amides

Summary

Summary: Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed)

Top Publications

  1. ncbi A ROCK inhibitor permits survival of dissociated human embryonic stem cells
    Kiichi Watanabe
    Organogenesis and Neurogenesis Group, Center for Developmental Biology, RIKEN, Kobe 650 0047, Japan
    Nat Biotechnol 25:681-6. 2007
  2. ncbi Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension
    M Uehata
    Discovery Research Tokyo, Yoshitomi Pharmaceutical Industries Ltd, Saitama, Japan
    Nature 389:990-4. 1997
  3. pmc Mechanism of action of T-705 against influenza virus
    Yousuke Furuta
    Research Laboratories, Toyama Chemical Co, Ltd, 2 4 1 Shimookui, Toyama 930 8508, Japan
    Antimicrob Agents Chemother 49:981-6. 2005
  4. ncbi Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides
    B F Cravatt
    Department of Chemistry, The Scripps Research Institute, La Jolla, California 92307, USA
    Nature 384:83-7. 1996
  5. ncbi An essential part for Rho-associated kinase in the transcellular invasion of tumor cells
    K Itoh
    Department of Tumor Biology, Osaka Medical Center for Cancer and Cardiovascular Diseases, Japan
    Nat Med 5:221-5. 1999
  6. ncbi Effect of the direct Renin inhibitor aliskiren, the Angiotensin receptor blocker losartan, or both on left ventricular mass in patients with hypertension and left ventricular hypertrophy
    Scott D Solomon
    Cardiovascular Division, Brigham and Women s Hospital, 75 Francis St, Boston, MA 02115, USA
    Circulation 119:530-7. 2009
  7. pmc Effect of T-705 treatment on western equine encephalitis in a mouse model
    Justin G Julander
    Institute for Antiviral Research, Utah State University, Logan, 84322 5600, United States
    Antiviral Res 82:169-71. 2009
  8. ncbi Bimatoprost: a review of its use in open-angle glaucoma and ocular hypertension
    Monique P Curran
    Adis, a Wolters Kluwer Business, Auckland, New Zealand
    Drugs Aging 26:1049-71. 2009
  9. ncbi Lipid emulsion reverses Levobupivacaine-induced responses in isolated rat aortic vessels
    Seong Ho Ok
    Department of Anesthesiology and Pain Medicine, Gyeongsang National University Hospital, Jinju, Republic of Korea
    Anesthesiology 114:293-301. 2011
  10. pmc T-705 (favipiravir) activity against lethal H5N1 influenza A viruses
    Maki Kiso
    Division of Virology, Department of Microbiology and Immunology, and International Research Center for Infectious Diseases, Institute of Medical Science, University of Tokyo, Tokyo 108 8639, Japan
    Proc Natl Acad Sci U S A 107:882-7. 2010

Detail Information

Publications392 found, 100 shown here

  1. ncbi A ROCK inhibitor permits survival of dissociated human embryonic stem cells
    Kiichi Watanabe
    Organogenesis and Neurogenesis Group, Center for Developmental Biology, RIKEN, Kobe 650 0047, Japan
    Nat Biotechnol 25:681-6. 2007
    ..We demonstrate that the protective ability of Y-27632 enables SFEB-cultured hES cells to survive and differentiate into Bf1(+) cortical and basal telencephalic progenitors, as do SFEB-cultured mouse ES cells...
  2. ncbi Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension
    M Uehata
    Discovery Research Tokyo, Yoshitomi Pharmaceutical Industries Ltd, Saitama, Japan
    Nature 389:990-4. 1997
    ..Our findings indicate that p160ROCK-mediated Ca2+ sensitization is involved in the pathophysiology of hypertension and suggest that compounds that inhibit this process might be useful therapeutically...
  3. pmc Mechanism of action of T-705 against influenza virus
    Yousuke Furuta
    Research Laboratories, Toyama Chemical Co, Ltd, 2 4 1 Shimookui, Toyama 930 8508, Japan
    Antimicrob Agents Chemother 49:981-6. 2005
    ..These results suggest that T-705RTP, which is generated in infected cells, may function as a specific inhibitor of influenza virus RNA polymerase and contributes to the selective anti-influenza virus activity of T-705...
  4. ncbi Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides
    B F Cravatt
    Department of Chemistry, The Scripps Research Institute, La Jolla, California 92307, USA
    Nature 384:83-7. 1996
    ..serve as the general inactivating enzyme for a growing family of bioactive signalling molecules, the fatty-acid amides. Therefore we will hereafter refer to oleamide hydrolase as fatty-acid amide hydrolase, in recognition of the ..
  5. ncbi An essential part for Rho-associated kinase in the transcellular invasion of tumor cells
    K Itoh
    Department of Tumor Biology, Osaka Medical Center for Cancer and Cardiovascular Diseases, Japan
    Nat Med 5:221-5. 1999
    ..These results indicate that ROCK plays an essential part in tumor cell invasion, and demonstrate its potential as a therapeutic target for the prevention of cancer invasion and metastasis...
  6. ncbi Effect of the direct Renin inhibitor aliskiren, the Angiotensin receptor blocker losartan, or both on left ventricular mass in patients with hypertension and left ventricular hypertrophy
    Scott D Solomon
    Cardiovascular Division, Brigham and Women s Hospital, 75 Francis St, Boston, MA 02115, USA
    Circulation 119:530-7. 2009
    ..We compared the effect of aliskiren, the first orally active direct renin inhibitor, the angiotensin-receptor blocker losartan, and their combination on the reduction of LV mass in hypertensive patients...
  7. pmc Effect of T-705 treatment on western equine encephalitis in a mouse model
    Justin G Julander
    Institute for Antiviral Research, Utah State University, Logan, 84322 5600, United States
    Antiviral Res 82:169-71. 2009
    ..Treatment with T-705 improved morbidity and mortality of WEEV-infected mice, further illustrating the broad-spectrum activity of T-705 in the treatment of RNA viruses...
  8. ncbi Bimatoprost: a review of its use in open-angle glaucoma and ocular hypertension
    Monique P Curran
    Adis, a Wolters Kluwer Business, Auckland, New Zealand
    Drugs Aging 26:1049-71. 2009
    ..Other adverse events included increases in the pigmentation of the iris, perorbital areas and eyelashes...
