrea Witteck
    Department of Pharmacology, Johannes Gutenberg University, Obere Zahlbacher Strasse 67, D-55101, Mainz, Germany
    Exp Cell Res 287:106-15. 2003
    ..In conclusion, our data suggest that Rho protein-mediated changes of the actin cytoskeleton negatively modulate the expression of human iNOS...
  16. ncbi Synergistic effects of peloruside A and laulimalide with taxoid site drugs, but not with each other, on tubulin assembly
    Ernest Hamel
    Toxicology and Pharmacology Branch, Developmental Threapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute at Frederick, MD 21702, USA
    Mol Pharmacol 70:1555-64. 2006
    ....
  17. ncbi Peloruside A synergizes with other microtubule stabilizing agents in cultured cancer cell lines
    Anja Wilmes
    School of Biological Sciences, Victoria University of Wellington, Wellington, New Zealand
    Mol Pharm 4:269-80. 2007
    ....
  18. ncbi Effector mechanisms of norcantharidin-induced mitotic arrest and apoptosis in human hepatoma cells
    Yan-Nian Chen
    School of Chinese Medicine, China Medical College, Taichung, Taiwan
    Int J Cancer 100:158-65. 2002
    ..Furthermore, the increase of p21(Cip1/Waf1), phosphorylation of Bcl-2 and Bcl-X(L), activation of caspase-9 and caspase-3 may be the molecular mechanism through which NCTD induces apoptosis...
  19. ncbi Actin filaments are involved in the maintenance of Golgi cisternae morphology and intra-Golgi pH
    Francisco Lázaro-Diéguez
    Departament de Biologia Cellular i Anatomia Patologica, Facultat de Medicina, Universitat de Barcelona, 08036 Barcelona, Spain
    Cell Motil Cytoskeleton 63:778-91. 2006
    ..This maintenance seems to be mediated by the regulation of the state of F-actin assembly on the Golgi pH homeostasis...
  20. ncbi NMR determination of the bioactive conformation of peloruside A bound to microtubules
    Jesus Jimenez-Barbero
    Centro de Investigaciones Biologicas, CSIC, Ramiro de Maeztu 9, 28040 Madrid, Spain
    J Am Chem Soc 128:8757-65. 2006
    ..A model of the binding mode to tubulin has also been proposed, by docking the bioactive conformation of peloruside, which involves the alpha-tubulin monomer, in contrast with taxol, which binds to the beta-monomer...
  21. ncbi Salicylihalamide A inhibits the V0 sector of the V-ATPase through a mechanism distinct from bafilomycin A1
    Xiao Song Xie
    Eugene McDermott Center for Human Growth and Development, University of Texas Southwestern Medical Center at Dallas, Dallas, TX 75390, USA
    J Biol Chem 279:19755-63. 2004
    ....
  22. ncbi A contractile nuclear actin network drives chromosome congression in oocytes
    Peter Lenart
    Gene Expression and Cell Biology Biophysics Programmes, European Molecular Biology Laboratory EMBL, Meyerhofstrasse 1, D 69117 Heidelberg, Germany
    Nature 436:812-8. 2005
    ..We show that this mechanism is essential for preventing chromosome loss and aneuploidy of the egg--a leading cause of pregnancy loss and birth defects in humans...
  23. ncbi The effects of NN414, a SUR1/Kir6.2 selective potassium channel opener, in healthy male subjects
    Milan Zdravkovic
    Novo Nordisk A/S, Medical Development, Bagsvaerd, Denmark
    J Clin Pharmacol 45:763-72. 2005
    ..NN414 treatment lowered glucose during the OGTT and 24-hour insulin and glucose levels. In conclusion, a single dose of NN414 is associated with improvements in glucose-related parameters in healthy male subjects...
  24. ncbi An expedient total synthesis of (-)-dactylolide and formal synthesis of (-)-zampanolide
    Fei Ding
    Department of Chemistry, The University of Alabama, Tuscaloosa, Alabama 35487-0336, USA
    Org Lett 7:2321-4. 2005
    ..reaction: see text] A highly convergent and efficient total synthesis of (-)-dactylolide and formal synthesis of (-)-zampanolide is reported...
  25. ncbi Actin polymerization promotes the reversal of streaming in the apex of pollen tubes
    Luis Cardenas
    Biology Department, and the Plant Biology Graduate Program, Morrill Science Center, University of Massachusetts, Amherst, USA
    Cell Motil Cytoskeleton 61:112-27. 2005
    ..Taken together, our results support the idea that actin polymerization promotes reversal of streaming in the apex of the lily pollen tube...
  26. ncbi Rapid hop diffusion of a G-protein-coupled receptor in the plasma membrane as revealed by single-molecule techniques
    Kenichi Suzuki
    Kusumi Membrane Organizer Project, Exploratory Research for Advanced Technology Organization, Department of Biological Science and Institute for Advanced Research, Nagoya University, Nagoya 464-8602, Japan
    Biophys J 88:3659-80. 2005
    ....
  27. ncbi AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties
    Narender R Gavva
    Department of Neuroscience, Amgen Inc, MS-29-2-B, Thousand Oaks, CA 91320-1799, USA
    J Pharmacol Exp Ther 313:474-84. 2005
    ..AMG 9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain...
  28. ncbi Norcantharidin-induced apoptosis in oral cancer cells is associated with an increase of proapoptotic to antiapoptotic protein ratio
    Sang-Heng Kok
    School of Dentistry, College of Medicine, National Taiwan University, 1 Chang-Te Street, Taipei 10016, Taiwan, ROC
    Cancer Lett 217:43-52. 2005
    ..Since oral cancer cells with mutant p53 or elevated Bcl-XL levels showed resistance to multiple chemotherapeutic agents, NCTD may overcome the chemoresistance of these cells and provide potential new avenues for treatment...
