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. 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
  2. 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
  3. 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
  4. pmc High rates of actin filament turnover in budding yeast and roles for actin in establishment and maintenance of cell polarity revealed using the actin inhibitor latrunculin-A
    K R Ayscough
    Department of Molecular and Cell Biology, University of California, Berkeley 94720 3202, USA
    J Cell Biol 137:399-416. 1997
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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

Detail Information

Publications232 found, 100 shown here

  1. 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...
  2. 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
    ....
  3. 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...
  4. pmc High rates of actin filament turnover in budding yeast and roles for actin in establishment and maintenance of cell polarity revealed using the actin inhibitor latrunculin-A
    K R Ayscough
    Department of Molecular and Cell Biology, University of California, Berkeley 94720 3202, USA
    J Cell Biol 137:399-416. 1997
    ..Finally, transient actin depolymerization caused many cells to abandon one bud site or mating projection and to initiate growth at a second site. Thus, actin filaments are also required for maintenance of an axis of cell polarity...
  5. 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...
  6. 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...
  7. 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
    ....
  8. 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...
  9. 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...
  10. 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...
  11. 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...
  12. 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...
  13. 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...
  14. 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...
  15. 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...
  16. 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...
  17. ncbi Localization of [3H]nicotine, [3H]cytisine, [3H]epibatidine, and [125I]alpha-bungarotoxin binding sites in the brain of Macaca mulatta
    Zhi yan Han
    CNRS URA 2182 Récepteurs et Cognition, Institut Pasteur, 75724 Paris Cedex 15, France
    J Comp Neurol 461:49-60. 2003
    ..The distribution of the binding sites for alpha-bungarotoxin is larger in the brain of rhesus monkeys than in rodent brain, suggesting a more important role of alpha7 receptors in primates...
  18. 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...
  19. pmc Actin disassembly by cofilin, coronin, and Aip1 occurs in bursts and is inhibited by barbed-end cappers
    Hao Yuan Kueh
    Department of Systems Biology, Harvard Medical School, Boston, MA 02115, USA
    J Cell Biol 182:341-53. 2008
    ..The differential effects of drugs in cells argue for physiological relevance of this new disassembly pathway and potentially explain discordant results previously found with these drugs...
  20. 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...
  21. pmc CFTR surface expression and chloride currents are decreased by inhibitors of N-WASP and actin polymerization
    Radhika Ganeshan
    Department of Physiology and Biophysics, Gregory Fleming James Cystic Fibrosis Research Center, University of Alabama at Birmingham, 1918 University Blvd, MCLM 985, Birmingham, AL 35294, USA
    Biochim Biophys Acta 1773:192-200. 2007
    ..Our studies implicate a role for N-WASP-mediated actin polymerization in regulating CFTR surface expression and channel activity...
  22. ncbi SSR180711, a novel selective alpha7 nicotinic receptor partial agonist: (1) binding and functional profile
    Bruno Biton
    Central Nervous System Research Department, Sanofi Aventis, Bagneux, France
    Neuropsychopharmacology 32:1-16. 2007
    ..Together, these results demonstrate that SSR180711 is a selective and partial agonist at human, rat and mouse alpha7 n-AChRs, increasing glutamatergic neurotransmission, ACh release and LTP in the hippocampus...
  23. ncbi The comparative pharmacology and up-regulation of rat neuronal nicotinic receptor subtype binding sites stably expressed in transfected mammalian cells
    Yingxian Xiao
    Department of Pharmacology, Georgetown University School of Medicine, Washington, DC 20057 2195, USA
    J Pharmacol Exp Ther 310:98-107. 2004
    ....
  24. ncbi Activation of ATP-sensitive K+ channels in the ventromedial hypothalamus amplifies counterregulatory hormone responses to hypoglycemia in normal and recurrently hypoglycemic rats
    Rory J McCrimmon
    Department of Internal Medicine and Endocrinology, Yale University School of Medicine, Section of Endocrinology, P O Box 208020, New Haven, CT 06520 8020, USA
    Diabetes 54:3169-74. 2005
    ..We also conclude that KCOs may offer a future potential therapeutic option for individuals with insulin-treated diabetes who develop defective counterregulation...