  9. ncbi Lipid emulsion reverses Levobupivacaine-induced responses in isolated rat aortic vessels
    Seong Ho Ok
    Department of Anesthesiology and Pain Medicine, Gyeongsang National University Hospital, Jinju, Republic of Korea
    Anesthesiology 114:293-301. 2011
    ....
  10. pmc T-705 (favipiravir) activity against lethal H5N1 influenza A viruses
    Maki Kiso
    Division of Virology, Department of Microbiology and Immunology, and International Research Center for Infectious Diseases, Institute of Medical Science, University of Tokyo, Tokyo 108 8639, Japan
    Proc Natl Acad Sci U S A 107:882-7. 2010
    ..We conclude that T-705 shows promise as a therapeutic agent for the treatment of highly pathogenic H5N1 influenza patients...
  11. pmc In vitro and in vivo activities of anti-influenza virus compound T-705
    Y Furuta
    Research Laboratories, Toyama Chemical Co, Ltd, 2 4 1 Shimookui, Toyama, Japan
    Antimicrob Agents Chemother 46:977-81. 2002
    ....
  12. ncbi Favipiravir (T-705) inhibits in vitro norovirus replication
    J Rocha-Pereira
    Laboratorio de Microbiologia, Departamento de Ciencias Biologicas, Faculdade de Farmacia, Universidade do Porto, Rua de Jorge Viterbo Ferreira n 228, 4050 313 Porto, Portugal
    Biochem Biophys Res Commun 424:777-80. 2012
    ..Time-of-drug addition studies reveal that T-705 exerts its activity at a time-point that coincides with onset of viral RNA synthesis, which is in line with the viral polymerase as the presumed target...
  13. ncbi Aliskiren prevents cardiovascular complications and pancreatic injury in a mouse model of obesity and type 2 diabetes
    Y F Dong
    Department of Pharmacology and Molecular Therapeutics, Kumamoto University Graduate School of Medical Sciences, Kumamoto 860 8556, Japan
    Diabetologia 53:180-91. 2010
    ..The present study was undertaken to examine the efficacy of aliskiren, a direct renin inhibitor, on cardiovascular injuries, glucose intolerance and pancreatic injury in a mouse model of type 2 diabetes...
  14. ncbi Direct renin inhibition in addition to or as an alternative to angiotensin converting enzyme inhibition in patients with chronic systolic heart failure: rationale and design of the Aliskiren Trial to Minimize OutcomeS in Patients with HEart failuRE (ATMOS
    Henry Krum
    Centre of Cardiovascular Research and Education in Therapeutics, Department of Epidemiology and Preventive Medicine, Monash University Alfred Hospital, Melbourne VIC 3004, Australia
    Eur J Heart Fail 13:107-14. 2011
    ..Perspective The ATMOSPHERE study will definitively determine the role of a DRI strategy additional to or as an alternative to conventional RAAS blockade in patients with chronic systolic HF...
  15. ncbi High-volume infiltration analgesia in total knee arthroplasty: a randomized, double-blind, placebo-controlled trial
    L Ø Andersen
    Department of Anesthesiology, Hvidovre University Hospital, Copenhagen, Denmark
    Acta Anaesthesiol Scand 52:1331-5. 2008
    ..The present placebo-controlled study was carried out to evaluate the analgesic effect of high-volume infiltration analgesia in bilateral total knee arthroplasty, along with a detailed description of the infiltration technique...
  16. pmc Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice
    Robert W Sidwell
    Institute for Antiviral Research, Utah State University, 5600 Old Main Hill, Logan, UT 84322 5600, USA
    Antimicrob Agents Chemother 51:845-51. 2007
    ..These data indicate that T-705 may be useful for the treatment of avian influenza virus infections...
  17. pmc RhoA is required for monocyte tail retraction during transendothelial migration
    R A Worthylake
    Department of Cell and Developmental Biology, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
    J Cell Biol 154:147-60. 2001
    ..Finally, we find that p160ROCK signaling negatively regulates integrin adhesions and that inhibition of RhoA results in an accumulation of beta2 integrin in the unretracted tails...
  18. ncbi Local infiltration analgesia: a technique for the control of acute postoperative pain following knee and hip surgery: a case study of 325 patients
    Dennis R Kerr
    Joint Orthopaedic Centre, New South Wales, Australia
    Acta Orthop 79:174-83. 2008
    ..The technique allows virtually immediate mobilization and earlier discharge from hospital...
  19. pmc Effective oral favipiravir (T-705) therapy initiated after the onset of clinical disease in a model of arenavirus hemorrhagic Fever
    Michelle Mendenhall
    Department of Animal, Dairy, and Veterinary Sciences, Utah State University, Logan, Utah, United States of America
    PLoS Negl Trop Dis 5:e1342. 2011
    ..At present, ribavirin is the only antiviral drug indicated for use in treatment of these diseases, but because of its limited efficacy in advanced cases of disease and its toxicity, safer and more effective antivirals are needed...
  20. ncbi Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and
    Patricia L Podolin
    Respiratory and Inflammation Center of Excellence for Drug Discovery, GlaxoSmithKline, King of Prussia, PA 19406, USA
    J Pharmacol Exp Ther 312:373-81. 2005
    ..5 mg/kg, i.p., every other day. These results suggest that reduction of proinflammatory mediators and inhibition of antigen-induced T cell proliferation are mechanisms underlying the attenuation of CIA by the IKK-2 inhibitor, TPCA-1...
  21. ncbi A compression bandage improves local infiltration analgesia in total knee arthroplasty
    Lasse Ø Andersen
    Departments of Anesthesiology, Hvidovre University Hospital, Copenhagen, Denmark
    Acta Orthop 79:806-11. 2008
    ..High-volume local infiltration analgesia has been shown to be an effective pain treatment after knee replacement, but the role of bandaging to prolong analgesia has not been evaluated...
