azepines

Summary

Summary: Seven membered heterocyclic rings containing a NITROGEN atom.

Top Publications

  1. pmc Targeting MYC dependence in cancer by inhibiting BET bromodomains
    Jennifer A Mertz
    Constellation Pharmaceuticals, Inc, Cambridge, MA 02142, USA
    Proc Natl Acad Sci U S A 108:16669-74. 2011
  2. doi Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays
    Mark G Manfredi
    Millennium Pharmaceuticals, Inc, Cambridge, 40 Landsdowne Street, Cambridge, MA 02139, USA
    Clin Cancer Res 17:7614-24. 2011
  3. doi Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease
    David B Henley
    Eli Lilly and Company, Lilly Corporate Center, Clinical Research Physician, Alzheimer s Team, DC 6161, Indianapolis, IN 46285 6161, USA
    Expert Opin Pharmacother 10:1657-64. 2009
  4. ncbi Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139
    Thomas A Lanz
    Pfizer, Inc, Eastern Point Rd, MS 8220 4183, Groton, CT 06340, USA
    J Pharmacol Exp Ther 319:924-33. 2006
  5. pmc Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice
    Maxime Cazorla
    Neurobiology and Molecular Pharmacology, Centre de psychiatrie et Neurosciences, UMR 894 INSERM Université Paris Descartes, Paris, France
    J Clin Invest 121:1846-57. 2011
  6. ncbi Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase
    Stefan Kubicek
    Research Institute of Molecular Pathology, Vienna Biocenter, Dr Bohrgasse 7, A 1030 Vienna, Austria
    Mol Cell 25:473-81. 2007
  7. pmc Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria
    Wolfgang Haas
    Bausch and Lomb, Inc, 1400 N Goodman St, Rochester, NY 14609, USA
    Antimicrob Agents Chemother 53:3552-60. 2009
  8. pmc Small-molecule inhibition of BRDT for male contraception
    Martin M Matzuk
    Department of Pathology and Immunology, Baylor College of Medicine, Houston, TX 77030, USA
    Cell 150:673-84. 2012
  9. pmc Identification of regulators of polyploidization presents therapeutic targets for treatment of AMKL
    Qiang Wen
    Division of Hematology Oncology, Northwestern University, Chicago, IL 60611, USA
    Cell 150:575-89. 2012
  10. pmc Growth inhibition and differentiation of human breast cancer cells by the PAFR antagonist WEB-2086
    C Cellai
    Department of Experimental Pathology and Oncology, School of Medicine, University of Florence, Viale G B Morgagni 50, 50134 Florence, Italy
    Br J Cancer 94:1637-42. 2006

Research Grants

Detail Information

Publications207 found, 100 shown here

  1. pmc Targeting MYC dependence in cancer by inhibiting BET bromodomains
    Jennifer A Mertz
    Constellation Pharmaceuticals, Inc, Cambridge, MA 02142, USA
    Proc Natl Acad Sci U S A 108:16669-74. 2011
    ..These findings demonstrate that pharmacologic inhibition of MYC is achievable through targeting BET bromodomains. Such inhibitors may have clinical utility given the widespread pathogenetic role of MYC in cancer...
  2. doi Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays
    Mark G Manfredi
    Millennium Pharmaceuticals, Inc, Cambridge, 40 Landsdowne Street, Cambridge, MA 02139, USA
    Clin Cancer Res 17:7614-24. 2011
    ..Here, we describe preclinical characterization of alisertib (MLN8237), a selective AAK inhibitor, incorporating these novel pharmacodynamic assays...
  3. doi Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease
    David B Henley
    Eli Lilly and Company, Lilly Corporate Center, Clinical Research Physician, Alzheimer s Team, DC 6161, Indianapolis, IN 46285 6161, USA
    Expert Opin Pharmacother 10:1657-64. 2009
    ..Therefore, pharmacological agents that reduce A beta formation may be of therapeutic benefit...
  4. ncbi Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139
    Thomas A Lanz
    Pfizer, Inc, Eastern Point Rd, MS 8220 4183, Groton, CT 06340, USA
    J Pharmacol Exp Ther 319:924-33. 2006
    ..These results suggest that LY-450139 modulates the gamma-secretase complex, eliciting Abeta lowering at high concentrations but Abeta elevation at low concentrations...
  5. pmc Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice
    Maxime Cazorla
    Neurobiology and Molecular Pharmacology, Centre de psychiatrie et Neurosciences, UMR 894 INSERM Université Paris Descartes, Paris, France
    J Clin Invest 121:1846-57. 2011
    ..We further propose that ANA-12 may be a valuable tool for studying BDNF/TrkB signaling and may constitute a lead compound for developing the next generation of therapeutic agents for the treatment of mood disorders...
  6. ncbi Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase
    Stefan Kubicek
    Research Institute of Molecular Pathology, Vienna Biocenter, Dr Bohrgasse 7, A 1030 Vienna, Austria
    Mol Cell 25:473-81. 2007
    ..Our data identify a biologically active HMTase inhibitor that allows for the transient modulation of H3K9me2 marks in mammalian chromatin...
  7. pmc Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria
    Wolfgang Haas
    Bausch and Lomb, Inc, 1400 N Goodman St, Rochester, NY 14609, USA
    Antimicrob Agents Chemother 53:3552-60. 2009
    ..Besifloxacin demonstrated potent, broad-spectrum activity, which was particularly notable against gram-positive and gram-negative isolates that were resistant to other fluoroquinolones and classes of antibacterial agents...
  8. pmc Small-molecule inhibition of BRDT for male contraception
    Martin M Matzuk
    Department of Pathology and Immunology, Baylor College of Medicine, Houston, TX 77030, USA
    Cell 150:673-84. 2012
    ..These data establish a new contraceptive that can cross the blood:testis boundary and inhibit bromodomain activity during spermatogenesis, providing a lead compound targeting the male germ cell for contraception...
  9. pmc Identification of regulators of polyploidization presents therapeutic targets for treatment of AMKL
    Qiang Wen
    Division of Hematology Oncology, Northwestern University, Chicago, IL 60611, USA
    Cell 150:575-89. 2012
    ..Our findings provide a rationale to support clinical trials of MLN8237 and other inducers of polyploidization and differentiation in AMKL...
  10. pmc Growth inhibition and differentiation of human breast cancer cells by the PAFR antagonist WEB-2086
    C Cellai
    Department of Experimental Pathology and Oncology, School of Medicine, University of Florence, Viale G B Morgagni 50, 50134 Florence, Italy
    Br J Cancer 94:1637-42. 2006
    ..Overall, WEB-2086 can be proposed as an effective antiproliferative and differentiative agent with interesting translational opportunities to treat breast cancers in support to conventional chemotherapy...
