azepines

Summary

Summary: Seven membered heterocyclic rings containing a NITROGEN atom.

Top Publications

  1. ncbi 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
  2. ncbi 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
  3. ncbi 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
  4. ncbi 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
  5. 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
  6. ncbi 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
  7. ncbi 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
  8. ncbi 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
  9. ncbi 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
  10. ncbi 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

Research Grants

  1. New Methods for Nitrogen Heterocycle Synthesis
    Sherry Chemler; Fiscal Year: 2009
  2. New Methods for Nitrogen Heterocycle Synthesis
    Sherry R Chemler; Fiscal Year: 2010
  3. New Methods for Nitrogen Heterocycle Synthesis
    Sherry Chemler; Fiscal Year: 2007
  4. New Methods for Nitrogen Heterocycle Synthesis
    Sherry Chemler; Fiscal Year: 2009
  5. N-Heterocycles from Azides through Rhodium-Catalyzed Nitrenoid Transfer
    TOM GREGORY DRIVER; Fiscal Year: 2010
  6. N-Heterocycles from Azides through Rhodium-Catalyzed Nitrenoid Transfer
    TOM DRIVER; Fiscal Year: 2009
  7. N-Heterocycles from Azides through Rhodium-Catalyzed Nitrenoid Transfer
    TOM GREGORY DRIVER; Fiscal Year: 2010
  8. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 1992
  9. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 1993
  10. INVESTIGATIONS OF INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 1993