  22. ncbi Gene-silencing properties of siRNAs that contain internal amide-bond linkages
    Wei Gong
    Faculty of Science, University of Ontario Institute of Technology, 2000 Simcoe Street North, Oshawa, Ontario, Canada L1H 7K4
    Bioorg Med Chem Lett 22:6934-7. 2012
    ..Biophysical data indicates that melting temperatures of the siRNAs decrease when the modification is located internally...
  23. ncbi A single point mutation in the novel PvCesA3 gene confers resistance to the carboxylic acid amide fungicide mandipropamid in Plasmopara viticola
    Mathias Blum
    Institute of Botany, University of Basel, Basel, Switzerland
    Fungal Genet Biol 47:499-510. 2010
    ..Our data demonstrate that the identified genes are putative cellulose synthases and that one recessive mutation in PvCesA3 causes inheritable resistance to the CAA fungicide mandipropamid...
  24. ncbi Structure-based design of aliskiren, a novel orally effective renin inhibitor
    Jeanette M Wood
    Novartis Institute for Biomedical Research, Klybeckstrasse 220, CH 4002 Basel, Switzerland
    Biochem Biophys Res Commun 308:698-705. 2003
    ..Aliskiren represents the first in a novel class of renin inhibitors with the potential for treatment of hypertension and related cardiovascular diseases...
  25. ncbi Mandipropamid targets the cellulose synthase-like PiCesA3 to inhibit cell wall biosynthesis in the oomycete plant pathogen, Phytophthora infestans
    Mathias Blum
    Syngenta Crop Protection AG, CH 4332 Stein, Switzerland
    Mol Plant Pathol 11:227-43. 2010
    ..The transformation and expression of a mutated PiCesA3 allele was carried out in a sensitive wild-type isolate to demonstrate that the mutations in PiCesA3 were responsible for the MPD insensitivity phenotype...
  26. ncbi Aliskiren reduces sympathetic nerve activity and blood pressure in chronic kidney disease patients
    Laima Siddiqi
    Department of Nephrology and Hypertension, University Medical Centre Utrecht, Utrecht, The Netherlands
    Nephrol Dial Transplant 26:2930-4. 2011
    ..Hypertensive chronic kidney disease (CKD) patients often have sympathetic hyperactivity. In this pilot study, we evaluated the effect of 6 weeks treatment with aliskiren on sympathetic activity in hypertensive Stages 2-4 CKD patients...
  27. ncbi Beneficial cardiac effects of the renin inhibitor aliskiren in spontaneously hypertensive rats
    Joep H M van Esch
    Department of Internal Medicine, Division of Vascular Medicine and Pharmacology, Erasmus MC, Rotterdam, The Netherlands
    J Hypertens 28:2145-55. 2010
    ..Here, we compared the cardiac effects of aliskiren, the AT1 receptor blocker irbesartan and the ACE inhibitor captopril in spontaneously hypertensive rats (SHR) at equi-hypotensive doses...
  28. pmc Maporal virus as a surrogate for pathogenic New World hantaviruses and its inhibition by favipiravir
    Kristin K Buys
    Institute for Antiviral Research and Department of Animal, Dairy, and Veterinary Sciences, Utah State University, Logan, UT, USA
    Antivir Chem Chemother 21:193-200. 2011
    ..Dobrava virus causes HFRS in Europe. Maporal virus (MPRLV), recently isolated from western Venezuela, is phylogenetically similar to Andes virus, the principal cause of HCPS in Argentina...
  29. pmc T-705 (favipiravir) inhibition of arenavirus replication in cell culture
    Michelle Mendenhall
    Institute for Antiviral Research and Department of Animal, Dairy, and Veterinary Sciences, Utah State University, Logan, UT 84322 5600, USA
    Antimicrob Agents Chemother 55:782-7. 2011
    ..Our findings indicate that T-705 acts to inhibit arenavirus replication/transcription and may directly target the viral RNA-dependent RNA polymerase...
  30. ncbi ROCK inhibition and CNTF interact on intrinsic signalling pathways and differentially regulate survival and regeneration in retinal ganglion cells
    Paul Lingor
    1Department of Neurology, Georg August University Gottingen, University Medicine, Waldweg 33, 37073 Gottingen, Germany
    Brain 131:250-63. 2008
    ..The interaction of intracellular signalling pathways may, however, attenuate more pronounced synergy and has to be taken into account for future treatment strategies...
  31. ncbi ROCK inhibition promotes adult retinal ganglion cell neurite outgrowth only in the presence of growth promoting factors
    Zubair Ahmed
    Molecular Neuroscience Group, School of Clinical and Experimental Medicine, College of Medical and Dental Sciences, University of Birmingham, Room WX2 17 Institute of Biomedical Research West, Edgbaston, Birmingham, B15 2TT, UK
    Mol Cell Neurosci 42:128-33. 2009
    ..Our results suggest that Y27632-induced ROCK inhibition promotes robust disinhibited axon regeneration of adult neurons only when growth promoting factors are added and/or cAMP levels are raised...
  32. ncbi Pharmacological inhibition of Rho-kinase signaling with Y-27632 blocks melanoma tumor growth
    Alissa Routhier
    Ghosh Science and Technology Center, Department of Biology, Worcester State College, Worcester, MA 01602, USA
    Oncol Rep 23:861-7. 2010
    ..IP injection of Y-27632 in tumor-bearing mice resulted in a reduction in melanoma tumor volume compared to control treated mice. These findings suggest that ROCK inhibition can reduce melanoma tumorigenicity...
  33. ncbi Rapid neurite outgrowth in neurosecretory cells and neurons is sustained by the exocytosis of a cytoplasmic organelle, the enlargeosome
    Gabriella Racchetti
    Division of Neuroscience, Vita Salute San Raffaele University and Scientific Institute San Raffaele, National Institute of Neuroscience Italy, IIT Network, Research Unit of Molecular Neuroscience, Via Olgettina 58, I 20132 Milan, Italy
    J Cell Sci 123:165-70. 2010
    ..However, its properties and its physiological and pathological role remain to be investigated...