  29. ncbi Peloruside A enhances apoptosis in H-ras-transformed cells and is cytotoxic to proliferating T cells
    J H Miller
    School of Biological Sciences, Victoria University of Wellington, PO Box 600, Wellington, New Zealand
    Apoptosis 9:785-96. 2004
    ..It is concluded that peloruside preferentially targets oncogene-transformed cells over non-transformed cells by inducing transformed cells to undergo apoptosis...
  30. ncbi Regulation of G protein-coupled receptor trafficking by inefficient plasma membrane expression: molecular basis of an evolved strategy
    Jo Ann Janovick
    Division of Neuroscience, Oregon National Primate Research Center, Oregon Health and Science University, Beaverton, Oregon 97006, USA
    J Biol Chem 281:8417-25. 2006
    ....
  31. ncbi Computational comparison of microtubule-stabilising agents laulimalide and peloruside with taxol and colchicine
    Oriol Pineda
    , , Universitat de Barcelona, 08028 Barcelona, Catalonia, Spain, EU
    Bioorg Med Chem Lett 14:4825-9. 2004
    ..All together provides a plausible rationalisation of the singular binding features of these microtubule stabilisers and paves the way for future structural studies...
  32. ncbi The metabotropic glutamate receptor 5 antagonist MPEP and the mGluR2 agonist LY379268 modify disease progression in a transgenic mouse model of Huntington's disease
    Johannes Schiefer
    Department of Neurology, University Hospital RWTH Aachen, Pauwelsstrasse 30, D-52074 Aachen, Germany
    Brain Res 1019:246-54. 2004
    ..These data suggest that inhibition of glutamate neurotransmission via specific interaction with mGluRs might be interesting for both inhibition of disease progression as well as early symptomatic treatment in HD...
  33. ncbi Actin cytoskeleton derangement induces apoptosis in renal ischemia/reperfusion
    M Genesca
    Department of Experimental Pathology, IIBB CSIC, IDIBAPS, Barcelona, Spain
    Apoptosis 11:563-71. 2006
    ..CONCLUSION: The disruption of the actin cytoskeleton during ischemic conditions associated with kidney preservation induces apoptosis upon reperfusion through caspase-3 activation...
  34. ncbi Actin- and protein-4.1-containing filaments link nuclear pore complexes to subnuclear organelles in Xenopus oocyte nuclei
    Elena Kiseleva
    Department of Structural Cell Biology, Paterson Institute for Cancer Research, Christie Hospital, Manchester, M20 9BX, UK
    J Cell Sci 117:2481-90. 2004
    ..1 and actin contribute to the structure of a network of heterogeneous filaments that link nuclear pore complexes to subnuclear organelles, and discuss possible functions for PLFs in nuclear assembly and intranuclear traffic...
  35. ncbi Actin polymerization-driven molecular movement of mDia1 in living cells
    Chiharu Higashida
    Department of Pharmacology, Kyoto University Faculty of Medicine, Yoshida konoe cho, Sakyo ku, Kyoto, Japan
    Science 303:2007-10. 2004
    ..mDia1 probably moves processively along the growing end of actin filaments in cells, and Formins may be a molecular motility machinery that is independent from motor proteins...
  36. ncbi Reversible protein phosphorylation regulates the dynamic organization of the pollen tube cytoskeleton: effects of calyculin A and okadaic acid
    Ilse Foissner
    Institut für Pflanzenphysiologie, Universitat Salzburg, Austria
    Protoplasma 220:1-15. 2002
    ..The effects of the PP2A inhibitors could be ameliorated with nanomolar concentrations of latrunculin B...
  37. ncbi Role of actin cytoskeletal dynamics in activation of the cyclic AMP pathway and HWP1 gene expression in Candida albicans
    Michael J Wolyniak
    Microbiology and Molecular Pathogenesis Program, Dartmouth Medical School, Vail Building, HB7550, Hanover, NH 03755, USA
    Eukaryot Cell 6:1824-40. 2007
    ..The results reveal a new role for F-actin as a regulatory agent of hypha-specific gene expression at the bud-hypha transition...
  38. ncbi Peloruside B, a potent antitumor macrolide from the New Zealand marine sponge Mycale hentscheli: isolation, structure, total synthesis, and bioactivity
    A Jonathan Singh
    Centre for Biodiscovery, Victoria University of Wellington, Wellington, New Zealand
    J Org Chem 75:2-10. 2010
    ..The synthesis features Sharpless dihydroxylation, Brown's asymmetric allylboration reaction, reductive aldol coupling, Yamaguchi macrolactonization, and selective methylation...
  39. ncbi A unique mode of microtubule stabilization induced by peloruside A
    J Torin Huzil
    Division of Experimental Oncology, Cross Cancer Institute, 11560 University Avenue, Edmonton, Alberta, Canada
    J Mol Biol 378:1016-30. 2008
    ..Using data-directed molecular docking simulations, we propose that peloruside A binds within a pocket on the exterior of beta-tubulin at a previously unknown ligand site, rather than on alpha-tubulin as suggested in earlier studies...
  40. ncbi Cortical actin filaments potentially interact with cortical microtubules in regulating polarity of cell expansion in primary roots of maize (Zea mays L.)
    E B Blancaflor
    Plant Biology Division, The Samuel Roberts Noble Foundation Inc, Ardmore, Oklahoma 73401, USA
    J Plant Growth Regul 19:406-14. 2000
    ..The results from this study provide evidence that cortical microtubules and actin filaments respond in a coordinated way to environmental signals and may well depend on both elements of the cytoskeleton...