Detail Information

Publications182 found, 100 shown here

  1. ncbi 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
    ....
  2. ncbi 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...
  3. ncbi 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...
  4. ncbi 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...
  5. 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...
  6. ncbi 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...
  7. ncbi 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...
  8. ncbi 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...
  9. ncbi 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...
  10. ncbi 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...
  11. 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...
  12. 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...
  13. 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
    ..CONCLUSIONS: These results demonstrate that the majority of actin in the CR is highly dynamic and establish novel roles for myosin II in the retention and dynamic turnover of actin in the CR...
  14. 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, , Av. Prof. Lineu Prestes, 1730, , 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...
  15. 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...
  16. 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
    ....
  17. 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...
  18. 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...
  19. 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
    ....
  20. ncbi 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...
  21. 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...
  22. 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...
  23. ncbi 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...
  24. 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...
  25. ncbi 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...
  26. 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
    ....
  27. 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...
  28. ncbi 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...
  29. ncbi 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...
  30. 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...
  31. 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...
  32. 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
    ....
  33. 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...
  34. ncbi Platelet-activating factor induces cardioprotection in isolated rat heart akin to ischemic preconditioning: role of phosphoinositide 3-kinase and protein kinase C activation
    Claudia Penna
    Dipartimento di Scienze Cliniche e Biologiche, ASO S. Luigi, Orbassano, Italy
    Am J Physiol Heart Circ Physiol 288:H2512-20. 2005
    ..Moreover, the study suggests that endogenous release of PAF, induced by brief periods of ischemia and reperfusion, may participate to the triggering of the IP of the heart...
  35. ncbi Acute stress-induced hypersensitivity to colonic distension depends upon increase in paracellular permeability: role of myosin light chain kinase
    Afifa Ait-Belgnaoui
    Neuro-Gastroenterology and Nutrition Unit, INRA, 180, chemin de Tournefeuille BP 03, 31931 Toulouse Cedex 9, France
    Pain 113:141-7. 2005
    ..The increase of colonic permeability induced by PRS results from epithelial cell cytoskeleton contraction through myosin light chain kinase activation and this increase is responsible for stress-induced rectal hypersensitivity...
  36. ncbi Key role of myosin light chain (MLC) kinase-mediated MLC2a phosphorylation in the alpha 1-adrenergic positive inotropic effect in human atrium
    Michael Grimm
    Institute of Experimental and Clinical Pharmacology, University Hospital Eppendorf, Martinistrasse 52, 20246 Hamburg, Germany
    Cardiovasc Res 65:211-20. 2005
    ..This study investigated alpha(1)-adrenergic contractile effects and the role of MLC kinase (MLCK)-dependent phosphorylation of MLC2 in human atrial muscle strips...
  37. ncbi 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...
  38. 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...
  39. 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...
  40. 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...
  41. ncbi 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...
  42. ncbi 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...
  43. ncbi 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...
  44. 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...
  45. ncbi 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...
  46. ncbi Theoretical and experimental investigation of calcium-contraction coupling in airway smooth muscle
    Prisca Mbikou
    , 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...
  47. ncbi 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
    ....
  48. 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
    ....
  49. 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...
  50. 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
    ....
  51. 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...
  52. 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
    ....
  53. 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...
  54. ncbi Endothelial cell myosin light chain kinase (MLCK) regulates TNFalpha-induced NFkappaB activity
    Raj Wadgaonkar
    Division of Pulmonary and Critical Care Medicine, Department of Medicine, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21224, USA
    J Cell Biochem 94:351-64. 2005
    ..Together, these novel observations indicate that TNFalpha-induced cytoskeletal rearrangement driven by MLCK activity is necessary for TNFalpha-dependent NFkappaB activation and amplification of pro-survival signals...
  55. 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...
  56. 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...
  57. 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
    ....
  58. 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...
  59. ncbi Mechanisms underlying pervanadate-induced contraction of rat cremaster muscle arterioles
    Timothy V Murphy
    Microvascular Biology Group, School of Medical Sciences, RMIT University, PO Box 71, 3083 Bundoora, Victoria, Australia
    Eur J Pharmacol 442:107-14. 2002
    ..These observations suggest that pervanadate-induced contraction of smooth muscle in the cremaster arteriole involves Ca2+/calmodulin-dependent myosin phosphorylation and possibly sensitization of the contractile apparatus to Ca2+...
  60. 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...
  61. 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
    ....
  62. 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...
  63. 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...
  64. 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...
  65. 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...
  66. 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...
  67. ncbi Role of rho-kinase activity in angiotensin II-induced contraction of rabbit clitoral cavernosum smooth muscle
    J K Park
    Department of Urology, Chonbuk National University Medical School, Chonju, South Korea
    Int J Impot Res 14:472-7. 2002
    ..RhoA/Rho-kinase pathway acts in the ANG II-induced contraction independently of the NO pathway...
  68. ncbi 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...
  69. ncbi Effect of SNI-2011 on amylase secretion from parotid tissue in rats and in neuronal nitric oxide synthase knockout mice
    Zhenfang Yuan
    Department of Pharmacology, Tokushima University School of Dentistry, Kuramoto-cho, Tokushima City, Japan
    Eur J Pharmacol 464:197-206. 2003
    ..These results indicate the implication of the activation of Ca(2+)- and calmodulin-dependent enzymes and NOS-PKG signaling pathway in SNI-2011-induced amylase secretion from parotid acinar cells...
  70. 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...
  71. 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...
  72. 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...
  73. ncbi Inhibition of contractile activation reduces reoxygenation-induced endothelial gap formation
    C Schafer
    Institute of Physiology, Justus Liebig University Giessen, Germany