  34. ncbi Baseline characteristics in the Aliskiren Trial in Type 2 Diabetes Using Cardio-Renal Endpoints (ALTITUDE)
    Hans Henrik Parving
    Department of Medical Endocrinology, Rigshospitalet, University of Copenhagen, Denmark
    J Renin Angiotensin Aldosterone Syst 13:387-93. 2012
    ..Aliskiren, a novel direct renin inhibitor, which lowers plasma renin activity, may thereby provide greater cardio-renal protection compared with angiotensin converting enzyme inhibitor (ACEi) or angiotensin receptor blocker (ARB) alone...
  35. pmc Synthesis and structure-activity relationships of N-(2-oxo-3-oxetanyl)amides as N-acylethanolamine-hydrolyzing acid amidase inhibitors
    Carlos Solorzano
    Department of Pharmacology, University of California, Irvine, 360 MSRII, Irvine, California 92697 4625, USA
    J Med Chem 53:5770-81. 2010
    ....
  36. pmc Diarylethynyl amides that recognize the parallel conformation of genomic promoter DNA G-quadruplexes
    Jyotirmayee Dash
    The University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK
    J Am Chem Soc 130:15950-6. 2008
    ..Our results indicate that the recognition of the c-kit2 quadruplex by these ligands is achieved through groove binding, which favors the formation of a parallel conformation...
  37. ncbi The increase in renin during renin inhibition: does it result in harmful effects by the (pro)renin receptor?
    A H Jan Danser
    Division of Pharmacology, Vascular and Metabolic Diseases, Department of Internal Medicine, Erasmus MC, Rotterdam, The Netherlands
    Hypertens Res 33:4-10. 2010
    ....
  38. ncbi Periorbital fat atrophy - an unfamiliar side effect of prostaglandin analogues
    Anuradha Jayaprakasam
    Ophthalmology Department, Broomfield Hospital, Court Road, Chelmsford, Essex
    Orbit 29:357-9. 2010
    ..The periorbital fat atrophy is most apparent with uniocular use and both doctors and patients need to be aware of this side effect before commencing treatment. The effects, however, appear to be reversible with treatment cessation...
  39. ncbi Rationale and design of the multicentre, randomized, double-blind, placebo-controlled Aliskiren Trial on Acute Heart Failure Outcomes (ASTRONAUT)
    Mihai Gheorghiade
    Center for Cardiovascular Innovation, Northwestern University Feinberg School of Medicine, 645 N Michigan Avenue, Suite 1006, Chicago, IL 60611, USA
    Eur J Heart Fail 13:100-6. 2011
    ..The aim of the Aliskiren Trial on Acute Heart Failure Outcomes (ASTRONAUT) study is to evaluate the effect of aliskiren on cardiovascular death and HF in AHFS patients...
  40. ncbi Enhancement on primate corneal endothelial cell survival in vitro by a ROCK inhibitor
    Naoki Okumura
    Department of Ophthalmology, Kyoto Prefectural University of Medicine, Kyoto, Japan
    Invest Ophthalmol Vis Sci 50:3680-7. 2009
    ..The present study was conducted to investigate the applicability of the Rho kinase (ROCK) inhibitor Y-27632 in promoting cultivation of cynomolgus monkey (M)CECs...
  41. pmc Myosin light chain kinase activation and calcium sensitization in smooth muscle in vivo
    Yusuke Mizuno
    Dept Physiology, UT Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390 9040, USA
    Am J Physiol Cell Physiol 295:C358-64. 2008
    ..Thus the onset of agonist-induced contraction in phasic smooth muscle results from the rapid and coordinated activation of MLCK with hierarchical inhibition of MLCP by CPI-17 and MYPT1 phosphorylation...
  42. ncbi Cuticular lipids of the booklouse, Liposcelis bostrychophila: hydrocarbons, aldehydes, fatty acids, and fatty acid amides
    Ralph W Howard
    USDA ARS, GMPRC, 1515 College Avenue, Manhattan, KS 66502, USA
    J Chem Ecol 29:615-27. 2003
    ..the first report of the hydrocarbons of any member of the Order Psocoptera and the first report of fatty acid amides as cuticular components for any insect). No unsaturated hydrocarbons were present...
  43. ncbi Patients with acute coronary syndromes and elevated levels of natriuretic peptides: the results of the AVANT GARDE-TIMI 43 Trial
    Benjamin M Scirica
    TIMI Study Group, Cardiovascular Division, Brigham and Women s Hospital, 75 Francis Street, Boston, MA 02115, USA
    Eur Heart J 31:1993-2005. 2010
    ....
  44. pmc ROCK inhibition enhances the recovery and growth of cryopreserved human embryonic stem cells and human induced pluripotent stem cells
    David A Claassen
    Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, Nebraska 68198 6805, USA
    Mol Reprod Dev 76:722-32. 2009
    ..Together, these results argue that Y-27632 is a useful tool in overcoming obstacles to studies involving the cultivation of both hES cells and human iPS cells...
  45. pmc Age-related changes in human crystallins determined from comparative analysis of post-translational modifications in young and aged lens: does deamidation contribute to crystallin insolubility?
    P A Wilmarth
    Department of Integrative Biosciences, School of Dentistry, Oregon Health and Science University, 611 South West Campus Drive, Portland, Oregon 97239, USA
    J Proteome Res 5:2554-66. 2006
    ..On the basis of spectral counting, the most abundant PTMs in aged lenses were deamidations and methylated cysteines with other PTMs present at lower levels...
  46. ncbi Effect of ROCK inhibitor Y-27632 on normal and variant human embryonic stem cells (hESCs) in vitro: its benefits in hESC expansion
    Kalamegam Gauthaman
    Department of Obstetrics and Gynaecology, Yong Loo Lin School of Medicine, National University of Singapore, 5 Lower Kent Ridge Road, Singapore, 119074, Singapore
    Stem Cell Rev 6:86-95. 2010
    ..The results confirmed that Y-27632 is a useful agent that aids in the expansion of undifferentiated hESC numbers for downstream applications in regenerative medicine...
  47. ncbi Bupivacaine, levobupivacaine and ropivacaine: are they clinically different?
    Andrea Casati
    Department of Anaesthesiology, University of Parma, Italy
    Best Pract Res Clin Anaesthesiol 19:247-68. 2005
    ....