  41. ncbi Evidence for the role of metabotropic glutamate (mGlu)2 not mGlu3 receptors in the preclinical antipsychotic pharmacology of the mGlu2/3 receptor agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid (LY404039)
    Matthew J Fell
    Neuroscience Discovery Research, Lilly Research Laboratories, Lilly Corporate Center, DC0510, Indianapolis, IN 46285, USA
    J Pharmacol Exp Ther 326:209-17. 2008
    ....
  42. ncbi Actin polymerization is essential for pollen tube growth
    L Vidali
    Biology Department, Molecular and Cellular Biology Program, University of Massachusetts, Amherst, Massachusetts 01003, USA
    Mol Biol Cell 12:2534-45. 2001
    ....
  43. ncbi Human MCF10A mammary epithelial cells undergo apoptosis following actin depolymerization that is independent of attachment and rescued by Bcl-2
    S S Martin
    Department of Genetics, Howard Hughes Medical Institute, Harvard Medical School, Boston, Massachusetts 02115, USA
    Mol Cell Biol 21:6529-36. 2001
    ..We demonstrate that inhibition of actin polymerization is sufficient to stimulate apoptosis in attached MCF10A cells, and we present a novel role for Bcl-2 in cell death induced by direct disruption of the actin cytoskeleton...
  44. ncbi An aldol-based synthesis of (+)-peloruside a, a potent microtubule stabilizing agent
    David A Evans
    Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA
    J Am Chem Soc 131:3840-1. 2009
    ..This approach afforded a 22-step synthesis of this natural product. The influence of resident stereocenters on aldol reaction diastereoselection has been examined in detail...
  45. ncbi Laminar distribution of nicotinic receptor subtypes in cortical regions in schizophrenia
    A Marutle
    Karolinska Institutet, Department of Clinical Neuroscience, Occupational Therapy and Elderly Care Research (NEUROTEC, Division of Molecular Neuropharmacology, Huddinge University Hospital, B84, S-141 86, Stockholm, Sweden
    J Chem Neuroanat 22:115-26. 2001
    ....
  46. ncbi Total synthesis of (-)-zampanolide and questionable existence of (-)-dactylolide as the elusive biosynthetic precursor of (-)-zampanolide in an Okinawan sponge
    Jun ichi Uenishi
    Kyoto Pharmaceutical University, Misasagi, Yamashina, Kyoto 607 8412 Japan
    Org Lett 11:3262-5. 2009
    ..A marine sponge extract was analyzed for the presence of (-)-2 as the biosynthetic precursor of (-)-zampanolide...
  47. ncbi Delaying the onset of experimental autoimmune encephalomyelitis with the microtubule-stabilizing compounds, paclitaxel and Peloruside A
    Kevin P Crume
    School of Biological Sciences, Victoria University of Wellington, Wellington, New Zealand 6140
    J Leukoc Biol 86:949-58. 2009
    ..These results indicate that microtubule-stabilizing drugs are effective at reducing disease but require a prolonged exposure to paclitaxel in vivo to alter proliferation in the myeloid and lymphoid cell compartments...
  48. ncbi Dynamics of immature secretory granules: role of cytoskeletal elements during transport, cortical restriction, and F-actin-dependent tethering
    R Rudolf
    Department of Neurobiology, Interdisciplinary Center for Neuroscience, University of Heidelberg, Im Neuenheimer Feld 364, D-69120 Heidelberg, Germany
    Mol Biol Cell 12:1353-65. 2001
    ..In a late phase of maturation, 60% of secretory granules were found to be immobile and about half of these underwent F-actin-dependent tethering...
  49. ncbi Endocytosis and the development of cell polarity in yeast require a dynamic F-actin cytoskeleton
    K R Ayscough
    Institute of Biomedical and Life Sciences, Division of Biochemistry and Molecular Biology, Davidson Building, University of Glasgow, Glasgow G12 8QQ, UK
    Curr Biol 10:1587-90. 2000
    ..These structures, however, still contained components that are normally associated with cortical actin patches. A dynamic actin cytoskeleton was found to be critical for the generation of cell polarity and endocytosis...
  50. ncbi Participation of actin on Giardia lamblia growth and encystation
    Araceli Castillo-Romero
    Departamento de Biologia Celular, CINVESTAV IPN, Mexico Distrito Federal, Mexico
    PLoS ONE 4:e7156. 2009
    ..Microfilaments play a determinant role in different cell processes such as: motility, cell division, phagocytosis and intracellular transport; however, these structures are poorly understood in the parasite Giardia lamblia...
  51. ncbi Regional distribution of nicotinic receptor subunit mRNAs in human brain: comparison between Alzheimer and normal brain
    E Hellström-Lindahl
    Department of Clinical Neuroscience, Occupational Therapy and Elderly Care Research, Division of Molecular Neuropharmacology, Karolinska Institute, Huddinge University Hospital, S 14186 Huddinge, Sweden
    Brain Res Mol Brain Res 66:94-103. 1999
    ..The increased mRNA level of alpha7 previously found in lymphocytes, and now also in the hippocampus of AD patients, indicate that subunit specific changes in gene expression of nAChRs is associated with AD...
  52. ncbi Plasma membrane expression of GnRH receptors: regulation by antagonists in breast, prostate, and gonadotrope cell lines
    Ann R Finch
    Laboratories for Integrative Neuroscience and Endocrinology, University of Bristol, Dorothy Hodgkin Building, Whitson Street, Bristol BS1 3NY, UK
    J Endocrinol 196:353-67. 2008
    ..The low PCSE of hGnRHRs and this novel peptide antagonist effect may be important for understanding GnRHR function in extrapituitary sites...
