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 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
  2. 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
  3. 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
  4. 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
  5. pmc 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
  6. pmc Phospholipids undergo hop diffusion in compartmentalized cell membrane
    Takahiro Fujiwara
    Kusumi Membrane Organizer Project, Exploratory Research for Advanced Technology Organization, Japan Science and Technology Corporation, Nagoya 460 0012, Japan
    J Cell Biol 157:1071-81. 2002
  7. pmc Actin filament dynamics are dominated by rapid growth and severing activity in the Arabidopsis cortical array
    Christopher J Staiger
    Department of Biological Sciences, Hansen Life Sciences Research Building, Purdue University, West Lafayette, IN 47907, USA
    J Cell Biol 184:269-80. 2009
  8. ncbi Local actin polymerization and dynamin recruitment in SV40-induced internalization of caveolae
    Lucas Pelkmans
    Swiss Federal Institute of Technology Zurich ETHZ, HPM1 Building, ETH Honggerberg, CH 8093 Zurich, Switzerland
    Science 296:535-9. 2002
  9. pmc 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
  10. pmc Chemoattractant-induced phosphatidylinositol 3,4,5-trisphosphate accumulation is spatially amplified and adapts, independent of the actin cytoskeleton
    Chris Janetopoulos
    Department of Cell Biology, Johns Hopkins University School of Medicine, 725 North Wolfe Street, Baltimore, MD 21205, USA
    Proc Natl Acad Sci U S A 101:8951-6. 2004

Detail Information

Publications213 found, 100 shown here

  1. 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...
  2. 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...
  3. 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...
  4. 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...
  5. pmc 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...
  6. pmc Phospholipids undergo hop diffusion in compartmentalized cell membrane
    Takahiro Fujiwara
    Kusumi Membrane Organizer Project, Exploratory Research for Advanced Technology Organization, Japan Science and Technology Corporation, Nagoya 460 0012, Japan
    J Cell Biol 157:1071-81. 2002
    ..We propose that various transmembrane proteins anchored to the actin-based membrane skeleton meshwork act as rows of pickets that temporarily confine phospholipids...
  7. pmc Actin filament dynamics are dominated by rapid growth and severing activity in the Arabidopsis cortical array
    Christopher J Staiger
    Department of Biological Sciences, Hansen Life Sciences Research Building, Purdue University, West Lafayette, IN 47907, USA
    J Cell Biol 184:269-80. 2009
    ..These observations indicate a mechanism inconsistent with treadmilling. Instead, cortical actin filament dynamics resemble the stochastic dynamics of an in vitro biomimetic system for actin assembly...
  8. ncbi Local actin polymerization and dynamin recruitment in SV40-induced internalization of caveolae
    Lucas Pelkmans
    Swiss Federal Institute of Technology Zurich ETHZ, HPM1 Building, ETH Honggerberg, 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...
  9. pmc 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
    ....
  10. pmc Chemoattractant-induced phosphatidylinositol 3,4,5-trisphosphate accumulation is spatially amplified and adapts, independent of the actin cytoskeleton
    Chris Janetopoulos
    Department of Cell Biology, Johns Hopkins University School of Medicine, 725 North Wolfe Street, Baltimore, MD 21205, USA
    Proc Natl Acad Sci U S A 101:8951-6. 2004
    ..These results support a local excitation/global inhibition model and argue against other schemes proposed to explain directional sensing...
  11. 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...
  12. 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
    ....
  13. 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...
  14. 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...
  15. pmc 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...
  16. ncbi Evolved regulation of gonadotropin-releasing hormone receptor cell surface expression
    Jo Ann Janovick
    Oregon Health and Science University, Portland, OR 97239 3098, USA
    Endocrine 22:317-27. 2003
    ..The data further reveal that additional modifications must have occurred in primates that are important for both the diminution of the PME and the development of the dominant negative effect of the mutants...
  17. ncbi Coupling between clathrin-coated-pit invagination, cortactin recruitment, and membrane scission observed in live cells
    Christien J Merrifield
    MRC Laboratory of Molecular Biology, Hills Road, Cambridge CB2 2QH, United Kingdom
    Cell 121:593-606. 2005
    ..We propose that CCP invagination, actin polymerization, and CCV formation are highly coordinated for efficient endocytosis...