  25. pmc Nebulin regulates the assembly and lengths of the thin filaments in striated muscle
    Abigail S McElhinny
    Department of Cell Biology and Anatomy, University of Arizona, Tucson, AZ 85724, USA
    J Cell Biol 170:947-57. 2005
    ..These data are consistent with nebulin functioning as a thin filament ruler and provide insight into mechanisms dictating macromolecular assembly...
  26. pmc Differential effects of Latrunculin-A on myofibrils in cultures of skeletal muscle cells: insights into mechanisms of myofibrillogenesis
    Jushuo Wang
    Department of Cell and Developmental Biology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6058, USA
    Cell Motil Cytoskeleton 62:35-47. 2005
    ..These Lat-A and CapZ results are discussed in the context of various models of myofibrillogenesis...
  27. ncbi Phencyclidine-induced impairment in attention and response control depends on the background genotype of mice: reversal by the mGLU(2/3) receptor agonist LY379268
    Barbara Greco
    Department of Neuroscience, Istituto di Ricerche Farmacologiche Mario Negri, 20157 Milan, Italy
    Psychopharmacology (Berl) 179:68-76. 2005
    ..Converging evidence implicates glutamate neurotransmission in attention and inhibitory response control...
  28. 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...
  29. ncbi Protective role of group-II metabotropic glutamate receptors against nigro-striatal degeneration induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine in mice
    Giuseppe Battaglia
    I R C C S Istituto Neurologico Mediterraneo Neuromed, Localita Camerelle, 86077 Pozzilli, Italy
    Neuropharmacology 45:155-66. 2003
    ..We conclude that mGlu2/3 receptors play a protective role against MPTP toxicity, and that the efficacy of the agonist, LY379268, critically depends on the extent of the nigro-striatal lesion...
  30. ncbi Dissection of keratin dynamics: different contributions of the actin and microtubule systems
    Stefan Wöll
    Department of Anatomy, Johannes Gutenberg University Mainz, Becherweg 13, D 55128 Mainz, Germany
    Eur J Cell Biol 84:311-28. 2005
    ..We therefore conclude that keratin motility relies both on intact actin filaments and microtubules and is not dependent on epithelium-specific cellular factors...
  31. ncbi Involvement of the alpha3 subunit in central nicotinic binding populations
    Paul Whiteaker
    Institute for Behavioral Genetics, University of Colorado, Boulder, Colorado 80309, USA
    J Neurosci 22:2522-9. 2002
    ..However, widespread but lower levels of alpha3-independent -resistant [125I]epibatidine binding were also seen. Again, this may indicate the existence of an additional, minor population of non-alpha3 -resistant sites...
  32. 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
    ....
  33. ncbi Entamoeba invadens: enhancement of excystation and metacystic development by cytochalasin D
    A Makioka
    Department of Tropical Medicine, Jikei University School of Medicine, 3-25-8 Nishi-shinbashi, Minato-ku, Tokyo 105-8461, Japan
    Exp Parasitol 98:145-51. 2001
    ..Thus, the results indicate that cytochalasin D, unlike latrunculin A and jasplakinolide, caused enhancement of the excystation and metacystic development of this parasite...
  34. pmc Evaluating the potential of vacuolar ATPase inhibitors as anticancer agents and multigram synthesis of the potent salicylihalamide analog saliphenylhalamide
    Sylvain Lebreton
    Department of Biochemistry, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, TX 75390 9038, USA
    Bioorg Med Chem Lett 18:5879-83. 2008
    ..To further validate the potential of V-ATPase inhibitors as leads for cancer chemotherapy, we developed a multigram synthesis of the potent salicylihalamide analog saliphenylhalamide...
  35. pmc Rop GTPase-dependent dynamics of tip-localized F-actin controls tip growth in pollen tubes
    Y Fu
    Department of Botany and Plant Sciences, University of California, Riverside, California 92521, USA
    J Cell Biol 152:1019-32. 2001
    ..Together, these results indicate that the dynamics of tip actin are essential for tip growth and provide the first direct evidence to link Rho GTPase to actin organization in controlling cell polarity and polar growth in plants...
  36. 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...
  37. ncbi Actin microfilaments facilitate the retrograde transport from the Golgi complex to the endoplasmic reticulum in mammalian cells
    F Valderrama
    , Facultat de Medicina, , Universitat de Barcelona, E-08036 Barcelona, Spain
    Traffic 2:717-26. 2001
    ....