  48. ncbi Oxygen activates the Rho/Rho-kinase pathway and induces RhoB and ROCK-1 expression in human and rabbit ductus arteriosus by increasing mitochondria-derived reactive oxygen species: a newly recognized mechanism for sustaining ductal constriction
    Hidemi Kajimoto
    Vascular Biology Group, Alberta Cardiovascular and Stroke Research Centre ABACUS, University of Alberta, Edmonton, Canada
    Circulation 115:1777-88. 2007
    ..Subsequent membrane depolarization and calcium influx through L-type calcium channels initiates functional closure. We hypothesize that Rho-kinase activation is an additional mechanism that sustains DA constriction...
  49. pmc Prediction of protein deamidation rates from primary and three-dimensional structure
    N E Robinson
    Division of Chemistry, California Institute of Technology, Pasadena, CA 91125, USA
    Proc Natl Acad Sci U S A 98:4367-72. 2001
    ..The relative importance of primary structure and three-dimensional structure in Asn deamidation is estimated...
  50. ncbi Phenolamides: bridging polyamines to the phenolic metabolism
    Jean Etienne Bassard
    Institute of Plant Molecular Biology, CNRS UPR 2357, University of Strasbourg, 28 rue Goethe, 67000 Strasbourg, France
    Phytochemistry 71:1808-24. 2010
    ..Phenolamides were often considered as accumulated end-chain products. Recent data bring a light on their biosynthesis and suggests their possible contribution in the branching of the phenylpropanoid metabolism...
  51. ncbi Molecular characterization of the effects of Y-27632
    Hassina Darenfed
    Department of Anatomy and Cell Biology, McGill University, Montreal, Quebec, Canada
    Cell Motil Cytoskeleton 64:97-109. 2007
    ..We conclude that several kinases contribute to the global effect of Y-27632 on cellular responses...
  52. ncbi Effects of aliskiren on blood pressure, albuminuria, and (pro)renin receptor expression in diabetic TG(mRen-2)27 rats
    David L Feldman
    Novartis Institutes for BioMedical Research, Bldg 437, Rm 3317, One Health Plaza, E Hanover, NJ 07936, USA
    Hypertension 52:130-6. 2008
    ....
  53. pmc ROCK1 feedback regulation of the upstream small GTPase RhoA
    Alan T Tang
    Department of Pharmacology and Toxicology, Medical College of Wisconsin, Milwaukee, WI 53226, United States
    Cell Signal 24:1375-80. 2012
    ....
  54. ncbi Activation of the intracellular renin-angiotensin system in cardiac fibroblasts by high glucose: role in extracellular matrix production
    Vivek P Singh
    Cardiovascular Research Institute, Texas A and M HSC, Temple, TX 76504, USA
    Am J Physiol Heart Circ Physiol 294:H1675-84. 2008
    ....
  55. ncbi Effect of the direct renin inhibitor aliskiren on left ventricular remodelling following myocardial infarction with systolic dysfunction
    Scott D Solomon
    Cardiovascular Division, Brigham and Women s Hospital, Boston, MA, USA
    Eur Heart J 32:1227-34. 2011
    ....
  56. ncbi Crystal structures of the CERT START domain with inhibitors provide insights into the mechanism of ceramide transfer
    Norio Kudo
    Structural Biology Research Center, Photon Factory, Institute of Materials Structure Science, High Energy Accelerator Research Organization KEK, Tsukuba, Ibaraki, Japan
    J Mol Biol 396:245-51. 2010
    ..These results provide insights into not only the molecular mechanism of inhibition by HPAs but also possible mechanisms by which CERT interacts with ceramide...
  57. pmc In vitro and in vivo activities of T-705 against arenavirus and bunyavirus infections
    Brian B Gowen
    Institute for Antiviral Research, Utah State University, Logan, UT 84322, USA
    Antimicrob Agents Chemother 51:3168-76. 2007
    ..Our results suggest that T-705 may be a viable alternative for the treatment of life-threatening bunyaviral and arenaviral infections...
  58. ncbi Central nervous system and cardiac effects from long-acting amide local anesthetic toxicity in the intact animal model
    Leanne Groban
    Department of Anesthesiology, Wake Forest University School of Medicine, Winston Salem, North Carolina 27157 1009, USA
    Reg Anesth Pain Med 28:3-11. 2003
    ....
  59. ncbi Twelve-month, randomized, controlled trial of bimatoprost 0.01%, 0.0125%, and 0.03% in patients with glaucoma or ocular hypertension
    L Jay Katz
    Wills Eye Hospital, Philadelphia, PA 19107, USA
    Am J Ophthalmol 149:661-671.e1. 2010
    ..To evaluate the intraocular pressure (IOP)-lowering efficacy and safety of ophthalmic formulations of bimatoprost 0.01% and 0.0125% compared with bimatoprost 0.03%...
  60. pmc Identification and pharmacological characterization of the prostaglandin FP receptor and FP receptor variant complexes
    Y Liang
    Departments of Biological and Chemical Sciences, Allergan Inc, Irvine, CA, USA
    Br J Pharmacol 154:1079-93. 2008
    ..Hence, to elucidate the molecular mechanisms of this effect of bimatoprost, we focused on pharmacologically characterizing prostaglandin FP receptor (FP) and FP receptor variant (altFP) complexes...
  61. pmc ROCK inhibitor Y-27632 suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells and increases their cloning efficiency
    Li Zhang
    Department of Molecular and Cell Biology, Baylor College of Medicine, Houston, Texas, United States of America
    PLoS ONE 6:e18271. 2011
    ....
  62. ncbi The rho-kinase inhibitors Y-27632 and fasudil act synergistically with imatinib to inhibit the expansion of ex vivo CD34(+) CML progenitor cells
    J Burthem
    Division of Laboratory and Regenerative Medicine, Stopford Building, Manchester, UK
    Leukemia 21:1708-14. 2007
    ..Our studies may indicate therapeutic benefit in some cases for the combination of rho-kinase inhibitors with imatinib...