  53. ncbi Rescue of hypogonadotropic hypogonadism-causing and manufactured GnRH receptor mutants by a specific protein-folding template: misrouted proteins as a novel disease etiology and therapeutic target
    Jo Ann Janovick
    Oregon Regional Primate Research Center, Department of Physiology and Pharmacology, Oregon Health and Science University, 595 NW 185th Avenue, Beaverton, OR 97006, USA
    J Clin Endocrinol Metab 87:3255-62. 2002
    ..The present findings demonstrate the efficacy of an approach based on pharmacological rescue and suggest the basis of new approaches for intervention in this and similar diseases...
  54. ncbi Improvement of cisplatin-induced emesis and delayed gastric emptying by KB-R6933, a novel 5-HT3 receptor antagonist
    A Ozaki
    Pharmaceuticals R and D Center, Kanebo, Ltd, Osaka, Japan
    Gen Pharmacol 33:283-8. 1999
    ..KB-R6933 reversed the reduction of gastric emptying induced by cisplatin. These results suggest that KB-R6933 is an antiemetic agent, and could improve the cisplatin-induced delay of gastric emptying...
  55. ncbi The mGlu2 but not the mGlu3 receptor mediates the actions of the mGluR2/3 agonist, LY379268, in mouse models predictive of antipsychotic activity
    M L Woolley
    GlaxoSmithKline plc, Harlow, Essex, CM19 5AW, UK
    Psychopharmacology (Berl) 196:431-40. 2008
    ..Conversely, pre-clinical studies suggest that mGluR2 may be responsible for mediating the antipsychotic activity of mGluR2/3 agonists, although to date, the role of mGluR3 has not been specifically assessed...
  56. ncbi Lipid products of PI(3)Ks maintain persistent cell polarity and directed motility in neutrophils
    Fei Wang
    Department of Cellular and Molecular Pharmacology and the Cardiovascular Research Institute, University of California, San Francisco, CA 94143-0450, USA
    Nat Cell Biol 4:513-8. 2002
    ..Thus reciprocal interplay between PtdIns(3,4,5)P(3) and polymerized actin initiates and maintains the asymmetry of intracellular signals responsible for cell polarity and directed motility...
  57. ncbi Total syntheses of (+)-zampanolide and (+)-dactylolide exploiting a unified strategy
    Amos B Smith
    Contribution from the Department of Chemistry, Monell Chemical Senses Center, and Laboratory for Research on the Structure of Matter, University of Pennsylvania, Philadelphia, Pennsylvania 19104
    J Am Chem Soc 124:11102-13. 2002
    ..The complete relative and absolute stereochemistries for both (+)-zampanolide and (+)-dactylolide were also assigned, albeit tentatively in the case of (+)-zampanolide (1)...
  58. ncbi Peloruside A, a novel antimitotic agent with paclitaxel-like microtubule- stabilizing activity
    Kylie A Hood
    School of Biological Sciences, Victoria University of Wellington, New Zealand
    Cancer Res 62:3356-60. 2002
    ..The relatively simple structure of peloruside makes it suitable for the design and synthesis of analogues with improved tumor targeting and reduced tumor cross-resistance...
  59. ncbi Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized Phase 2 clinical trial
    Sandeep T Patil
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    Nat Med 13:1102-7. 2007
    ..These data suggest that mGlu2/3 receptor agonists have antipsychotic properties and may provide a new alternative for the treatment of schizophrenia...
  60. ncbi Induction of apoptosis by norcantharidin in human colorectal carcinoma cell lines: involvement of the CD95 receptor/ligand
    F Peng
    Center for Biotherapy of Cancer and Cancer Center, West China Hospital, Sichuan University, Guo Xue Xiang, Number 37, Chengdu, Sichuan 610041, P.R. China
    J Cancer Res Clin Oncol 128:223-30. 2002
    ....
  61. ncbi Local actin polymerization and dynamin recruitment in SV40-induced internalization of caveolae
    Lucas Pelkmans
    Swiss Federal Institute of Technology Zurich (ETHZ, HPM1 Building, , CH-8093 Zurich, Switzerland
    Science 296:535-9. 2002
    ..They were necessary for formation of caveolae-derived endocytic vesicles and for infection of the cell. Thus, caveolar endocytosis is ligand-triggered and involves extensive rearrangement of the actin cytoskeleton...
  62. ncbi Visualization of peroxisomes in living plant cells reveals acto-myosin-dependent cytoplasmic streaming and peroxisome budding
    Gregory Jedd
    Laboratory of Plant Molecular Biology, The Rockefeller University, 1230 York Avenue, New York, NY 10021 6399, USA
    Plant Cell Physiol 43:384-92. 2002
    ..Peroxisome movement is most intense in elongated cells and those involved in long distance transport, suggesting that higher plants use cytoplasmic streaming to help transport vesicles and organelles over long distances...
  63. ncbi Synthesis and pharmacological characterization of exo-2-(2'-chloro-5-pyridinyl)-7-(endo and exo)-aminobicyclo[2.2.1]heptanes as novel epibatidine analogues
    F Ivy Carroll
    Chemistry and Life Sciences, Research Triangle Institute, P O Box 12194, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 48:7491-5. 2005
    ..Compounds 3a and 3b possessed alpha4beta2 nAChR binding properties similar to those of (-)-nicotine and were nAChR agonists in all four mouse assays...