  11. pmc Initial testing of the aurora kinase A inhibitor MLN8237 by the Pediatric Preclinical Testing Program (PPTP)
    John M Maris
    Children s Hospital of Philadelphia, Philadelphia, Pennsylvania 19104 4318, USA
    Pediatr Blood Cancer 55:26-34. 2010
    ..MLN8237 is a small molecule inhibitor of Aurora Kinase A (AURKA) that is currently in early phase clinical testing. AURKA plays a pivotal role in centrosome maturation and spindle formation during mitosis...
  12. pmc Myosin light chain kinase is involved in lipopolysaccharide-induced disruption of colonic epithelial barrier and bacterial translocation in rats
    Raphael Moriez
    Institut National de la Recherche Agronomique, Neuro Gastroenterology and Nutrition Unit, 180 chemin de Tournefeuille, BP 3, 31931 Toulouse Cedex 9, France
    Am J Pathol 167:1071-9. 2005
    ..Inhibition of MLCK-dependent colonocyte cytoskeleton contraction by ML-7 prevents the LPS-induced alterations of CPP and its subsequent effects...
  13. pmc A gamma-secretase inhibitor decreases amyloid-beta production in the central nervous system
    Randall J Bateman
    Department of Neurology, Washington University School of Medicine, St Louis, MO, USA
    Ann Neurol 66:48-54. 2009
    ..The objective of this study was to determine the effects of a gamma-secretase inhibitor on the production of Abeta in the human CNS...
  14. ncbi PAF antagonist treatment reduces pro-inflammatory cytokine mRNA after spinal cord injury
    Mary Ellen Hostettler
    Department of Anatomy and Neurobiology, University of Kentucky Medical Center, Lexington 40536, USA
    Neuroreport 13:21-4. 2002
    ..p.) 15 min prior to injury significantly decreased mRNA levels for all three cytokines at 6 h post-injury, but not at I h post-injury. These results demonstrate a role for PAF in proinflammatory cytokine induction after SCI...
  15. pmc Self-organized podosomes are dynamic mechanosensors
    Olivier Collin
    Department of Mechanical Science and Engineering, University of Illinois at Urbana Champaign, Urbana, IL 61801, USA
    Curr Biol 18:1288-94. 2008
    ..Our results suggest that podosomes are dynamic mechanosensors in which interactions of myosin tension and actin dynamics are crucial for regulating these self-organized structures in living cells...
  16. ncbi Myosin light chain kinase inhibitors induce retraction of mature oligodendrocyte processes
    María G Thomas
    IIB Fundación Campomar, IIB FCEyN, University of Buenos Aires and IIBBA CONICET, Buenos Aires, Argentina
    Neurochem Res 27:1305-12. 2002
    ..Our results suggest that the adhesion of the myelinating processes to the substrate depends on MLC phosphorylation, thus likely implicating myosin IIA...
  17. doi Mechanistic insight into WEB-2170-induced apoptosis in human acute myelogenous leukemia cells: the crucial role of PTEN
    Cristina Cellai
    Department of Experimental Pathology and Oncology, University of Florence, 50134 Florence, Italy
    Exp Hematol 37:1176-1185.e21. 2009
    ..This study aimed to investigate the mechanisms of action of WEB-2170, an inverse agonist of platelet-activating factor receptor, capable of inducing apoptosis in human acute myelogenous leukemia (AML) cells...
  18. ncbi WEB-2086 and WEB-2170 trigger apoptosis in both ATRA-sensitive and -resistant promyelocytic leukemia cells and greatly enhance ATRA differentiation potential
    A Laurenzana
    Department of Experimental Pathology and Oncology, University of Florence, Italy
    Leukemia 19:390-5. 2005
    ....
  19. doi Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development
    Michael A Letavic
    Johnson and Johnson Pharmaceutical Research and Development L L C, 3210 Merryfield Row, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:4210-4. 2010
    ..Several compounds were extensively profiled pre-clinically leading to the identification of two compounds suitable for nomination as development candidates...
  20. pmc Relative inhibitory potency of molinate and metabolites with aldehyde dehydrogenase 2: implications for the mechanism of enzyme inhibition
    Erin M G Allen
    Division of Medicinal and Natural Products Chemistry, College of Pharmacy, The University of Iowa, Iowa City, Iowa 52242, USA
    Chem Res Toxicol 23:1843-50. 2010
    ..It was determined that molinate sulfone is capable of covalently modifying Cys residues, including catalytic Cys302 of ALDH, accounting for the observed enzyme inhibition...
  21. pmc Ca2+-store-dependent and -independent reversal of Stim1 localization and function
    Jeremy T Smyth
    Laboratory of Signal Transduction, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, PO Box 12233, Research Triangle Park, NC 27709, USA
    J Cell Sci 121:762-72. 2008
    ..We conclude that SOCE is tightly coupled to formation of Stim1 puncta, and both SOCE and puncta formation involve a dynamic, reversible signaling complex that probably consists of components in addition to Stim1 and Orai channels...
  22. doi Cyclic stretch-induced stress fiber dynamics - dependence on strain rate, Rho-kinase and MLCK
    Chin Fu Lee
    Department of Biomedical Engineering, Texas A and M University, College Station, TX 77843 3120, United States
    Biochem Biophys Res Commun 401:344-9. 2010
    ..These results shed new light on the mechanism by which stress fibers reorient in response to cyclic stretch in different regions of the actin cytoskeleton...
  23. ncbi Pharmacological properties of GABAA receptors containing gamma1 subunits
    S Khom
    Department of Pharmacology and Toxicology, University of Vienna, Austria
    Mol Pharmacol 69:640-9. 2006
    ..05). These data provide new insight into the pharmacological properties of GABA(A) receptors containing gamma(1) subunits and may aid in the design of specific ligands for this receptor subtype...
  24. ncbi Selective inhibition of catalytic activity of smooth muscle myosin light chain kinase
    M Saitoh
    J Biol Chem 262:7796-801. 1987
    ..The potent vaso-relaxing effect of ML-9 on rabbit vascular strips and on saponin-treated skinned smooth muscle cells was discussed in relation to the in vivo inhibition by this drug of smooth muscle myosin light chain kinase...