  38. pmc Role of actin and Myo2p in polarized secretion and growth of Saccharomyces cerevisiae
    T S Karpova
    Department of Cell Biology and Physiology, Washington University, St Louis, Missouri 63110, USA
    Mol Biol Cell 11:1727-37. 2000
    ..This effect is similar to that of latrunculin, suggesting that Myo2p interacts with filamentous actin. However, inhibition of Myo2p function by expression of its tail domain completely abolished growth...
  39. ncbi Nicotinic alpha5 subunit deletion locally reduces high-affinity agonist activation without altering nicotinic receptor numbers
    Robert W B Brown
    Institute for Behavioral Genetics, University of Colorado, Boulder, Colorado, USA
    J Neurochem 103:204-15. 2007
    ..Together, these results describe the receptor-level changes underlying altered behavioral responses to nicotine in nicotinic acetylcholine receptor alpha5 subunit-null mutants...
  40. ncbi Cytochalasin D and latrunculin affect chromosome behaviour during meiosis in crane-fly spermatocytes
    A Forer
    Biology Department, York University, Downsview, Ontario, Canada
    Chromosome Res 6:533-49. 1998
    ..As CD and LAT are different antiactin drugs, but have the same effect on chromosome behaviour, the results implicate actin in early interactions of chromosomes with spindle fibres and in anaphase chromosome movements...
  41. 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...
  42. 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...
  43. 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...
  44. 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...
  45. 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...
  46. 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...
  47. 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
    ....
  48. 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...
  49. 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...
  50. 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
    ....
  51. 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...
  52. 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...
  53. 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...
  54. 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...
  55. 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
    ....
  56. 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
    ....
  57. 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...
  58. 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...
  59. 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...
  60. 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...
  61. 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...
  62. 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...
  63. 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...
  64. 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...
  65. 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
    ....
  66. 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...
  67. 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
    ....
  68. 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...
  69. 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...
  70. 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...
  71. 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...
  72. 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...
  73. 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...
  74. 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
    ....
  75. 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
    ....
  76. 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...
  77. 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
    ....
  78. 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)...
  79. 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...
  80. 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...
  81. 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...
  82. 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...
  83. 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...
  84. 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...
  85. 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...
  86. 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...
  87. 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
    ....
  88. 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...
  89. 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...
  90. 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...
  91. 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...
  92. 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...
  93. 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...
  94. 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...
  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 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...
  97. 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...
  98. 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
    ....
  99. 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...
  100. 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...
  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
    Institut fur Pharmazeutische Chemie der Philipps Universitat Marburg, 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 Grants63

  1. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 2007
    ..abstract_text> ..
  2. NOVEL PHARMACOTHERAPY FOR TREATMENT OF COCAINE ADDICTION
    Frank Carroll; Fiscal Year: 2008
    ..abstract_text> ..
  3. 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. ..
  4. 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. ..
  5. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2004
    ....
  6. SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTS
    AMOS SMITH; Fiscal Year: 2007
    ..abstract_text> ..
  7. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2009
    ..In the course of these studies new methods will be developed that are of general utility for preparing drugs more economically. ..
  8. SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORS
    AMOS SMITH; Fiscal Year: 2001
    ..abstract_text> ..
  9. 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]..
  10. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  11. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  12. Radiotracer R and D in Nuclear Medicine and Neuroscience
    Yu Shin Ding; Fiscal Year: 2006
    ..abstract_text> ..
  13. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  14. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  15. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  16. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  17. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 2009
    ..Daphnicyclidin A. This recent discovery has revealed a new molecular architecture which exhibits significant antitumor activity. Our research will investigate strategies for chemical synthesis of these complex polycyclic systems. ..
  18. Synthesis through N-Acylnitrenium Ion Cyclization
    DUNCAN WARDROP; Fiscal Year: 2006
    ..abstract_text> ..
  19. 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. ..
  20. INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 2006
    ..The selective synthesis of contiguous stereotriads will advance basic methodology for asymmetric conjugate additions. ..
  21. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
  22. Forebrain-Cerebellar Interaction During Learning
    John Disterhoft; Fiscal Year: 2008
    ..The data gathered here will also be useful for understanding and treating deficits in learning and memory in young and aging persons. ..