  63. ncbi Molecular interactions of CCR5 with major classes of small-molecule anti-HIV CCR5 antagonists
    Rama Kondru
    Department of Medicinal Chemistry, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 94304, USA
    Mol Pharmacol 73:789-800. 2008
    ..The fully mapped binding pocket of CCR5 is being used for structure-based design and lead optimization of novel anti-HIV CCR5 inhibitors with improved potency and better resistance profile...
  64. pmc Reduced hospital stay, morphine consumption, and pain intensity with local infiltration analgesia after unicompartmental knee arthroplasty
    Per Essving
    Department of Orthopedic Surgery, University of Linkoping, Sweden
    Acta Orthop 80:213-9. 2009
    ..The degree of postoperative pain is usually moderate to severe following knee arthroplasty. We investigated the efficacy of local administration of analgesics into the operating area, both intraoperatively and postoperatively...
  65. ncbi Sphingosine 1-phosphate stimulates smooth muscle cell differentiation and proliferation by activating separate serum response factor co-factors
    Kashelle Lockman
    Department of Pathology and Laboratory Medicine, University of North Carolina, Chapel Hill, North Carolina 27599, USA
    J Biol Chem 279:42422-30. 2004
    ..Taken together these results demonstrate that S1P activates multiple signaling pathways in SMC and regulates proliferation by ERK-dependent activation of Elk-1 and differentiation by RhoA-dependent activation of MRTF-A...
  66. pmc Treatment of late stage disease in a model of arenaviral hemorrhagic fever: T-705 efficacy and reduced toxicity suggests an alternative to ribavirin
    Brian B Gowen
    Institute for Antiviral Research, Logan, UT, USA
    PLoS ONE 3:e3725. 2008
    ..Our findings support further pre-clinical development of T-705 for the treatment of severe arenaviral infections...
  67. pmc Protein deamidation
    Noah E Robinson
    Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA
    Proc Natl Acad Sci U S A 99:5283-8. 2002
    ..The calculated values have good quantitative reliability when compared with experimental measurements. These rates demonstrate that deamidation may be a biologically relevant phenomenon in a remarkably large percentage of proteins...
  68. ncbi Smooth muscle differentiation marker gene expression is regulated by RhoA-mediated actin polymerization
    C P Mack
    Department of Molecular Physiology and Biological Physics, University of Virginia Medical School, Charlottesville, Virginia 22908, USA
    J Biol Chem 276:341-7. 2001
    ..The results also suggest that RhoA signaling may serve as a convergence point for the multiple signaling pathways that regulate SMC differentiation...
  69. ncbi Activation of RhoA and inhibition of myosin phosphatase as important components in hypertension in vascular smooth muscle
    Tetsuya Seko
    First Department of Internal Medicine, Mie University School of Medicine, 2 174 Edobashi, Tsu, Mie 514 8507, Japan
    Circ Res 92:411-8. 2003
    ..These results suggest that independent of the cause of hypertension, a common point in downstream signaling and a critical component of hypertension is activation of RhoA and subsequent activation of Rho-kinase...
  70. pmc Pungent agents from Szechuan peppers excite sensory neurons by inhibiting two-pore potassium channels
    Diana M Bautista
    Department of Physiology, University of California, San Francisco, 600 16th St, San Francisco, California 94143 2140, USA
    Nat Neurosci 11:772-9. 2008
    ....
  71. pmc Rho-dependent formation of epithelial "leader" cells during wound healing
    T Omelchenko
    Program in Cellular and Molecular Biodynamics and Department of Biological Sciences, Rutgers University, Newark, NJ 07102, USA
    Proc Natl Acad Sci U S A 100:10788-93. 2003
    ..The transition between these two patterns is controlled by Rho activity, which in turn controls the dynamic distribution and activity of actin filament bundles, myosin II, and microtubules...
  72. pmc Intracellular angiotensin II production in diabetic rats is correlated with cardiomyocyte apoptosis, oxidative stress, and cardiac fibrosis
    Vivek P Singh
    Division of Molecular Cardiology, Department of Medicine, Texas A and M Health Science Center, College of Medicine, Scott and White, Central Texas Veterans Health Care System, Temple, TX, USA
    Diabetes 57:3297-306. 2008
    ..In the present study, we determined whether hyperglycemia activates the cardiac intracellular renin-Ang system (RAS) in vivo and whether ARBs, ACE, or renin inhibitors block synthesis and effects of intracellular Ang II (iAng II)...
  73. ncbi Successful resuscitation of a patient with ropivacaine-induced asystole after axillary plexus block using lipid infusion
    R J Litz
    Department of Anaesthesiology and Intensive Care Medicine, Fetscher Str 74, University Hospital Dresden, 01307 Dresden, Germany
    Anaesthesia 61:800-1. 2006
    ..This case shows that lipid infusion may have a beneficial role in cases of local anaesthetic toxicity when conventional resuscitation has been unsuccessful...
  74. pmc A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5
    T Dragic
    Aaron Diamond AIDS Research Center, The Rockefeller University, New York, NY 10016, USA
    Proc Natl Acad Sci U S A 97:5639-44. 2000
    ....
  75. ncbi Pharmacokinetics and efficacy of ropivacaine continuous wound instillation after joint replacement surgery
    M Bianconi
    Department of Anesthesiology and Intensive Care, St Anna Hospital Ferrara, Ferrara, Italy
    Br J Anaesth 91:830-5. 2003
    ....
  76. ncbi Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase
    Torsten Steinmetzer
    Curacyte Chemistry GmbH, Winzerlaer Strasse 2, D 07745 Jena, Germany
    J Med Chem 49:4116-26. 2006
    ..Through screening, we have identified bis-basic secondary amides of sulfonylated 3-amidinophenylalanine as matriptase inhibitors...
  77. ncbi Aliskiren combined with losartan in immunoglobulin A nephropathy: an open-labeled pilot study
    Sydney C W Tang
    Nephrology Division, Department of Medicine, Queen Mary Hospital, The University of Hong Kong, Hong Kong, China
    Nephrol Dial Transplant 27:613-8. 2012
    ..Its potential efficacy in nondiabetic chronic kidney diseases that are driven by renin-angiotensin system activation remains to be explored...