  25. ncbi Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine
    T W Ho
    Merck Research Laboratories, UG 4C 18, PO Box 1000, North Wales, PA 19454 1099, USA
    Neurology 70:1304-12. 2008
    ..To determine an effective and tolerable dose of a novel oral calcitonin gene-related peptide (CGRP) receptor antagonist, MK-0974, for the acute treatment of migraine...
  26. pmc Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294
    Yanqi Chang
    Department of Biochemistry, Emory University School of Medicine, 1510 Clifton Road, Atlanta, Georgia 30322, USA
    Nat Struct Mol Biol 16:312-7. 2009
    ..The inhibitor resembles the bound conformation of histone H3 Lys4 to Arg8, and is positioned in place by residues specific for G9a and GLP through specific interactions...
  27. ncbi Specific PAF antagonist WEB-2086 induces terminal differentiation of murine and human leukemia cells
    Cristina Cellai
    Department of Experimental Pathology and Oncology, University of Florence, 50134, Firenze, Italy
    FASEB J 16:733-5. 2002
    ....
  28. doi Efficacy and safety of besifloxacin ophthalmic suspension 0.6% compared with moxifloxacin ophthalmic solution 0.5% for treating bacterial conjunctivitis
    Marguerite B McDonald
    Corneal Specialist and Cataract and Refractive Surgery, Ophthalmic Consultants of Long Island, Lynbrook, NY, USA
    Ophthalmology 116:1615-1623.e1. 2009
    ..To compare the clinical and antimicrobial efficacy of besifloxacin ophthalmic suspension 0.6% with that of moxifloxacin ophthalmic solution 0.5% for the treatment of bacterial conjunctivitis...
  29. doi Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237
    Dominic A Sloane
    Yorkshire Cancer Research Institute for Cancer Studies, University of Sheffield, UK
    ACS Chem Biol 5:563-76. 2010
    ....
  30. doi Ocular pharmacokinetics of besifloxacin following topical administration to rabbits, monkeys, and humans
    Joel W Proksch
    Global Research and Development, Bausch and Lomb, 1400 N Goodman Street, Rochester, NY 14609, USA
    J Ocul Pharmacol Ther 25:335-44. 2009
    ..Studies were conducted to evaluate the ocular penetration and systemic exposure to besifloxacin, a fluoroquinolone antibiotic, following topical ocular administration to animals and humans...
  31. pmc Treatment of migraine attacks based on the interaction with the trigemino-cerebrovascular system
    Andrea Stephanie Link
    Biomedical Center Lund, Lund, Sweden
    J Headache Pain 9:5-12. 2008
    ..The purpose of this review is to give a short overview of the pathological background of migraine headache and to illustrate the mechanisms behind the actions of triptans and the promising CGRP receptor blockers...
  32. ncbi Studies of Abeta pharmacodynamics in the brain, cerebrospinal fluid, and plasma in young (plaque-free) Tg2576 mice using the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]az
    Thomas A Lanz
    Pfizer Inc, Eastern Point Road, MS 8220 4183, Groton, CT 06340, USA
    J Pharmacol Exp Ther 309:49-55. 2004
    ..Overall, Abeta in the CSF and not plasma seems to be a better biomarker of brain Abeta reduction; however, the time course of Abeta changes needs to be established in clinical studies...
  33. doi Excellent tolerability but relatively low initial clinical efficacy of telcagepant in migraine
    Peer Tfelt-Hansen
    Danish Headache Centre, Department of Neurology, University of Copenhagen, Glostrup Hospital, Glostrup, Denmark
    Headache 51:118-23. 2011
    ..The introduction of calcitonin gene-related peptide receptor antagonism in the acute treatment of migraine is a major step forward but so far mostly because of its specific mode of action and excellent tolerability...
  34. doi Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial
    Tony W Ho
    Merck Research Laboratories, North Wales, PA 19454 1099, USA
    Lancet 372:2115-23. 2008
    ..We aimed to assess the clinical profile of MK-0974 (telcagepant), an orally bioavailable antagonist of CGRP receptor...
  35. pmc Randomized, controlled trial of telcagepant for the acute treatment of migraine
    K M Connor
    Merck Research Laboratories, North Wales, PA 19454 1099, USA
    Neurology 73:970-7. 2009
    ..In this large phase 3 clinical trial, we sought to confirm the efficacy of telcagepant, the first orally bioavailable CGRP receptor antagonist...
  36. ncbi Securinine, a GABAA receptor antagonist, enhances macrophage clearance of phase II C. burnetii: comparison with TLR agonists
    Kirk Lubick
    Veterinary Molecular Biology, Montana State University, Bozeman, MT 59718, USA
    J Leukoc Biol 82:1062-9. 2007
    ..Securinine has minimal toxicity in vivo, suggesting it or structurally similar compounds may represent novel, therapeutic adjuvants, which increase resistance to intracellular pathogens...
  37. ncbi Bengamides revisited: new structures and antitumor studies
    Z Thale
    Department of Chemistry and Biochemistry, University of California, Santa Cruz, CA 95064, USA
    J Org Chem 66:1733-41. 2001
    ..The best activity was observed for the natural bengamides A (IC(50) = 1 nM) and O (IC(50) = 0.3 nM)...
  38. doi Securinine induces p73-dependent apoptosis preferentially in p53-deficient colon cancer cells
    Sonia Rana
    Invenio Therapeutics, Cleveland, Ohio, USA
    FASEB J 24:2126-34. 2010
    ..These studies reveal a novel approach to specifically target colon cancer cells lacking p53 as well as identify a novel clinically relevant pathway to selectively induce p73 in p53-null cells...
  39. ncbi Myosin light-chain kinase contributes to short-term endothelial cell cytoskeletal alteration induced by serum from burned rats
    Bo Chen
    Department of Pathophysiology, First Military Medical University, Guangzhou 510515, China
    Di Yi Jun Yi Da Xue Xue Bao 24:481-4, 488. 2004
    ....
  40. ncbi Myosin-II-dependent localization and dynamics of F-actin during cytokinesis
    Kausalya Murthy
    Department of Biology and Program in Molecular and Cellular Biology, University of Massachusetts, Amherst, 01003, USA
    Curr Biol 15:724-31. 2005
    ..The mechanism(s) that contribute to the spatially and temporally regulated assembly and disassembly of the CR at the cell equator are poorly understood...
  41. ncbi Effects of anti-myosin drugs on anaphase chromosome movement and cytokinesis in crane-fly primary spermatocytes
    R V Silverman-Gavrila
    Biology Department, York University, Toronto, Ontario, Canada
    Cell Motil Cytoskeleton 50:180-97. 2001
    ..H-7 had no effect. These results confirm that the effects of BDM are on myosin and indicate that the myosin used for cytokinesis is activated starting from autosomal anaphase and continuing throughout cytokinesis...