  64. ncbi Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine
    F Ivy Carroll
    Organic and Medicinal Chemistry, Research Triangle Institute, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 50:6383-91. 2007
    ..Interestingly, N-methylepibatidine, prepared as a standard compound for the study of bridged analogues 6 and 7, was a potent nAChR mixed agonist antagonist...
  65. ncbi Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists
    Jianguo Ji
    Neuroscience Research, R47W, AP9A 1, Abbott, Abbott Park, Illinois 60064, USA
    J Med Chem 50:5493-508. 2007
    ..The SAR studies of these novel ligands led to the discovery of several compounds with interesting in vitro pharmacological profiles...
  66. ncbi Selective down-regulation of [(125)I]Y0-alpha-conotoxin MII binding in rat mesostriatal dopamine pathway following continuous infusion of nicotine
    M Mugnaini
    Biology Department, Psychiatry CEDD, GlaxoSmithKline S p A, Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy
    Neuroscience 137:565-72. 2006
    ....
  67. ncbi Rho kinase regulates fragmentation and phagocytosis of apoptotic cells
    Kelly A Orlando
    Department of Pharmacology, University of Pennsylvania, 3620 Hamilton Walk, Philadelphia, PA 19104, USA
    Exp Cell Res 312:5-15. 2006
    ..Finally, cells dying in the presence of the ROCK inhibitor Y-27632 are not efficiently phagocytized. These data show that ROCK plays an essential role in fragmentation and phagocytosis of apoptotic cells...
  68. ncbi Derivatives of (-)-7-methyl-2-(5-(pyridinyl)pyridin-3-yl)-7-azabicyclo[2.2.1]heptane are potential ligands for positron emission tomography imaging of extrathalamic nicotinic acetylcholine receptors
    Yongjun Gao
    Division of Nuclear Medicine, Department of Radiology, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287 0816, USA
    J Med Chem 50:3814-24. 2007
    ..2.1]heptane, exhibited good properties as a first practical PET radioligand for imaging of extrathalamic nAChR in baboon brain and holds promise for further investigation for human studies...
  69. ncbi Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonists
    Jennifer M Frost
    Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60064, USA
    J Med Chem 49:7843-53. 2006
    ..e., 24, 25, 28, 30, 32, and 47) exhibit equivalent or greater affinity for the halpha4beta2 receptor relative to epibatidine, and like epibatidine, many exhibit robust analgesic efficacy in the rat formalin model of persistent pain...
  70. ncbi Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationsh
    Donn G Wishka
    Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, USA
    J Med Chem 49:4425-36. 2006
    ....
  71. ncbi The state of the actin cytoskeleton determines its association with gephyrin: role of ena/VASP family members
    Melanie Bausen
    Department of Neurochemistry, Max Planck Institute for Brain Research, 60528 Frankfurt, Germany
    Mol Cell Neurosci 31:376-86. 2006
    ..Our data suggest that Mena binding to F-actin allows for gephyrin recruitment to the leading edge of uncapped actin filaments...
  72. ncbi From ligand design to therapeutic efficacy: the challenge for nicotinic receptor research
    Bruce K Cassels
    Department of Chemistry, Faculty of Sciences, University of Chile, Casilla 653, Santiago, Chile
    Drug Discov Today 10:1657-65. 2005
    ..Here, we focus on three natural products as lead compounds for drug discovery programs, nicotine, epibatidine and cytisine, and consider the aims and limitations that shape these drug discovery endeavors...
  73. ncbi Role of negatively charged amino acids in beta 4 F-loop in activation and desensitization of alpha 3 beta 4 rat neuronal nicotinic receptors
    Jiří Lindovský
    Institute of Physiology, Academy of Sciences of the Czech Republic, Videnska 1083, 142 20 Prague 4, Czech Republic
    Biochim Biophys Acta 1778:864-71. 2008
    ..The double mutation substantially accelerated the return from long-term desensitization induced by Epi...
  74. ncbi Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity
    Brad A Acker
    Neuroscience Research, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 18:3611-5. 2008
    ..The compound shows potent and selective alpha7 in vitro activity, excellent brain penetration, good rat oral bioavailability and robust in vivo efficacy in a rat auditory sensory gating model...
  75. ncbi Epibatidine and its analogues as nicotinic acetylcholine receptor agonist: an update
    Perumal Yogeeswari
    Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333 031, India
    Nat Prod Res 20:497-505. 2006
    ..In this article, isolation, synthetic methods, effect on neuronal and neuromuscular nicotinic receptors, therapeutic potential, toxicity, nicotinic pharmacophore structural modifications related issues of 1 are discussed...
  76. ncbi Role in the selectivity of neonicotinoids of insect-specific basic residues in loop D of the nicotinic acetylcholine receptor agonist binding site
    Masaru Shimomura
    Department of Applied Biological Chemistry, School of Agriculture, Kinki University, 3327-204 Nakamachi, Nara 631-8505, Japan
    Mol Pharmacol 70:1255-63. 2006
    ....
  77. ncbi Effects of nicotine on sensorimotor gating impairment induced by long-term treatment with neurotoxic NMDA antagonism
    Bruce A Rasmussen
    Department of Pharmacology and Physiology, George Washington University, Washington DC, USA
    Neurotox Res 13:151-61. 2008
    ..The results suggest a sustainable model of PPI impairment and possible role of nicotinic receptors in selective brain regions in this behavior...