  78. ncbi Measurement of 18 perfluorinated organic acids and amides in human serum using on-line solid-phase extraction
    Zsuzsanna Kuklenyik
    Division of Laboratory Sciences, National Center for Environmental Health, Centers for Disease Control and Prevention, Atlanta, Georgia 30341, USA
    Anal Chem 77:6085-91. 2005
    ..The high throughput and low limits of detection (0.05-0.8 ng/mL) using a small sample volume (100 microL of serum) and isotope dilution quantification make this method suitable for large-scale epidemiologic studies...
  79. ncbi Yaku'amides A and B, cytotoxic linear peptides rich in dehydroamino acids from the marine sponge Ceratopsion sp
    Reiko Ueoka
    Laboratory of Aquatic Natural Products Chemistry, Graduate School of Agricultural and Life Sciences, The University of Tokyo, Bunkyo ku, Tokyo 113 8657, Japan
    J Am Chem Soc 132:17692-4. 2010
    Two cytotoxic peptides, yaku'amides A (1) and B (2), were isolated from the marine sponge Ceratopsion sp...
  80. pmc No evidence of a clinically important effect of adding local infusion analgesia administrated through a catheter in pain treatment after total hip arthroplasty
    Kirsten Specht
    Clinical Research Unit, Department of Orthopaedics, Vejle Hospital, Denmark
    Acta Orthop 82:315-20. 2011
    ..LIA at the time of surgery is a validated treatment. We investigated the additional effect of giving postoperative LINFA after THA in patients already having LIA during surgery...
  81. ncbi Comparison of Travoprost and Bimatoprost plus timolol fixed combinations in open-angle glaucoma patients previously treated with latanoprost plus timolol fixed combination
    Marco Centofanti
    Unità Dipartimentale Semplice di Glaucoma, University of Tor Vergata, Rome, Italy Istituto di Ricovero e Cura a Carattere Scientifico Fondazione G B Bietti, Rome, Italy
    Am J Ophthalmol 150:575-80. 2010
    ....
  82. ncbi Latanoprost therapy after sunken eyes caused by travoprost or bimatoprost
    Shunsuke Nakakura
    Department of Ophthalmology, Saneikai Tsukazaki Hospital, Himeji, Hyogo Prefecture, Japan
    Optom Vis Sci 88:1140-4. 2011
    ..To report clinical results of switching to latanoprost therapy in patients with deepening of the upper eyelid sulcus caused by travoprost and bimatoprost...
  83. ncbi Aliskiren enhances the protective effects of valsartan against cardiovascular and renal injury in endothelial nitric oxide synthase-deficient mice
    Eiichiro Yamamoto
    Department of Pharmacology and Molecular Therapeutics, Kumamoto University Graduate School of Medical Sciences, 1 1 1 Honjyo, Kumamoto, Japan
    Hypertension 54:633-8. 2009
    ..The combination of aliskiren and valsartan seems to be a promising therapeutic strategy for hypertensive organ injury caused by endothelial NO synthase dysfunction...
  84. ncbi MT1-selective melatonin receptor ligands: synthesis, pharmacological evaluation, and molecular dynamics investigation of N-{[(3-O-substituted)anilino]alkyl}amides
    Silvia Rivara
    Dipartimento di Farmacia, Universita degli Studi di Parma, V le G P Usberti 27A, 43124 Parma Italy
    ChemMedChem 7:1954-64. 2012
    ..N-(Anilinoalkyl)amides are a versatile class of melatonin receptor ligands that include nonselective MT1/MT2 agonists and MT2-selective ..
  85. ncbi Antifungal amides from Piper arboreum and Piper tuberculatum
    Renata Vasques da Silva
    Instituto de Quimica, Universidade Estadual Paulista, CP 355, 14800 900, Araraquara SP, Brazil
    Phytochemistry 59:521-7. 2002
    In continuation of our study of the Piperaceae we have isolated several amides, mainly those bearing isobutyl, pyrrolidine, dihydropyridone and piperidine moieties...
  86. ncbi Prospective isolation and characterization of bipotent progenitor cells in early mouse liver development
    Ken Okada
    Division of Stem Cell Therapy, Center for Stem Cell Biology and Regenerative Medicine, The Institute of Medical Science, The University of Tokyo, Tokyo, Japan
    Stem Cells Dev 21:1124-33. 2012
    ..5 but decreased dramatically thereafter. These first prospective studies of early fetal HSPC candidates demonstrate that bipotent stem/progenitor cells exist before E11.5 and implicate Rock-myosin II signaling in their development...
  87. ncbi Pentapeptide amides interfere with the aggregation of beta-amyloid peptide of Alzheimer's disease
    Csaba Hetényi
    Department of Medical Chemistry, University of Szeged, Dom ter 8, Szeged, H 6720, Hungary
    Biochem Biophys Res Commun 292:931-6. 2002
    ..In the present study, the effects of two pentapeptide amides are reported. These compounds were designed by using the C-terminal sequence of the amyloid peptide as a template...
  88. ncbi Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers
    Eric Vieira
    Pharma Division, Discovery Research, F Hoffmann La Roche Ltd, CH 4070 Basel, Switzerland
    Bioorg Med Chem Lett 19:1666-9. 2009
    ..molecule mGluR1 enhancers, which are 9H-xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides, have been previously reported...
  89. ncbi Enrichment and clonal culture of progenitor cells during mouse postnatal liver development in mice
    Akihide Kamiya
    Division of Stem Cell Therapy, Center for Stem Cell Biology and Regenerative Medicine, Institute of Medical Science, University of Tokyo, Tokyo, Japan
    Gastroenterology 137:1114-26, 1126.e1-14. 2009
    ..This study aimed to establish a primary culture system for clone-sorted PLSCs...
  90. ncbi Aliskiren ameliorates chlorhexidine digluconate-induced peritoneal fibrosis in rats
    Chun Yen Ke
    Tzu Chi University, Hualien, Taiwan
    Eur J Clin Invest 40:301-9. 2010
    ..The present study was designed to investigate the protective effects of aliskiren on chlorhexidine digluconate-induced PF in rats...