  42. doi Target specificity of the new fluoroquinolone besifloxacin in Streptococcus pneumoniae, Staphylococcus aureus and Escherichia coli
    Emmanuelle Cambau
    Université Paris12, Creteil, France
    J Antimicrob Chemother 63:443-50. 2009
    ..We investigated its mode of action and resistance in two major ocular pathogens, Streptococcus pneumoniae and Staphylococcus aureus, and in the reference species Escherichia coli...
  43. ncbi Safety, tolerability, and changes in amyloid beta concentrations after administration of a gamma-secretase inhibitor in volunteers
    Eric Siemers
    Lilly Research Laboratories, Indianapolis, Indiana 46285, USA
    Clin Neuropharmacol 28:126-32. 2005
    ..A dose-dependent reduction in plasma Abeta was demonstrated, and changes in plasma Abeta concentrations were temporally related to the pharmacokinetic characteristics of LY450139...
  44. ncbi Phase III efficacy and safety study of besifloxacin ophthalmic suspension 0.6% in the treatment of bacterial conjunctivitis
    Michael E Tepedino
    Cornerstone Eye Care, High Point, NC, USA
    Curr Med Res Opin 25:1159-69. 2009
    ..To compare the clinical and antimicrobial efficacy of besifloxacin ophthalmic suspension 0.6% with that of vehicle in the treatment of bacterial conjunctivitis...
  45. doi Besifloxacin ophthalmic suspension 0.6% in patients with bacterial conjunctivitis: A multicenter, prospective, randomized, double-masked, vehicle-controlled, 5-day efficacy and safety study
    Paul Karpecki
    Koffler Vision Group, Lexington, Kentucky 40509, USA
    Clin Ther 31:514-26. 2009
    ..6% is a new topical fluoroquinolone for the treatment of bacterial conjunctivitis. Besifloxacin has potent in vitro activity against a broad spectrum of ocular pathogens, including drug-resistant strains...
  46. ncbi Effects of a gamma-secretase inhibitor in a randomized study of patients with Alzheimer disease
    E R Siemers
    Eli Lilly and Company, Indianapolis, IN 46085, USA
    Neurology 66:602-4. 2006
    ..Abeta(1-40) in plasma decreased by 38.2%; in CSF, Abeta(1-40) decreased by 4.42 +/- 9.55% (p = not significant). Higher drug doses may result in additional decreases in plasma Abeta concentrations and a measurable decrease in CSF Abeta...
  47. ncbi Structure of human cytidine deaminase bound to a potent inhibitor
    Sang J Chung
    Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, USA
    J Med Chem 48:658-60. 2005
    ..The structure reveals that inhibitor 1 is able to establish a canonical pi/pi-interaction with a key active site residue, Phe 137...
  48. ncbi Nonclinical pharmacodynamics, pharmacokinetics, and safety of BOL-303224-A, a novel fluoroquinolone antimicrobial agent for topical ophthalmic use
    Keith W Ward
    Global Preclinical Development, Bausch and Lomb, Rochester, NY 14603, USA
    J Ocul Pharmacol Ther 23:243-56. 2007
    ..In summary, BOL-303224-A exhibits an encouraging nonclinical pharmacodynamic, pharmacokinetic, and safety profile that supports clinical development as a topical agent for the potential treatment of ophthalmic infections...
  49. ncbi Potent inhibitors for the deamination of cytosine arabinoside and 5-aza-2'-deoxycytidine by human cytidine deaminase
    J Laliberte
    Departement de Pharmacologie, Universite de Montreal, Quebec, Canada
    Cancer Chemother Pharmacol 30:7-11. 1992
    ..The inhibition constants for diazepinone riboside lay in the range of 5-15 nM, suggesting that this inhibitor could be an excellent candidate for use in combination chemotherapy with either ARA-C or 5-AZA-CdR in patients with leukemia...
  50. pmc A multigram chemical synthesis of the gamma-secretase inhibitor LY411575 and its diastereoisomers
    Abdul H Fauq
    Department of Neuroscience, Mayo Clinic Jacksonville, 4500 San Pablo Road, Jacksonville, FL 32224, USA
    Bioorg Med Chem Lett 17:6392-5. 2007
    ..Starting from the resolved aminolactams 5a and 5b, all four diastereomers were produced in enantiomerically pure form...
  51. ncbi Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl
    Daniel V Paone
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, West Point, Pennsylvania 19486, USA
    J Med Chem 50:5564-7. 2007
    ....
  52. ncbi Redundant mechanisms for anaphase chromosome movements: crane-fly spermatocyte spindles normally use actin filaments but also can function without them
    Lacramioara Fabian
    Biology Department, York University, Toronto, Ontario, Canada
    Protoplasma 225:169-84. 2005
    ....
  53. ncbi Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related pept
    Christopher A Salvatore
    Merck Research Laboratories, WP26A 2000, West Point, PA 19486, USA
    J Pharmacol Exp Ther 324:416-21. 2008
    ..In conclusion, MK-0974 is a highly potent, selective, and orally bioavailable CGRP receptor antagonist, which may be valuable in the acute treatment of migraine...
  54. ncbi Phagocytosis of apoptotic and necrotic thymocytes is inhibited by PAF-receptor antagonists and affects LPS-induced COX-2 expression in murine macrophages
    Soraya Imon de Oliveira
    Department of Immunology, Institute of Biomedical Sciences, University of Sao Paulo, Av Prof Lineu Prestes, 1730, 05508 900 Sao Paulo, Brazil
    Prostaglandins Other Lipid Mediat 80:62-73. 2006
    ..These findings indicate that apoptotic and necrotic cells share common ligands with PAF and oxLDL and suggest the involvement of PAF-like receptors in the enhanced clearance of these cells...
  55. ncbi Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY411,575) in the CRND8 mouse
    Lynn A Hyde
    Department of Neurobiology, Schering Plough Research Institute, Kenilworth, New Jersey 07033, USA
    J Pharmacol Exp Ther 319:1133-43. 2006
    ....
  56. pmc Phospholipase C and myosin light chain kinase inhibition define a common step in actin regulation during cytokinesis
    Raymond Wong
    Program in Developmental and Stem Cell Biology, The Hospital for Sick Children, TMDT Building, East Tower, Toronto, Ontario, Canada
    BMC Cell Biol 8:15. 2007
    ..However, the specificity of U73122 is unclear, as its active group closely resembles the non-specific alkylating agent N-ethylmaleimide (NEM). In addition, the pathway by which PIP2 regulates cytokinesis remains to be elucidated...