  18. ncbi Human loss-of-function gonadotropin-releasing hormone receptor mutants retain wild-type receptors in the endoplasmic reticulum: molecular basis of the dominant-negative effect
    Shaun P Brothers
    Division of Neuroscience, Oregon National Primate Research Center and Oregon Health and Science University, Beaverton, Oregon 97006, USA
    Mol Endocrinol 18:1787-97. 2004
    ....
  19. ncbi Disruption of the actin cytoskeleton results in nuclear factor-kappaB activation and inflammatory mediator production in cultured human intestinal epithelial cells
    Zoltán H Németh
    Department of Surgery, UMD NJ New Jersey Medical School, Newark, New Jersey 07103, USA
    J Cell Physiol 200:71-81. 2004
    ..These results demonstrate that the actin cytoskeleton plays an important role in the regulation of NF-kappaB activation and inflammatory events in intestinal epithelial cells...
  20. pmc Endoplasmic reticulum dynamics, inheritance, and cytoskeletal interactions in budding yeast
    K L Fehrenbacher
    Department of Anatomy and Cell Biology, Columbia University, College of Physicians and Surgeons, New York, New York 10032, USA
    Mol Biol Cell 13:854-65. 2002
    ....
  21. ncbi Cortical microtubule arrays undergo rotary movements in Arabidopsis hypocotyl epidermal cells
    Jordi Chan
    Department of Cell and Developmental Biology, John Innes Centre, Norwich NR4 7UH, UK
    Nat Cell Biol 9:171-5. 2007
    ..Rotary movements could explain how the angle of cellulose microfibrils can change from layer to layer in the polylamellate cell wall...
  22. 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...
  23. 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...
  24. 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
    ..The etiology of dementia that occurs in patients with schizophrenia is not well understood. Nicotinic acetylcholine receptors have been implicated in cognitive function, and deficits in these receptors have been reported in schizophrenia...
  25. 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
    ..2/SUR2A), smooth muscle (Kir6.2/SUR2B) and pancreatic beta cell (Kir6.2/SUR1) types of K(ATP) channel...
  26. 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...
  27. 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
    ....
  28. 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...
  29. 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...
  30. 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...
  31. 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...
  32. 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...
  33. 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...
  34. 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...
  35. 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
    ..Jasplakinolide (JP), a compound that stabilizes actin filaments, was administered to evaluate the effect of actin stabilization. Apoptosis was evaluated at 3 h of ex vivo reperfusion using the isolated perfused rat kidney (IPK) model...
  36. ncbi Computational comparison of microtubule-stabilising agents laulimalide and peloruside with taxol and colchicine
    Oriol Pineda
    Departament de Quimica Organica, Facultat de Quimica, 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...
  37. 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
    ....
  38. 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...
  39. 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...
  40. 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...
  41. 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
    ....
  42. 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...
  43. 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
    ....
  44. 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...
  45. pmc 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...
  46. 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...
  47. 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
    ..The present study was designed to investigate whether norcantharidin exerts cytotoxic activity against colorectal cancer cells by inducing apoptosis and to examine the possible mechanism in the phenomenon...
  48. pmc 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...
  49. 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
    ....
  50. 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...
  51. pmc 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...
  52. pmc 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
    ....
  53. pmc 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...
  54. 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
    ....
  55. doi 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...
  56. pmc 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...
  57. 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...
  58. pmc 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...
  59. 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...
  60. 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...
  61. pmc 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...
  62. 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...
  63. 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
    ....
  64. 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)...
  65. 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
    ....
  66. pmc 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...
  67. 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...
  68. 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...
  69. 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...
  70. 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...
  71. 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...
  72. 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
    ....
  73. 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...
  74. 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...
  75. 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...
  76. 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...
  77. 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
    ....
  78. 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...
  79. 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...
  80. doi 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...
  81. 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...
  82. 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, Villigen and University Hospital of Zürich, Ramistrasse 100, CH 8091 Zurich, Switzerland
    Eur J Med Chem 41:640-50. 2006
    ....
  83. 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...
  84. 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...
  85. 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
    ....
  86. 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...
  87. 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...
  88. ncbi Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists
    F Ivy Carroll
    Chemistry and Life Sciences, Research Triangle Institute, P O Box 12194, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 48:1221-8. 2005
    ....
  89. 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
    ....
  90. 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...
  91. 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...
  92. 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
    ....
  93. 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...
  94. 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...
  95. 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
    ....
  96. 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...