  23. ASYMMETRIC SYNTHESIS OF IONOPHORE/MACROLIDE ANTIBIOTICS
    David Evans; Fiscal Year: 2005
    ..Our goal has been to set in place all of the reactions necessary for the rapid assemblage of any polyketide target structure. ..
  24. Sex Diffrerences in Opioid Antinociception
    Andrew Barrett; Fiscal Year: 2003
    ....
  25. ASYMMETRIC SYNTHESIS OF VANCOMYCIN ANTIBIOTICS
    David Evans; Fiscal Year: 2001
    ..During the course of this project we intend to confirm (correct) the absolute stereochemical assignments of the principal members of this family by total synthesis. ..
  26. NATURAL PRODUCT SYNTHESIS THROUGH TEMPLATE DIRECTED C-H
    DUNCAN WARDROP; Fiscal Year: 2003
    ..abstract_text> ..
  27. Effects of insulin on the mesoaccumbens dopamine system
    NICHOLAS BELLO; Fiscal Year: 2005
    ..Insulin's modulation of food-related dopamine release may serve to increase the positive effects of palatable foods to contribute to pathological overeating and diet-induced obesity. ..
  28. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  29. REGULATION OF SECRETION FROM HUMAN BASOPHILS
    Donald MacGlashan; Fiscal Year: 2009
    ..A population of subjects will be examined for this relationship. ..
  30. Chemical Genetic Analysis of Platelet Granule Secretion
    Robert Flaumenhaft; Fiscal Year: 2008
    ..Once identified, compounds will be tested in a previously established battery of platelet function tests and evaluated for antithrombotic potential in an in vivo murine model of thrombus formation. [unreadable] [unreadable] [unreadable]..
  31. Enteric Nervous System 2003
    Keith Sharkey; Fiscal Year: 2003
    ..From this picture there will be gaps - these are the challenges for the future. ..
  32. PRESYNAPTIC MECHANISMS IN THE INTESTINE
    James Galligan; Fiscal Year: 2008
    ..It is also anticipated that these studies will identify new targets for drugs that can be used to treat GI motility disorders. ..
  33. 5-LIPOXYGENASE PRODUCTS IN ASTHMATIC IMMUNE RESPONSE
    William Henderson; Fiscal Year: 2008
    ..abstract_text> ..
  34. Natural Product Leads for Drug Development
    KATHLYN PARKER; Fiscal Year: 2009
    ..Molecular modeling will allow the design of candidates for more active drugs. Candidates will be evaluated in the squalene synthase assay. Collaborations for the medicinal chemistry components of the project have been arranged. ..
  35. MYRIAPORONES: SYNTHETIC AND BIOLOGICAL STUDIES
    Richard Taylor; Fiscal Year: 2003
    ..abstract_text> ..
  36. TRAINING PROGRAM IN MOLECULAR CELL BIOLOGY OF CANCER
    James Keen; Fiscal Year: 2003
    ..The goal of this Program is to develop highly trained, technically competent research scientists capable of performing and eventually directing research in the molecular cell biology of cancer. ..
  37. THE ROLE OF EPSILON SUBUNIT IN GABAA RECEPTOR FUNCTION
    David C Perry; Fiscal Year: 2010
    ..A better understanding of GABAA receptors and their potential for adaptation will help increase our understanding of changes in neuronal inhibition during epilepsy. ..
  38. EICOSANOIDS AND PULMONARY VASCULAR TONE
    SANDRA PFISTER; Fiscal Year: 2002
    ....
  39. PHEROMONES--IDENTIFICATION/BIOCHEMICAL STUDIES
    Milos Novotny; Fiscal Year: 2001
    ..Understanding the aspects of chemical communication in the species could also be important in a population control of wild rodents. ..
  40. KILLER/DR5 AND TUMORIGENESIS
    Wafik El Deiry; Fiscal Year: 2001
    ..These experiments could lead to novel strategies for anti-cancer therapy. ..
  41. Study on Thalidomide as BACE1 inhibitor in Alzhiemer's disease
    Marwan N Sabbagh; Fiscal Year: 2010
    ..We propose that Thalidomide may represent a BACE1 inhibitor. ..