  57. ncbi The participation of the Na+-Ca2+ exchanger in primary cardiac myofibroblast migration, contraction, and proliferation
    Joshua E Raizman
    Institute of Cardiovascular Sciences, St Boniface General Hospital Research Centre and Department of Physiology, University of Manitoba, Winnipeg, Manitoba, Canada
    J Cell Physiol 213:540-51. 2007
    ..NCX1 may represent an important moiety in suppression of myofibroblast functions...
  58. doi Platelet-activating factor stimulates ovine foetal pulmonary vascular smooth muscle cell proliferation: role of nuclear factor-kappa B and cyclin-dependent kinases
    B O Ibe
    Division of Neonatology, Harbor UCLA Medical Center, Los Angeles Biomedical Institute, Harbor UCLA Medical Center, 1124 West Carson Street, Torrance, CA 90502, USA
    Cell Prolif 41:208-29. 2008
    ..We investigated involvement of PAF and PAF receptors in PVSMC proliferation...
  59. ncbi In vivo phosphorylation of regulatory light chain of myosin II in sea urchin eggs and its role in controlling myosin localization and function during cytokinesis
    Ryota Uehara
    Department of Biology, School of Arts and Sciences, University of Tokyo, 3 8 1 Komaba, Tokyo 153 8902, Japan
    Cell Motil Cytoskeleton 65:100-15. 2008
    ..These results suggested that RLC mono-phosphorylation by more than two RLC kinases play a main role in regulation and localization of myosin in the dividing sea urchin eggs...
  60. ncbi Cellular mechanisms of mainstream cigarette smoke-induced lung epithelial tight junction permeability changes in vitro
    Dorian S Olivera
    Program in Toxicology, College of Pharmacy, University of New Mexico Health Sciences Center, Albuquerque, New Mexico, USA
    Inhal Toxicol 19:13-22. 2007
    ..Additionally, our results indicate that activation of PTK and ROCK and inactivation of MLCK contribute to the increased airway permeability caused by mainstream cigarette smoke...
  61. doi 9-cyano-1-azapaullone (cazpaullone), a glycogen synthase kinase-3 (GSK-3) inhibitor activating pancreatic beta cell protection and replication
    Hendrik Stukenbrock
    Institut fur Pharmazeutische Chemie, Technische Universitat Braunschweig, Beethovenstrasse 55, Braunschweig, Germany
    J Med Chem 51:2196-207. 2008
    ..These features distinguish cazpaullone as a unique starting point for the development of beta cell regenerative agents which might be useful in the treatment of diabetes...
  62. pmc Dual role for myosin II in GLUT4-mediated glucose uptake in 3T3-L1 adipocytes
    F Kent Fulcher
    Department of Biology, University of North Carolina at Greensboro, Greensboro, North Carolina 27402, USA
    Exp Cell Res 314:3264-74. 2008
    ..Collectively, our results are the first to reveal that myosin IIA plays a critical role in mediating insulin-stimulated glucose uptake in 3T3-LI adipocytes, via both GLUT4 vesicle fusion at the plasma membrane and GLUT4 activity...
  63. ncbi Inhibition of the myosin light chain kinase prevents hypoxia-induced blood-brain barrier disruption
    Christoph R W Kuhlmann
    Institute of Physiology and Pathophysiology, Johannes Gutenberg University of Mainz, Mainz, Germany
    J Neurochem 102:501-7. 2007
    ..Furthermore, ML-7 and apocynin blocked hypoxia-dependent phosphorylation of MLC. Our data demonstrate that hypoxia causes a breakdown of the BBB in vitro and in vivo involving ROS and the contractile machinery...
  64. ncbi Myosin light chain kinase regulates synaptic plasticity and fear learning in the lateral amygdala
    R Lamprecht
    W M Keck Foundation Laboratory for Neurobiology, Center for Neural Science, New York University, 4 Washington Place, Room 809, New York, NY 10003, USA
    Neuroscience 139:821-9. 2006
    ..Impairment of this mechanism could contribute to pathological fear learning...
  65. ncbi Inhibiting myosin light chain kinase retards the growth of mammary and prostate cancer cells
    Lian Zhi Gu
    Department of Physiology and Biophysics, University of Illinois at Chicago, College of Medicine, 835 South Wolcott Ave, Chicago, IL 60612 7342, USA
    Eur J Cancer 42:948-57. 2006
    ..These results provide evidence for the efficacy of ML-7 as an adjuvant to etoposide in these models and warrants further development...
  66. ncbi Implication of phosphorylation of the myosin II regulatory light chain in insulin-stimulated GLUT4 translocation in 3T3-F442A adipocytes
    Young Ok Choi
    Department of Physiology, University of Ulsan College of Medicine, Seoul 138 736, Korea
    Exp Mol Med 38:180-9. 2006
    ..Our studies suggest that MLCK may be a regulatory target of Ca(2+)/calmodulin and may play an important role in insulin-stimulated glucose transport in adipocytes...
  67. ncbi Laminin-311 (Laminin-6) fiber assembly by type I-like alveolar cells
    Phillip J DeBiase
    Division of Pulmonary Medicine, Department of Cell and Molecular Biology, Feinberg School of Medicine, Northwestern University, Tarry 8 715, 303 E Chicago Avenue, Chicago, IL 60611, USA
    J Histochem Cytochem 54:665-72. 2006
    ..In summary, our data indicate that assembly of laminin-311 fibers by lung epithelial cells is integrin and actin cytoskeleton dependent, and that these fibers are characteristic of type I alveolar cells...
  68. ncbi [Effect of actomyosin contractility on focal contacts of myofibroblasts and structure of stress fibers]
    V B Dugina
    A N Belozersky Institute of Physico Chemical Biology, Moscow State University, Russia
    Tsitologiia 44:48-55. 2002
    ..Thus, actin-myosin contractility controls the structure of "supermature" focal contacts of myofibroblasts and alpha-SMA expression in stress fibers...
  69. ncbi An MLCK-dependent window in late G1 controls S phase entry of proliferating rodent hepatocytes via ERK-p70S6K pathway
    Anne Bessard
    INSERM U522, Unité de Recherches Hépatologiques IFR 140 Université de Rennes1, Rennes, France
    Hepatology 44:152-63. 2006
    ....