  97. ncbi Ligand-receptor interaction at the neural nicotinic acetylcholine binding site: a theoretical model
    A Morreale
    Departamento de Quimica Organica, Facultad de Farmacia, Universidad de Alcala, 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...
  98. 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...
  99. 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...
  100. 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)...
  101. 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...

Research Grants151 found, 100 shown here

  1. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2003
    ....
  2. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 1999
    ..abstract_text> ..
  3. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 2007
    ..abstract_text> ..
  4. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2004
    ....
  5. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2006
    ....
  6. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2008
    ..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. ..
  7. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2004
    ..Compounds that are potent delta selective opioid receptor inverse agonists will be evaluated by Dr. Chris Evans (UCLA) in a chronic antinociception rat model. ..
  8. 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. ..
  9. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2003
    ..abstract_text> ..
  10. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 1991
    ....
  11. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2008
    ..Compounds that are potent delta selective opioid receptor inverse agonists will be evaluated by Dr. Chris Evans (UCLA) in a chronic antinociception rat model. ..
  12. NOVEL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    Frank Carroll; Fiscal Year: 2000
    ..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. ..
  13. 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. ..
  14. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2002
    ....
  15. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2002
    ..abstract_text> ..
  16. NOVEL PHARMACOTHERAPY FOR TREATMENT OF COCAINE ADDICTION
    Frank Carroll; Fiscal Year: 2008
    ..abstract_text> ..
  17. 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. ..
  18. 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. ..
  19. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2001
    ..abstract_text> ..
  20. Design and Development of Pharmacotherapies for Treating Stimulant Abuse
    Frank Carroll; Fiscal Year: 2009
    ..3) To continue on a limited basis our development of selected 3-phenyltropane analogs as second-generation pharmacotherapies to treat cocaine addiction. ..
  21. Development of Pharmacotherapies for Nicotine Addiction
    Frank Carroll; Fiscal Year: 2008
    ....
  22. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2006
    ..Compounds that are potent delta selective opioid receptor inverse agonists will be evaluated by Dr. Chris Evans (UCLA) in a chronic antinociception rat model. ..
  23. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2000
    ..abstract_text> ..
  24. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2000
    ..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. ..
  25. Development of Pharmacotherapies for Nicotine Addiction
    Frank Carroll; Fiscal Year: 2005
    ....
  26. 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. ..
  27. SELECTIVE OPIOID ANTAGONIST AS MEDICATION FOR DRUG ABUSE
    Frank Carroll; Fiscal Year: 2005
    ..Compounds that are potent delta selective opioid receptor inverse agonists will be evaluated by Dr. Chris Evans (UCLA) in a chronic antinociception rat model. ..
  28. 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. ..
  29. 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. ..
  30. 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. ..
  31. NOVEL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    Frank Carroll; Fiscal Year: 1999
    ..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. ..
  32. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 1999
    ..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. ..
  33. DEVELOPMENT OF LIGANDS FOR NICOTINIC RECEPTORS
    Frank Carroll; Fiscal Year: 2005
    ....
  34. SYNTHESIS OF BIOACTIVE NATURAL PRODUCTS
    AMOS SMITH; Fiscal Year: 2000
    ..This philosophy of "unified synthetic strategies" will be further developed in this proposal. ..
  35. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2004
    ..The mechanism and synthetic utility of these cyclizations will be developed. ..
  36. SYNTHESIS OF BIOACTIVE NATURAL PRODUCTS
    AMOS SMITH; Fiscal Year: 1992
    ..We believe that this philosophy of "unified synthetic strategies" will be further developed by this proposal...
  37. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2003
    ....
  38. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2001
    ....
  39. ANTICANCER AGENTS--STRUCTURE AND SYNTHESIS
    AMOS SMITH; Fiscal Year: 2006
    ..Thus, as we develop an approach to each target structure, we will also prepare model compounds designed to permit the elucidation of structure-activity relationships. ..
  40. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2006
    ..In the course of these studies new methods will be developed that are of general utility for preparing drugs more economically. [unreadable] [unreadable]..
  41. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 1999
    ..8-1.1 mg/mL. The key step in this synthesis is the intramolecular Diels-Alder reaction of trienyl glyoxylate 192 to give 191 and stereoisomers. ..
  42. 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...
  43. 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...
  44. Pilot-Scale Libraries for High-throughput Screening
    AMOS SMITH; Fiscal Year: 2008
    ....
  45. 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. ..