  42. GONADOTROPIN-RELEASING HORMONE ACTION
    P Michael Conn; Fiscal Year: 2008
    ..The specific aims of this study will advance both our basic understanding and will identify new sites and approaches potentially amenable to therapeutic intervention. [unreadable] [unreadable]..
  43. Insulin Regulation of Adipocyte Microtubules
    ANN OLSON; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  44. REGULATION OF DETRUSOR SMOOTH MUSCLE CONTRACTION
    PAUL RATZ; Fiscal Year: 2005
    ..Collectively, these studies will provide new insights into the cellular mechanisms regulating DSM contractions. ..
  45. Vaccine Effects on Fetal Nicotine Exposure in Rats
    Paul Pentel; Fiscal Year: 2005
    ..abstract_text> ..
  46. Asymmetric Synthesis of Cytotoxic Natural Products
    Robert Coleman; Fiscal Year: 2005
    ..abstract_text> ..
  47. Antipsychotics: Temporal Effects on Cognitive Function
    Alvin Terry; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  48. Nicotine Modulation of Caspases in Non-Neuronal Cells
    LORISE GAHRING; Fiscal Year: 2006
    ....
  49. TRIOXANES FOR CHEMOTHERAPY OF MALARIA AND CANCER
    Gary Posner; Fiscal Year: 2005
    ....
  50. SYNTHESIS OF ANTITUMOR AGENTS AND RELATED CHEMISTRY
    Steven Burke; Fiscal Year: 2004
    ..5. To exploit, at the strategic level, symmetry and novel strategies for symmetry-breaking to simplify complex targets and to provide short and efficient syntheses thereof. ..
  51. Experimental approaches to understanding the ENS and its disorders
    James Galligan; Fiscal Year: 2006
    ..This will help the attendees develop a network of professional contacts who can help the young investigator in the career development process. [unreadable] [unreadable]..
  52. Cannabinoid Mechanisms in Human Gastrointestinal Motor and Sensory Functions
    MICHAEL L CAMILLERI; Fiscal Year: 2010
    ..These actions may be relevant to develop new treatments for IBS. The studies will also provide further understanding of the potential of medications like medical marijuana on stomach function that may be relevant to appetite control. ..
  53. Azinomycins - Total Synthesis and Mechanism of Action
    Robert Coleman; Fiscal Year: 2007
    ..abstract_text> ..
  54. Inhibition of Macrophage Innate Immunity in Tuberculosis
    WILLIAM NAUSEEF; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  55. NO-CGMP INHIBITION OF UROGENITAL SMOOTH MUSCLE
    Christopher Rembold; Fiscal Year: 2004
    ....
  56. Mapping the D2/D3 Dopamine Receptor Binding Sites
    ROBERT LUEDTKE; Fiscal Year: 2004
    ..LB dopamine receptor selective compounds bind to the neumtransmitter binding sate and 2) provide additional structural information that will assist us in the design of novel compounds with increased selectivity for LB dopamine receptors ..
  57. ALPHA-2 ADRENERGIC CONTROL OF COLONIC FUNCTION IN IBS
    Michael Camilleri; Fiscal Year: 2007
    ..abstract_text> ..
  58. Podocyte Protein Alterations Induced by Glucocorticoids
    Richard Ransom; Fiscal Year: 2005
    ..Identification of a potential mechanism for glucocorticoid action in the treatment of NS would permit the development of more highly targeted and less toxic therapies for this very common form of kidney disease. ..
  59. LOCAL AND GLOBAL CONFORMATIONS OF SUPERCOILED DNA
    Yuri Lyubchenko; Fiscal Year: 2007
    ..abstract_text> ..
  60. Role of Rho Kinase in Aqueous Humor Outflow Pathway
    P Rao; Fiscal Year: 2004
    ..Identification of specific signaling mechanisms regulating function of outflow pathway tissues could enable the design of target-specific approaches to the treatment of glaucoma. ..
  61. 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. ..
  62. Cellular Signaling Mechanisms in Macrophage Activation.
    Joseph Cuschieri; Fiscal Year: 2007
    ..Through an enhanced understanding of these mechanisms it is our goal that potential therapeutic targets may be discovered to regulate the inflammatory response following trauma/hemorrhage and ischemia/reperfusion. ..