  70. ncbi Theoretical and experimental investigation of calcium-contraction coupling in airway smooth muscle
    Prisca Mbikou
    Universite Bordeaux 2, Laboratoire de Physiologie Cellulaire Respiratoire, Bordeaux, F 33076 France Inserm, E356, Bordeaux, F 33076 France
    Cell Biochem Biophys 46:233-52. 2006
    ..The long-time phase of the contraction, associated with a second increase in MLC phosphorylation, may be explained, at least partially, by MLC phosphatase (MLCP) inhibition, possibly via PKC inhibition...
  71. pmc Calcium absorption by Cav1.3 induces terminal web myosin II phosphorylation and apical GLUT2 insertion in rat intestine
    Oliver J Mace
    Department of Biology, The University of York, York YO10 5YW, UK
    J Physiol 580:605-16. 2007
    ....
  72. ncbi Organized migration of epithelial cells requires control of adhesion and protrusion through Rho kinase effectors
    Ann M Hopkins
    Department of Pathology and Laboratory Medicine, Emory University, Atlanta, Georgia 30322, USA
    Am J Physiol Gastrointest Liver Physiol 292:G806-17. 2007
    ....
  73. ncbi Interaction of non-adherent suspended neutrophils to complement opsonized pathogens: a new assay using optical traps
    Tomoko Suzuki
    Department of Geriatric and Respiratory Medicine, Tohoku University School of Medicine, Sendai 980 8574, Japan
    Cell Res 16:887-94. 2006
    ....
  74. ncbi Mechanisms of endothelin-1-induced contraction in pulmonary arteries from chronically hypoxic rats
    Letitia Weigand
    Division of Pulmonary and Critical Care Medicine, Department of Medicine, Johns Hopkins Univ, 5501 Hopkins Bayview Circle, JHAAC 4B 82B, Baltimore, MD 21224, USA
    Am J Physiol Lung Cell Mol Physiol 290:L284-90. 2006
    ..We conclude that the component of ET-1-induced contraction that occurs without a change in [Ca2+]i in IPA from CH rats requires activation of Rho kinase and TKs, but not PKC...
  75. pmc Slipping or gripping? Fluorescent speckle microscopy in fish keratocytes reveals two different mechanisms for generating a retrograde flow of actin
    Carlos Jurado
    Department of Molecular and Cell Biology, University of Connecticut, Storrs, CT 06269, USA
    Mol Biol Cell 16:507-18. 2005
    ..The other involves slippage between adhesions and the substratum, which increases traction force production. We conclude that a biphasic relationship exists between retrograde actin flow and adhesiveness in moving keratocytes...
  76. ncbi Modulation of acto-myosin contractility in skeletal muscle myoblasts uncouples growth arrest from differentiation
    Jyotsna Dhawan
    Center for Cellular and Molecular Biology, Uppal Road, Hyderabad, 500 007, India
    J Cell Sci 117:3735-48. 2004
    ..We suggest that in myoblasts, the Rho pathway and regulation of acto-myosin contractility may define a control point for conditional uncoupling of differentiation and the cell cycle...
  77. ncbi Parallel liquid synthesis of N,N'-Disubstituted 3-amino azepin-2-ones as potent and specific farnesyl transferase inhibitors
    Thierry Le Diguarher
    Department of Medicinal Chemistry, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Bioorg Med Chem 11:3193-204. 2003
    ..The activities of the selected compounds were validated in vivo, and compounds 41a and 44a presented significant antitumour activity...
  78. ncbi Cyclic AMP-dependent protein kinase A plays a role in the directed migration of human keratinocytes in a DC electric field
    C E Pullar
    Department of Dermatology, University of California, Davis, CA 95616, USA
    Cell Motil Cytoskeleton 50:207-17. 2001
    ..The inhibitor studies described in this paper implicate a role for PKA in the regulation of the directional migratory response to applied electric fields, galvanotaxis...
  79. ncbi Involvement of platelet activating factor in immediate heart response to lipopolysaccharide
    A Jakubowski
    Department of Experimental Pharmacology, Jagiellonian University Medical College, Cracow, Poland
    J Physiol Pharmacol 55:409-21. 2004
    ..Accordingly, PAF may constitute the mediator that links acute and delayed phases of LPS-induced cardiovascular response...
  80. ncbi Rapid actin transport during cell protrusion
    Daniel Zicha
    Light Microscopy, Cancer Research UK, Lincoln s Inn Fields Laboratories, London WC2A 3PX, UK
    Science 300:142-5. 2003
    ..Monte Carlo modeling confirmed that this flow cannot be explained by diffusion and may involve active transport...
  81. ncbi Proteinase-activated receptor-2-induced colonic inflammation in mice: possible involvement of afferent neurons, nitric oxide, and paracellular permeability
    Nicolas Cenac
    Neuro Gastroenterology and Nutrition Unit, Institut National de la Recherche Agronomique, Toulouse, France
    J Immunol 170:4296-300. 2003
    ..Nevertheless, the inflammation process is not a consequence of increased permeability which results at least in part from the activation of myosin L chain kinase...
  82. ncbi Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors
    Thierry Le Diguarher
    Department of Medicinal Chemistry, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, France
    Bioorg Med Chem Lett 14:767-71. 2004
    ..A structure-activity study was performed by synthesis on N,N'-disubstitution of 3-aminobenzo[c] and [d]azepin-2-one 2 and 3 to afford potent and specific farnesyl transferase inhibitors with low nM enzymatic and cellular activities...
  83. ncbi The role of rho and rho-dependent kinase in serotonin-induced contraction observed in bovine middle cerebral artery
    Yasumasa Nishikawa
    Department of Physiology, School of Medicine, Iwate Medical University, Morioka 020 8505, Japan
    Tohoku J Exp Med 201:239-49. 2003
    ....
  84. ncbi Myofibrillogenesis in the first cardiomyocytes formed from isolated quail precardiac mesoderm
    Aiping Du
    Department of Cell and Developmental Biology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6058, USA
    Dev Biol 257:382-94. 2003
    ....
  85. ncbi Role of the actin cytoskeleton in regulating endothelial permeability in venules
    J Edward Valeski
    Department of Physiology, College of Medicine, University of Arizona, Tucson, AZ 85724 5051, USA
    Microcirculation 10:411-20. 2003
    ..This study was performed to determine the effect of myosin light chain kinase (MLCK) inhibition on histamine- and thrombin-induced venular permeability in the rat mesentery, coincidental with actin cytoskeleton changes...
  86. ncbi Degranulation in RBL-2H3 cells: regulation by calmodulin pathway
    Masayuki Funaba
    Laboratory of Nutrition, Azabu University School of Veterinary Medicine, 1 17 71 Fuchinobe, Sagamihara 229 8501, Japan
    Cell Biol Int 27:879-85. 2003
    ....