    Cardiovasc Res 58:149-55. 2003
    ..4) and reperfusion (30 min reoxygenation, pH(o) 7.4)...
  74. 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
    ....
  75. 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...
  76. 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
    ....
  77. 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...
  78. 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...
  79. ncbi The renal effects of Bothrops jararacussu venom and the role of PLA(2) and PAF blockers
    A Havt
    Department of Physiology and Pharmacology, Faculty of Medicine, Federal University of Ceara, Rua Cel. Nunes de Melo 1127, 60430-270 Fortaleza, CE, Brazil
    Toxicon 39:1841-6. 2001
    ..Dexamethasone did not block the renal effects maybe because of the concentration used in this work or maybe the renal effects are promoted by the myotoxin, which does not have PLA(2) activity...
  80. ncbi Myosin light chain kinase inhibitors can block invasion and adhesion of human pancreatic cancer cell lines
    Kenzo Kaneko
    Department of Gastroenterology, Division of Internal Medicine, Tohoku University Graduate School of Medicine, Sendai, Miyaga, Japan
    Pancreas 24:34-41. 2002
    ..A cytoskeletal component indispensable for these processes is myosin II, the cytoplasmic analogue of smooth and skeletal muscle myosin...
  81. 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...
  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 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...
  85. 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...
  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 Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel
    E J Warawa
    Department of Medicinal Chemistry, AstraZeneca Pharmaceuticals LP, Wilmington, Delaware 19850 5437, USA
    J Med Chem 44:372-89. 2001
    ..Thus, aromatic and N-substituted analogues of 6-(piperazin-1-yl)-11H-dibenz[b,e]azepines and 11-(piperazin-1-yl)dibenzo[b,f][1,4]thiazepines and -oxazepines were prepared and evaluated...
  88. ncbi Construction of indole- and isoquinoline-fused nitrogen-containing heterocycles through copper-catalyzed multi-component reaction
    Yusuke Ohta
    Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshidashimoadachi cho, Sakyo ku, Kyoto, Japan
    Yakugaku Zasshi 130:925-36. 2010
    ..the synthesis of 4-methylene-2,3,4,9-tetrahyro-1H-pyrido[3,4-b]indoles and 5,6,7,8-tetrahydrobenzo[e]indolo[2,3-c]azepines via palladium-catalyzed C-H functionalization at the 3-position of indole...
  89. ncbi Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase
    Andre Rosowsky
    Dana Farber Cancer Institute and Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115, USA
    J Med Chem 47:2475-85. 2004
    Six previously undescribed N-(2,4-diaminopteridin-6-yl)methyldibenz[b,f]azepines with water-solubilizing O-carboxyalkyloxy or O-carboxybenzyloxy side chains at the 2'-position were synthesized and compared with trimethoprim (TMP) and ..
  90. ncbi Analogues of morphanthridine and the tear gas dibenz[b,f][1,4]oxazepine (CR) as extremely potent activators of the human transient receptor potential ankyrin 1 (TRPA1) channel
    Harrie J M Gijsen
    Medicinal Chemistry Department, Johnson and Johnson Pharmaceutical Research and Development, Turnhoutseweg 30, 2340 Beerse, Belgium
    J Med Chem 53:7011-20. 2010
    ..In this paper, the discovery of 11H-dibenz[b,e]azepines (morphanthridines) and dibenz[b,f][1,4]oxazepines is described as extremely potent agonists of the TRPA1 receptor...
  91. ncbi Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain
    David C M Chan
    Dana Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115, USA
    J Med Chem 48:4420-31. 2005
    ..Three N-(2,4-diaminopteridin-6-yl)methyl)-2'-(omega-carboxy-1-alkynyl)dibenz[b,f]azepines (19-21) were also synthesized and tested...
  92. ncbi Diversity-oriented synthesis of azaspirocycles
    Peter Wipf
    Department of Chemistry, Center for Chemical Methodologies and Library Development, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, USA
    Org Lett 6:3009-12. 2004
    ..The resulting functionalized pyrrolidines, piperidines, and azepines are scaffolds of considerable relevance for chemistry-driven drug discovery.
  93. ncbi N-Arylated 3,5-Dihydro-4H-dinaphtho[2,1-c:1',2'-e]azepines: Axially Chiral Donors with High Helical Twisting Powers for Nonplanar Push-Pull Chromophores
    Brian B Frank
    , , HCI, , Fax 41 44 632 1109
    Chemistry 15:9005-16. 2009
    Axially chiral, N-arylated 3,5-dihydro-4H-dinaphtho[2,1-c:1',2'-e]azepines have been prepared by short synthetic protocols from enantiopure 1,1'-bi(2,2'-naphthol) (BINOL) and anilines...
  94. ncbi 1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties
    Alec D Lebsack
    Johnson and Johnson Pharmaceutical Research and Development LLC, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:7142-6. 2010
    ..reported lead compound 1, a series of 1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines were synthesized and evaluated for improved physiochemical and pharmacokinetic properties while maintaining TRPV1 ..
  95. ncbi Targeting of human Tmolt4 leukemic type II IMP dehydrogenase by cyclic imide related derivatives
    I H Hall
    Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599 7360, USA
    Arch Pharm (Weinheim) 334:229-34. 2001
    ..3-imino-1-oxoisodolines, homophthalimides, napthalidimides, diphenamides, and 6,7-dihydro-5H-dibenz[c,e]azepines proved to be potent inhibitors of the activity of human Tmolt4 T cell leukemia Type II IMP dehydrogenase (IMPDH)...
  96. ncbi An asn to lys polymorphism in the third intracellular loop of the human alpha 2A-adrenergic receptor imparts enhanced agonist-promoted Gi coupling
    K M Small
    Departments of Medicine and Molecular Genetics, University of Cincinnati College of Medicine, Cincinnati, Ohio 45267, USA
    J Biol Chem 275:38518-23. 2000
    ..This enhanced agonist function was observed with catecholamines, azepines, and imidazolines albeit to different degrees...
  97. ncbi Synthesis, anti-inflammatory and ulcerogenicity studies of some substituted pyrimido[1,6-a]azepine derivatives
    Nehad A El-Sayed
    Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El Eini street 11562 Cairo, Egypt
    Eur J Med Chem 45:3147-54. 2010
    New series of pyrimido[1,6-a]azepines were prepared through reaction of the key amino compound 4 with various reagents to give a variety of 3-N-substituted amino derivatives 5-13...
  98. ncbi The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines
    J D Albright
    Chemical Sciences, Wyeth Ayerst Research, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 10:695-8. 2000
    ..Potent orally active AVP receptor antagonists are produced when the benzamide moiety contains a phenyl group at the 2-position. Similar analogues of 4,6,7,8-tetrahydro-5H-thieno[3,2-b]azepine and VPA-985 are reported...
  99. ncbi Synthesis and receptor binding evaluation of clavizepine analogues with no ring D substituents
    M Carmen de la Fuente
    Departamento de Química Orgánica y Unidad Asociada al CSIC, Facultad de Quimica, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain
    J Org Chem 71:3963-6. 2006
    Assembly of the azepine ring of xantheno[9,1-cd]azepines by electrophilic cyclization of sulfonamide acetals provides access to clavizepine analogues in the form of 2,12b-dihydro- or 4-hydroxy-2,3,4,12b-tetrahydro-1H-xantheno[9,1-cd]..
  100. ncbi Rearrangement of N-aryl-2-vinylaziridines to benzoazepines and dihydropyrroles: a synthetic and theoretical study
    Simone Fantauzzi
    Dipartimento di Chimica Inorganica, Metallorganica e Analitica Lamberto Malatesta, Università degli Studi di Milano and ISTM CNR, via Venezian 21, I 20133 Milano, Italy
    Chemistry 15:1241-51. 2009
    ..of the synthetic methodology employed allowed us to obtain differently substituted 2,5-dihydro-1H-benzo[b]azepines in good yields and purities...
  101. ncbi Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence
    Paul E Brennan
    Genito Urinary Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent, UK
    Bioorg Med Chem Lett 19:4999-5003. 2009
    A range of heterocycle fused azepines were synthesized in order to find a CNS penetrant, selective 5-HT(2C) agonist for the treatment of incontinence...