  78. ncbi Relative toxicities and neuromuscular nicotinic receptor agonistic potencies of anabasine enantiomers and anabaseine
    Stephen T Lee
    Poisonous Plant Research Laboratory, Agricultural Research Service, United States Department of Agriculture, 1150 E 1400 N, Logan, UT 84341, USA
    Neurotoxicol Teratol 28:220-8. 2006
    ..The relative agonistic potencies of these three alkaloids on human fetal nicotinic neuromuscular receptors were of the same rank order: anabaseine>>R-anabasine>S-anabasine...
  79. ncbi Synthesis and radiosynthesis of [(18)F]FPhEP, a novel alpha(4)beta(2)-selective, epibatidine-based antagonist for PET imaging of nicotinic acetylcholine receptors
    Gaelle Roger
    Service Hospitalier Frederic Joliot, Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91401 Orsay, France
    Bioorg Med Chem 14:3848-58. 2006
    ..Taken together, the preliminary data obtained confirm that [(18)F]FPhEP ([(18)F]-1) has potential for in vivo imaging nAChRs in the brain with PET...
  80. ncbi Synthesis and binding studies of epibatidine analogues as ligands for the nicotinic acetylcholine receptors
    Linjing Mu
    Center for Radiopharmaceutical Sciences, Swiss Federal Institute of Technology Zurich, Paul Scherrer Institute, , , , Switzerland
    Eur J Med Chem 41:640-50. 2006
    ....
  81. ncbi P2X(7) receptors exert a permissive role on the activation of release-enhancing presynaptic alpha7 nicotinic receptors co-existing on rat neocortex glutamatergic terminals
    Laura Patti
    Department of Experimental Medicine, Pharmacology and Toxicology Section, University of Genoa, Viale Cembrano 4, 16148 Genova, Italy
    Neuropharmacology 50:705-13. 2006
    ....
  82. ncbi Lovastatin stimulates up-regulation of alpha7 nicotinic receptors in cultured neurons without cholesterol dependency, a mechanism involving production of the alpha-form of secreted amyloid precursor protein
    Jin Xiu
    Neurotec Department, Division of Molecular Neuropharmacology, Karolinska Institutet, Stockholm, Sweden
    J Neurosci Res 82:531-41. 2005
    ..We also show that the up-regulation of alpha7 nAChRs stimulated by lovastatin is involved in a mechanism that enhances production of alphaAPPs during APP processing...
  83. ncbi Syntheses and evaluation of halogenated cytisine derivatives and of bioisosteric thiocytisine as potent and selective nAChR ligands
    P Imming
    Department of Pharmaceutical Chemistry, Philipps-University, Marbacher Weg 6, D-35032 Marburg, Germany
    Eur J Med Chem 36:375-88. 2001
    ....
  84. ncbi Synthesis and biological evaluation at nicotinic acetylcholine receptors of N-arylalkyl- and N-aryl-7-azabicyclo[2.2.1]heptanes
    Jie Cheng
    Department of Chemistry, University of New Orleans, New Orleans, LA 70148, USA
    J Med Chem 45:3041-7. 2002
    ..However, when compounds 1 and 5a,b were administered intrathecally, all produced analgesia in the tail-flick test but only 5a produced analgesia in the hotplate test...
  85. ncbi Role of the actin cytoskeleton in store-mediated calcium entry in glioma C6 cells
    Pawelz Sabała
    Laboratory of Signal Transduction, Department of Molecular and Cellular Neurobiology, Nencki Institute of Experimental Biology, Polish Academy of Sciences, 3 Pasteur Str, Warsaw, Poland
    Biochem Biophys Res Commun 296:484-91. 2002
    ..While the agonists evoke a store-mediated Ca2+ entry that is dependent on the actin cytoskeleton, thapsigargin apparently activates an additional mechanism, which is independent of the disruption of the cytoskeleton...
  86. ncbi Effects of pyridine ring substitutions on affinity, efficacy, and subtype selectivity of neuronal nicotinic receptor agonist epibatidine
    Melva Avalos
    Department of Molecular and Cellular Pharmacology, University of Miami School of Medicine, Miami, FL 33101, USA
    J Pharmacol Exp Ther 302:1246-52. 2002
    ....
  87. ncbi Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues
    F Ivy Carroll
    Chemistry and Life Sciences, Research Triangle Institute, P O Box 12194, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 45:4755-61. 2002
    ..2,3-Disubstituted epibatidine analogues possessing a 2'-amino group combined with a 3'-bromo or 3'-iodo group showed in vitro and in vivo nAChR properties similar to nicotine...
  88. ncbi Ligand-receptor interaction at the neural nicotinic acetylcholine binding site: a theoretical model
    A Morreale
    , Facultad de Farmacia, Universidad de Alcal, Madrid, Spain
    J Mol Graph Model 21:111-8. 2002
    ..In this limited set of compounds, a good correlation between total interaction energies and biological affinity is observed...
  89. ncbi [125I]Epibatidine-labelled nicotinic receptors in the extended striatum and cerebral cortex: lack of association with serotonergic afferents
    Amynah A A Pradhan
    Department of Pharmacology and Therapeutics, McGill University, 3655 Promenade Sir William Osler, Montreal, Quebec, Canada H3G 1Y6
    Brain Res 954:227-36. 2002
    ..In conclusion, we report the failure to detect nAChRs on 5-HT terminals in extended striatum or cerebral cortex, using a sensitive [125I]epibatidine autoradiographic assay...
  90. ncbi Time-dependent changes in rat brain cholinergic receptor expression after experimental brain injury
    S Leigh Verbois
    Division of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536 0082, USA
    J Neurotrauma 19:1569-85. 2002
    ..Persistent deficits in alpha7* nAChr expression following TBI may contribute to impaired functional outcome following brain injury...