  87. ncbi Functional diversity between Rho-kinase- and MLCK-mediated cytoskeletal actions in a myofibroblast-like hepatic stellate cell line
    Mikio Yanase
    Department of Gastroenterology, Faculty of Medicine, University of Tokyo, 7 3 1 Hongo, Bunkyo ku, 113 0033, Tokyo, Japan
    Biochem Biophys Res Commun 305:223-8. 2003
    ..These findings suggest that the actomyosin-based cytoskeletal actions can be functionally diverse depending on the Rho-kinase-mediated pathway and the MLCK-mediated pathway...
  88. ncbi Dependence of metastatic cancer cell invasion on MLCK-catalyzed phosphorylation of myosin regulatory light chain
    R Tohtong
    Department of Biochemistry, Faculty of Science, Mahidol University, Phya Thai, Bangkok, Thailand
    Prostate Cancer Prostatic Dis 6:212-6. 2003
    ....
  89. ncbi Oxidized low-density lipoprotein downregulates endothelial basic fibroblast growth factor through a pertussis toxin-sensitive G-protein pathway: mediator role of platelet-activating factor-like phospholipids
    P Y Chang
    Department of Medicine, Baylor College of Medicine, Houston, TX 77030, USA
    Circulation 104:588-93. 2001
    ..CONCLUSIONS: OxLDL suppresses endothelial bFGF expression and DNA synthesis through a PTX-sensitive heterotrimeric G-protein pathway involving mediator phospholipids similar, but not identical, to PAF...
  90. ncbi Participation of prostaglandin E2 and platelet-activating factor in thapsigargin-induced production of interleukin-6
    Gaku Ichinowatari
    Laboratory of Pathophysiological Biochemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba Aramaki, Aoba ku, Sendai, Miyagi 980 8578, Japan
    Eur J Pharmacol 434:187-96. 2002
    ..These findings suggested that the concurrently produced prostaglandin E2 and intracellular PAF participate in the thapsigargin-induced increase in the interleukin-6 mRNA level and interleukin-6 production by rat peritoneal macrophages...
  91. ncbi ML-7 inhibits exocytosis of superoxide-producing intracellular compartments in human neutrophils stimulated with phorbol myristate acetate in a myosin light chain kinase-independent manner
    Keita Odani
    Department of Radiology, Kochi Medical School, Nankoku, 783 5305 Kochi, Japan
    Histochem Cell Biol 119:363-70. 2003
    ....
  92. ncbi Differential regulation of human lung epithelial and endothelial barrier function by thrombin
    Kamon Kawkitinarong
    Division of Pulmonary and Critical Care Medicine, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA
    Am J Respir Cell Mol Biol 31:517-27. 2004
    ....
  93. ncbi Role of platelet-activating factor in phosphatidylcholine secretion in primary cultures of rat type II pneumocytes
    E Benito
    Department of Biochemistry and Molecular Biology, Faculty of Chemistry, Universidad Complutense, Madrid, Spain
    Prostaglandins Other Lipid Mediat 67:197-208. 2002
    ..This involvement was further supported by the use of inhibitors of protein kinases and by the stimulation of cAMP production in type II pneumocytes incubated with PAF...
  94. ncbi Preventive effect of platelet-activating factor antagonist, Y-24180, against cyclosporine-induced acute nephrotoxicity
    A Kawaguchi
    Department of Clinical Pharmacology, Jichi Medical School, Kawachi-gun, Tochigi, Japan
    Life Sci 68:1181-90. 2001
    ..The present findings also support the idea that Et contributes to the CsA-induced acute nephrotoxicity...
  95. ncbi Effects of ML-7 and Y-27632 on carbachol- and endothelin-1-induced contraction of bovine trabecular meshwork
    Rita Rosenthal
    Augenklinik und Augenpoliklinik, Charite, Universitatsmedizin Berlin, Campus Benjamin Franklin, Berlin, Germany
    Exp Eye Res 80:837-45. 2005
    ..According to our concept of aqueous humor outflow regulation, trabecular meshwork relaxing substances appear to be ideal antiglaucomatous drugs, leading to increased outflow facility...
  96. ncbi LPS-induced lung inflammation is linked to increased epithelial permeability: role of MLCK
    H Eutamene
    Purpan College of Agriculture, Toulouse, France
    Eur Respir J 25:789-96. 2005
    ....
  97. pmc Pharmacological analysis of neutrophil chemotactic factor production by leucocytes and roles of PAF in allergic inflammation in rats
    M Watanabe
    Department of Biochemistry, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan
    Br J Pharmacol 111:123-30. 1994
    ..9. The mechanism of action of PAF antagonists on neutrophil infiltration into the inflammatory locus is discussed...
  98. ncbi Phosphoinositide-3-kinase-independent contractile activities associated with Fcgamma-receptor-mediated phagocytosis and macropinocytosis in macrophages
    Nobukazu Araki
    Department of Histology and Cell Biology, Kagawa Medical University, Miki, Kagawa 761 0793, Japan
    J Cell Sci 116:247-57. 2003
    ..These PI3K-independent myosin-II-based contractile activities that squeeze phagocytic cups and curve ruffles therefore represent a third component activity of the actin cytoskeleton during phagocytosis and macropinocytosis...
  99. ncbi Platelet-activating factor antagonists decrease the inflammatory nociceptive response in rats
    Lisa A Teather
    Massachusetts Institute of Technology, Department of Brain and Cognitive Sciences, 45 Carleton Street, E25 604, Cambridge, MA 02139, USA
    Psychopharmacology (Berl) 163:430-3. 2002
    ..Evidence suggests that PAF exerts cellular actions through a plasma membrane receptor as well as via intracellular (microsomal) PAF binding sites...
  100. ncbi Myosin light chain phosphorylation in neutrophil-stimulated coronary microvascular leakage
    Sarah Y Yuan
    Departments of Surgery and Medical Physiology, Cardiovascular Research Institute, Texas A and M University Health Science Center, Temple, Texas, USA yuan tamu edu
    Circ Res 90:1214-21. 2002
    ..Taken together, the results suggest that endothelial MLCK activation and MLC phosphorylation play an important role in mediating endothelial barrier dysfunction during neutrophil activation...
  101. ncbi PAF- and bradykinin-induced hyperpermeability of rat venules is independent of actin-myosin contraction
    R H Adamson
    Departmentof Human Physiology, School of Medicine, University of California Davis, Davis, CA 95616, USA
    Am J Physiol Heart Circ Physiol 285:H406-17. 2003
    ..The results are consistent with paracellular gap formation by local release of endothelial-endothelial cell adhesion structures in the absence of contraction by the actin-myosin network...