Research Grants143 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 DRIVER; Fiscal Year: 2009
    ..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 GREGORY DRIVER; Fiscal Year: 2010
    ..or o-anthranil decomposition to enable the rapid synthesis of heteroaromatic carbazoles, indoles, functionalized azepines, and aziridines...
  8. 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...
  9. 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...
  10. 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...
  11. 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. ..
  12. INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 2006
    ..The selective synthesis of contiguous stereotriads will advance basic methodology for asymmetric conjugate additions. ..
  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: 2004
    ..The intramolecular (4+2) cycloadditions of nitroalkene precursors will provide facile construction of trans-decalins. . ..
  15. 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. ..
  16. 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. ..
  17. 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. ..
  18. NEW APPROACHES TO ANTIFOLATE CHEMOTHERAPY
    Andre Rosowsky; Fiscal Year: 1993
    ....
  19. ANGIOTENSIN-VASOPRESSIN INTERACTIONS DURING ADAPTATION TO HYPOOSMOLALITY
    Joseph G Verbalis; Fiscal Year: 2010
    ....
  20. CGRP Regulation of iNOS and MAP Kinases/Phosphatases in Trigeminal Ganglia Glia
    Paul Durham; Fiscal Year: 2007
    ....
  21. 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. ..
  22. Asymmetric Lewis Base Catalysis in Main Group Chemistry
    Scott Eric Denmark; Fiscal Year: 2010
    ..Already, catalysis is involved in the processing of nearly a trillion dollars worth of goods produced annually in the US, and our contribution is for chemical reactions for which there is currently no catalytic process. ..
  23. HYPONATREMIA-INDUCED OSTEOPOROSIS
    Joseph Verbalis; Fiscal Year: 2009
    ....
  24. Azinomycins - Total Synthesis and Mechanism of Action
    Robert Coleman; Fiscal Year: 2007
    ..abstract_text> ..
  25. 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. ..
  26. ISOLATION OF THE NEUROBLASTOMA PREDISPOSITION GENE
    John Maris; Fiscal Year: 2002
    ..The successful completion of these studies should have considerable impact on the diagnosis and management of all children with neuroblastoma, a malignancy for which no causal genetic alterations have been identified. ..
  27. AZINOMYCINS--TOTAL SYNTHESIS AND MECHANISM OF ACTION
    Robert Coleman; Fiscal Year: 2001
    ....