  91. ncbi Synthesis and binding affinities of 5-(3-pyridinyl)- and 5-(3-quinolinyl)-4-azahomoadamantanes to alpha7 nicotinic acetylcholine receptors
    Dimitris Tataridis
    Department of Pharmaceutical Chemistry, School of Pharmacy, University of Athens, Panepistimioupoli-Zografou, GR 15 771 Athens, Greece
    Farmaco 57:979-84. 2002
    ..N-methyl substitution of 2a gives compound 3a which has about nine times lower binding affinity. The replacement of pyridinyl with a quinolinyl ring (compounds 2b, 3b) results in a dramatic reduction in potency (Ki > 1000 microM)...
  92. ncbi Benzylidene anabaseines act as high-affinity agonists for insect nicotinic acetylcholine receptors
    I Sultana
    Department of Life Science and Biotechnology, Shimane University, Matsue, 690-8504, Japan
    Insect Biochem Mol Biol 32:637-43. 2002
    ..6 microg/ml. These findings suggest that benzylidene anabaseines act as high-affinity agonists in P. americana nAChRs and that they might therefore prove useful as probes for insect nAChRs...
  93. ncbi Actin cytoskeletal modulation of pressure-induced depolarization and Ca(2+) influx in cerebral arteries
    Natalia I Gokina
    Department of Obstetrics and Gynecology, University of Vermont College of Medicine, Burlington, Vermont 05405, USA
    Am J Physiol Heart Circ Physiol 282:H1410-20. 2002
    ..Together, these results implicate vascular smooth muscle actin cytoskeletal dynamics in the control of cerebral artery diameter through their influence on membrane potential as well as via a direct effect on L-type Ca(2+) channels...
  94. ncbi Smooth muscle differentiation marker gene expression is regulated by RhoA-mediated actin polymerization
    C P Mack
    Department of Molecular Physiology and Biological Physics, University of Virginia Medical School, Charlottesville, Virginia 22908, USA
    J Biol Chem 276:341-7. 2001
    ..The results also suggest that RhoA signaling may serve as a convergence point for the multiple signaling pathways that regulate SMC differentiation...
  95. ncbi Human and rodent bronchial epithelial cells express functional nicotinic acetylcholine receptors
    A D Maus
    Department of Biochemistry, University of Minnesota, St Paul, Minnesota 55108, USA
    Mol Pharmacol 54:779-88. 1998
    ..This may mediate or facilitate some of the toxic effects of cigarette smoking in the respiratory system...
  96. ncbi Differential effects of chronic drug treatment on alpha3* and alpha7 nicotinic receptor binding sites, in hippocampal neurones and SH-SY5Y cells
    D L Ridley
    Department of Biology and Biochemistry, University of Bath, Bath, BA2 7AY
    Br J Pharmacol 133:1286-95. 2001
    ..In contrast, alpha3* nicotinic AChR are not upregulated by KCl. This difference may reflect the distinct physiological roles proposed for alpha7 nicotinic AChR...
  97. ncbi Synthesis and evaluation of diazine containing bioisosteres of (-)-ferruginine as ligands for nicotinic acetylcholine receptors
    D Gündisch
    Department of Pharmaceutical Chemistry, Rhein Friedr Wilhelm University, Kreuzbergweg 26, D 53115, Bonn, Germany
    Bioorg Med Chem 9:2683-91. 2001
    ..7 nM (alpha4beta2). Compared with the lead 3, this value represents a 30-fold improvement in the affinity for the alpha4beta2 subtype combined with a substantially improved selectivity ratio between the alpha4beta2 and alpha7* subtypes...
  98. ncbi Dorsal root ganglion neurons express multiple nicotinic acetylcholine receptor subtypes
    J R Genzen
    Committee on Neurobiology, University of Chicago, Chicago, Illinois 60637, USA
    J Neurophysiol 86:1773-82. 2001
    ..Both the alpha7-like and alpha3beta4-like responses could be desensitized by prolonged applications of the analgesic epibatidine...
  99. ncbi The actin cytoskeleton is required for the trafficking of the B cell antigen receptor to the late endosomes
    B K Brown
    Department of Cell Biology and Molecular Genetics, University of Maryland, College Park, MD 20742, USA
    Traffic 2:414-27. 2001
    ..Thus, BCR-trafficking requires functional actin filaments for both internalization and movement to late endosomes/lysosomes, defining critical control points in BCR-antigen targeting...
  100. ncbi Rho/ROCK pathway contributes to the activation of extracellular signal-regulated kinase/GATA-4 during myocardial cell hypertrophy
    Tetsuhiko Yanazume
    Department of Cardiovascular Medicine, Graduate School of Medicine, Kyoto University, 54 Kawara cho, Shogoin, Sakyo ku, Kyoto 606 8507, Japan
    J Biol Chem 277:8618-25. 2002
    ..The results also suggest that changes in actin dynamics provide a convergence point for Rho/ROCK to the downstream signals during this process...
  101. ncbi Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo[4.2.1]non-2-ene UB-165
    Holger Gohlke
    , Marbacher Weg 6, D-35032 Marburg, Germany
    J Med Chem 45:1064-72. 2002
    ..The nitrogens in this anatoxinoid 8 show by far the most negative atomic charges (calculated using the AM1 Hamiltonian). This qualitatively correlates with the highest binding affinity observed for 8 for all subtypes under consideration...

Research Grants151 found, 100 shown here

  1. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 2007
    ..abstract_text> ..
  2. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2006
    ....
  3. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2003
    ..abstract_text> ..
  4. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 1991
    ....
  5. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2007
    ..Compounds that are potent delta selective opioid receptor inverse agonists will be evaluated by Dr. Chris Evans (UCLA) in a chronic antinociception rat model. ..