Research Grants166 found, 100 shown here

  1. New Methods for Nitrogen Heterocycle Synthesis
    Sherry Chemler; Fiscal Year: 2009
    ..hexahydro-1 H-benz[f]indoles, isoquinolines, pyrrolidines, vicinal diamines and potentially aporphines and azepines demonstrate a broad range of biological activity such as 1) dopamine antagonists, important in mood regulation ..
  2. New Methods for Nitrogen Heterocycle Synthesis
    Sherry R Chemler; Fiscal Year: 2010
    ..hexahydro-1 H-benz[f]indoles, isoquinolines, pyrrolidines, vicinal diamines and potentially aporphines and azepines demonstrate a broad range of biological activity such as 1) dopamine antagonists, important in mood regulation ..
  3. New Methods for Nitrogen Heterocycle Synthesis
    Sherry Chemler; Fiscal Year: 2007
    ..hexahydro-1 H-benz[f]indoles, isoquinolines, pyrrolidines, vicinal diamines and potentially aporphines and azepines demonstrate a broad range of biological activity such as 1) dopamine antagonists, important in mood regulation ..
  4. New Methods for Nitrogen Heterocycle Synthesis
    Sherry Chemler; Fiscal Year: 2009
    ..hexahydro-1 H-benz[f]indoles, isoquinolines, pyrrolidines, vicinal diamines and potentially aporphines and azepines demonstrate a broad range of biological activity such as 1) dopamine antagonists, important in mood regulation ..
  5. N-Heterocycles from Azides through Rhodium-Catalyzed Nitrenoid Transfer
    TOM GREGORY DRIVER; Fiscal Year: 2010
    ..or o-anthranil decomposition to enable the rapid synthesis of heteroaromatic carbazoles, indoles, functionalized azepines, and aziridines...
  6. N-Heterocycles from Azides through Rhodium-Catalyzed Nitrenoid Transfer
    TOM GREGORY DRIVER; Fiscal Year: 2010
    ..or o-anthranil decomposition to enable the rapid synthesis of heteroaromatic carbazoles, indoles, functionalized azepines, and aziridines...
  7. N-Heterocycles from Azides through Rhodium-Catalyzed Nitrenoid Transfer
    TOM DRIVER; Fiscal Year: 2009
    ..or o-anthranil decomposition to enable the rapid synthesis of heteroaromatic carbazoles, indoles, functionalized azepines, and aziridines...
  8. Translational Center on Serotonin and Stimulant Addiction
    KATHRYN CUNNINGHAM; Fiscal Year: 2007
    ..Through clinical and laboratory methods, we will test the ability of existing medications and the potential for newly designed drugs to enhance abstinence in stimulant-dependent individuals. ..
  9. NEUROBEHAVIORAL PHARMACOLOGY OF STIMULANTS
    KATHRYN CUNNINGHAM; Fiscal Year: 1999
    ..DA interactions and ultimately may reveal how these interactions are altered by cocaine, perhaps suggesting new strategies for pharmacological intervention in abusers. ..
  10. NEUROBEHAVIORAL PHARMACOLOGY OF STIMULANTS
    KATHRYN CUNNINGHAM; Fiscal Year: 1992
    ..This knowledge is essential to the development of novel approaches to stimulant antagonism and pharmacological treatment strategies for abusers...
  11. NEUROBEHAVIORAL PHARMACOLOGY OF STIMULANTS
    KATHRYN CUNNINGHAM; Fiscal Year: 2004
    ..As a consequence, new insight into the potential therapeutic strategies for cocaine dependence and a number of psychiatric disorders dependent upon normal 5-HT function will be gained. ..
  12. NEUROPSYCHOPHARMACOLOGY MDMA--MONOAMINERGIC MECHANISMS
    KATHRYN CUNNINGHAM; Fiscal Year: 2005
    ..abstract_text> ..
  13. 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. ..
  14. 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. ..
  15. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 2000
    ..These macrocyclic antitumor agents exhibit important antibiotic effects against resistant organisms. New strategies for macrocyclization are introduced. Acyl nitrene insertions for preparation of lankacyclinol are described. ..
  16. INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 2006
    ..The selective synthesis of contiguous stereotriads will advance basic methodology for asymmetric conjugate additions. ..
  17. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 2004
    ..The intramolecular (4+2) cycloadditions of nitroalkene precursors will provide facile construction of trans-decalins. . ..
  18. INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 2002
    ..A particularly rich spectrum of biological activity, including important anti-tumor activity, is exhibited throughout this class of novel medium-ring metabolites. ..
  19. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 1993
    ..Secondly, studies of the Michael reaction will be explored for ring annulation. Finally, new methodology for carbanions in nitrogen-containing, chiral synthons will be detailed...
  20. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 1992
    ..They also show strong atimicrobial activities, principally against Gram-positive bacteria, including some strains of clinically resistant isolates...
  21. INVESTIGATIONS OF INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 1993
    ..Finally, we have outlined explorations of fundamental heterocyclic oxazole chemistry as a precursor to our plans for total synthesis of the ulapualides, extraordinarily potent and unique antitumor marine natural products...
  22. NEW APPROACHES TO ANTIFOLATE CHEMOTHERAPY
    Andre Rosowsky; Fiscal Year: 1993
    ....
  23. ANGIOTENSIN-VASOPRESSIN INTERACTIONS DURING ADAPTATION TO HYPOOSMOLALITY
    Joseph G Verbalis; Fiscal Year: 2010
    ....
  24. The Genetic Basis of Neuroblastoma Tumorigenesis
    John Maris; Fiscal Year: 2009
    ..These insights will lead to new molecular diagnostic assays and/or new treatments for this frequently devastating malignancy of young children. ..
  25. CGRP Regulation of iNOS and MAP Kinases/Phosphatases in Trigeminal Ganglia Glia
    Paul Durham; Fiscal Year: 2007
    ....
  26. Azinomycins - Total Synthesis and Mechanism of Action
    Robert Coleman; Fiscal Year: 2007
    ..abstract_text> ..
  27. ISOLATION OF THE NEUROBLASTOMA PREDISPOSITION GENE
    John Maris; Fiscal Year: 2006
    ..Ultimately, these experiments should lead to the identification of a common pathway to neuroblastoma tumorigenesis that will be an outstanding target for rationally designed therapeutics. ..