  46. RECEPTORS FOR COCAINE AND DOPAMINE
    Philip Seeman; Fiscal Year: 1991
    ..The availability of clones for these receptors would facilitate new drug design and provide new markers for disease linkage studies in families...
  47. RECEPTORS FOR COCAINE AND DOPAMINE
    Philip Seeman; Fiscal Year: 1992
    ..The availability of clones for these receptors would facilitate new drug design and provide new markers for disease linkage studies in families...
  48. RECEPTORS MEDIATING DRUG DEPENDENCE
    Philip Seeman; Fiscal Year: 1999
    ....
  49. Peripheral Receptor Mechanisms in Orofacial Muscle Pain
    JIN RO; Fiscal Year: 2007
    ..These studies will contribute to understanding the pathophysiology of chronic orofacial muscle pain and provide direct insights for the development of new treatment modalities. ..
  50. 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. ..
  51. IDO-expressing immunoregulatory dendritic cells
    David Munn; Fiscal Year: 2006
    ..The applicants hypothesize that IDO-mediated mechanisms may contribute to this pathologic state of acquired tolerance. ..
  52. SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTS
    AMOS SMITH; Fiscal Year: 2006
    ..abstract_text> ..
  53. LOCAL AND GLOBAL CONFORMATIONS OF SUPERCOILED DNA
    Yuri Lyubchenko; Fiscal Year: 2007
    ..abstract_text> ..
  54. NMR systems : 2 Bruker Avance 500 Consoles
    AMOS SMITH; Fiscal Year: 2006
    ..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. [unreadable] [unreadable] [unreadable]..
  55. SYNTHESIS OF BIOACTIVE NATURAL PRODUCTS
    Amos B Smith; Fiscal Year: 2010
    ..Our experience with discodermolide gives us great confidence in this area. ..
  56. TRAUMA & SEPSIS INDUCED CHANGES IN IMMUNE CELL MEMBRANE RECEPTOR TRAFFICKING
    Joseph Cuschieri; Fiscal Year: 2010
    ....
  57. 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. ..
  58. 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. ..
  59. IDO-mediated immune regulation in established tumors
    David H Munn; Fiscal Year: 2010
    ....
  60. 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. ..
  61. Alzhelmer's Disease Drug Development Program
    AMOS SMITH; Fiscal Year: 2008
    ....
  62. Alpha-Conotoxin MII: A Selective Nicotinic Receptor Probe
    Paul Whiteaker; Fiscal Year: 2008
    ..These insights may also guide the design of nicotinic therapies for other conditions. ..
  63. Discovery of Bifunctional NOP/Opioid Receptor Ligands for Drug Abuse Therapy
    Nurulain T Zaveri; Fiscal Year: 2010
    ....
  64. Regulation of vascular smooth muscle calcium sensitivity
    PAUL RATZ; Fiscal Year: 2008
    ..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. ..
  65. Trabecular Meshwork Cytoskeletal Signaling-Regulation of Aqueous Humor Outflow
    P Rao; Fiscal Year: 2008
    ....
  66. Role of IDO malignancy
    David Munn; Fiscal Year: 2007
    ....
  67. TRAUMA & SEPSIS INDUCED CHANGES IN IMMUNE CELL MEMBRANE RECEPTOR TRAFFICKING
    Joseph Cuschieri; Fiscal Year: 2007
    ....
  68. Pilot-Scale Libraries for High-throughput Screening
    AMOS SMITH; Fiscal Year: 2007
    ....
  69. 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. ..
  70. 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. ..
  71. Rho GTpase in the Lens - Role in Growth and Development
    P Rao; Fiscal Year: 2004
    ....
  72. REGULATION OF DETRUSOR SMOOTH MUSCLE CONTRACTION
    PAUL RATZ; Fiscal Year: 2003
    ..Collectively, these studies will provide new insights into the cellular mechanisms regulating DSM contractions. ..
  73. REGULATION OF VASCULAR SMOOTH MUSCLE Ca2+ SENSITIVITY
    PAUL RATZ; Fiscal Year: 2002
    ..Collectively, these studies will provide new insights into the cellular mechanisms regulating Ca2+ sensitivity and VSM reactivity to contractile stimuli. ..
  74. 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...
  75. ASYMMETRIC SYNTHESIS OF IONOPHORE & MACROLIDE ANTIBIOTIC
    David Evans; Fiscal Year: 1992
    ....