  6. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2001
    ..5) The potency of the epibatidine analogs prepared at RTI in activating expressed alpha4beta2 receptors was shown by studies at MCV to correlate well with the K-app binding affinities. ..
  7. NOVEL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    Frank Carroll; Fiscal Year: 2001
    ..An ideal candidate compound would not only have efficacy in the preclinical models but would be safe, orally active, and potent, would not show tolerance or sensitization, and if abusable, would be less so than cocaine. ..
  8. Development of Pharmacotherapies for Nicotine Addiction
    Frank Carroll; Fiscal Year: 2005
    ....
  9. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2009
    ..This application addresses this problem by proposing studies to develop competitive antagonists and partial agonists as well as allosteric modulators of nicotinic acetylcholine receptors as new pharmacotherapies to treat smokers. ..
  10. Design and Development of Pharmacotherapies for Treating Stimulant Abuse
    Frank Ivy Carroll; Fiscal Year: 2010
    ..3) To continue on a limited basis our development of selected 3-phenyltropane analogs as second-generation pharmacotherapies to treat cocaine addiction. ..
  11. Selective Opioid Antagonists as Medications for Drug Abuse
    Frank Ivy Carroll; Fiscal Year: 2010
    ..This application addresses these problems by proposing to identify and develop selective ? opioid receptor antagonists as new pharmacotherapies to treat patients addicted to drugs of abuse. ..
  12. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Ivy Carroll; Fiscal Year: 2010
    ..This application addresses this problem by proposing studies to develop competitive antagonists and partial agonists as well as allosteric modulators of nicotinic acetylcholine receptors as new pharmacotherapies to treat smokers. ..
  13. RECEPTORS FOR COCAINE AND DOPAMINE
    Philip Seeman; Fiscal Year: 1993
    ..The availability of clones for these receptors would facilitate new drug design and provide new markers for disease linkage studies in families...
  14. SYNTHESIS OF CYCLOPENTENOID ANTITUMOR AGENTS
    AMOS SMITH; Fiscal Year: 1980
    ..Once such features are identified the design of new and possibly more effective antitumor drugs should be feasible...
  15. Anticancer Agents: Structure and Synthesis
    Amos B Smith; Fiscal Year: 2010
    ..To this end, new synthetic chemistry will be developed that will have utility not only for this program, but also be of general value to the academic and pharmaceutical communities engaged in Cancer Biology. ..
  16. RECEPTORS MEDIATING DRUG DEPENDENCE
    Philip Seeman; Fiscal Year: 1999
    ....
  17. Chemogenomics to Identify New Molecular Targets in PF
    William Henderson; Fiscal Year: 2006
    ..These studies represent a focused effort using chemogenomics to identify, develop, and validate small molecule inhibitors of AP-1/TGFBeta-driven profibrotic gene expression as novel therapies in PF patients. ..
  18. LOCAL AND GLOBAL CONFORMATIONS OF SUPERCOILED DNA
    Yuri Lyubchenko; Fiscal Year: 2007
    ..abstract_text> ..
  19. 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. ..
  20. SYNTHESIS OF BIOACTIVE NATURAL PRODUCTS
    Amos B Smith; Fiscal Year: 2010
    ..Our experience with discodermolide gives us great confidence in this area. ..
  21. TRAUMA & SEPSIS INDUCED CHANGES IN IMMUNE CELL MEMBRANE RECEPTOR TRAFFICKING
    Joseph Cuschieri; Fiscal Year: 2010
    ....
  22. Synthesis of Polyketides and Terpenes
    David A Evans; Fiscal Year: 2010
    ..As a consequence, organic synthesis is a critical discipline that continues to have an important impact on the fields of both medicine and biology. ..
  23. DISCOVERY OF SMALL-MOLECULE ORPHANIN FQ RECEPTOR LIGANDS
    Nurulain Zaveri; Fiscal Year: 2009
    ..The proposed studies will significantly accelerate the translation of the project toward the development of therapeutically viable NOP agonists as drug abuse treatment medications. ..
  24. IDO-mediated immune regulation in established tumors
    David H Munn; Fiscal Year: 2010
    ....
  25. Role of 4.1 proteins in kainate receptor localization and function
    Geoffrey T Swanson; Fiscal Year: 2010
    ..In this grant, we will elucidate the role of a set of intracellular proteins in moving kainate receptors to their site(s) of functional activity in neurons. ..
  26. Discovery of Bifunctional NOP/Opioid Receptor Ligands for Drug Abuse Therapy
    Nurulain T Zaveri; Fiscal Year: 2010
    ....
  27. Role of IDO malignancy
    David Munn; Fiscal Year: 2007
    ....
  28. TRAUMA & SEPSIS INDUCED CHANGES IN IMMUNE CELL MEMBRANE RECEPTOR TRAFFICKING
    Joseph Cuschieri; Fiscal Year: 2007
    ....
  29. Pilot-Scale Libraries for High-throughput Screening
    AMOS SMITH; Fiscal Year: 2007
    ....
  30. IDO-expressing immunoregulatory dendritic cells
    David Munn; Fiscal Year: 2007
    ..The applicants hypothesize that IDO-mediated mechanisms may contribute to this pathologic state of acquired tolerance. ..
  31. DISCOVERY OF SMALL-MOLECULE ORPHANIN FQ RECEPTOR LIGANDS
    Nurulain T Zaveri; Fiscal Year: 2010
    ..The work proposed in this application will discover novel compounds that can be powerful analgesics with reduced tolerance and side effects, or potential treatments for drug abuse. ..
  32. 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...