  91. pmc Impact of baseline renal function on the efficacy and safety of aliskiren added to losartan in patients with type 2 diabetes and nephropathy
    Frederik Persson
    Steno Diabetes Center, Gentofte, Denmark
    Diabetes Care 33:2304-9. 2010
    ..This post hoc analysis assessed the efficacy and safety of aliskiren added to the maximal recommended dose of losartan according to baseline estimated GFR (eGFR) (stage 1-3 chronic kidney disease [CKD])...
  92. pmc Genetic analysis of fenhexamid-resistant field isolates of the phytopathogenic fungus Botrytis cinerea
    Sabine Fillinger
    INRA UMR1290 BIOGER CPP, F 78000 Versailles, France
    Antimicrob Agents Chemother 52:3933-40. 2008
    ..The HydR3 mutations possibly modify the affinity of the 3-ketoreductase enzyme for its specific inhibitor, fenhexamid...
  93. pmc Aliskiren in combination with losartan reduces albuminuria independent of baseline blood pressure in patients with type 2 diabetes and nephropathy
    Frederik Persson
    Steno Diabetes Center, Niels Steensensvej 1, DK 2820 Gentofte, Denmark
    Clin J Am Soc Nephrol 6:1025-31. 2011
    ..Our post hoc analysis assessed the baseline BP influence on the antiproteinuric effect in the Aliskiren in the Evaluation of Proteinuria in Diabetes (AVOID) study...
  94. ncbi Design, synthesis and insecticidal activities of novel pyrazole amides containing hydrazone substructures
    Jian Wu
    State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang, China
    Pest Manag Sci 68:801-10. 2012
    ..In an effort to discover new molecules with good insecticidal activities, a series of pyrazole amide derivatives containing hydrazone substructures were synthesised and bioassayed...
  95. ncbi Safety and efficacy of aliskiren in the treatment of hypertension: a systematic overview
    Fabio Angeli
    Hospital Media Valle del Tevere Pantalla, AUSL 2 Umbria, Department of Cardiology, Section of Cardiology, Perugia, Italy
    Expert Opin Drug Saf 11:659-70. 2012
    ..Aliskiren's inhibitory effect on angiotensin I generation, through renin blockade, is highly specific and long-lasting (24 hours). This feature differentiates aliskiren from traditional antihypertensive drugs...
  96. ncbi The Fps1p aquaglyceroporin facilitates the use of small aliphatic amides as a nitrogen source by amidase-expressing yeasts
    Andrew Shepherd
    Department of Molecular Biology and Biotechnology, University of Sheffield, Sheffield, UK
    FEMS Yeast Res 10:527-34. 2010
    ..However, in Z. rouxii, the loss of Fps1p severely compromised the use of acetamide and several other small amides as sources of nitrogen, an indication that these amides enter the cells of this yeast by passive diffusion through ..
  97. ncbi Baseline sensitivity of natural population and resistance of mutants in Phytophthora capsici to zoxamide
    Yang Bi
    Department of Plant Pathology, China Agricultural University, Beijing, China
    Phytopathology 101:1104-11. 2011
    ..There was no cross resistance between zoxamide and either flumorph, metalaxyl, azoxystrobin, or etridiazole. Based on the results above, P. capsici can develop resistance to zoxamide, and the risk is predicted to be moderate in nature...
  98. ncbi A study of dose-proportionality in the pharmacokinetics of the oral direct renin inhibitor aliskiren in healthy subjects
    D Limoges
    Novartis Pharma AG, Basel, Switzerland
    Int J Clin Pharmacol Ther 46:252-8. 2008
    ..To evaluate the dose-proportionality of the pharmacokinetics of aliskiren, the first in a new class of orally active direct renin inhibitors approved for the treatment of hypertension...
  99. pmc Blocking the RAAS at different levels: an update on the use of the direct renin inhibitors alone and in combination
    Francesca Cagnoni
    Internal Medicine, Ospedale Unificato Broni Stradella, Stradella PV, Italy
    Vasc Health Risk Manag 6:549-59. 2010
    ..Renin system blockade with aliskiren and another RAAS agent has been, and still is, the subject of many large-scale clinical trials and furthermore, is already available in some countries as a fixed combination...
  100. ncbi Effects of amide constituents from pepper on adipogenesis in 3T3-L1 cells
    Hailong Zhang
    Kyoto Pharmaceutical University, Misasagi, Yamashina ku, Kyoto 607 8412, Japan
    Bioorg Med Chem Lett 18:3272-7. 2008
    ....
  101. ncbi Enhancing the growth of natural eyelashes: the mechanism of bimatoprost-induced eyelash growth
    Joel L Cohen
    AboutSkin Dermatology and DermSurgery, Englewood and Lone Tree, Colorado, USA
    Dermatol Surg 36:1361-71. 2010
    ..Many women desire prominent eyelashes. In December 2008, bimatoprost ophthalmic solution 0.03% was approved for the treatment of hypotrichosis of the eyelashes in the United States...

Research Grants64

  1. MECHANISM AND CONTROL OF UREA BIOSYNTHESIS
    Frank M Raushel; Fiscal Year: 2011
    ..Cobyric acid synthetase functions to form amides from carboxylates b, d, e, and g in coenzyme B12 via a mechanism that is apparently ordered and dissociative...
  2. Lipidomic profile of endocannabinoids from neuronal cells
    VINCENT JO DAVISSON; Fiscal Year: 2010
    ..The endogenous cannabinoids are a family of lipid signaling molecules that are typically amides or esters derived from long-chain fatty acids...
  3. Chemical Probes Targeting the Protein Arginine Deiminases
    Paul R Thompson; Fiscal Year: 2013
    ..Two strategies are proposed: (i) the replacement of the backbone amides in Cl-amidine, an inhibitor developed by the PI's lab, with libraries of triazoles and tetrazoles;and (i) a ..
  4. Biosynthesis of HSAF, an antifungal natural product with a novel mode of action
    Liangcheng Du; Fiscal Year: 2009
    ..A key feature of HSAF is that it has two amides that are formed from the same amino acid (ornithine)...
  5. Synthesis and discovery of biologically active cell-permeable cyclic peptides
    R Scott Lokey; Fiscal Year: 2012
    ..in cyclic peptides is often determined by key modification - namely, N-methylation of one or more peptide amides - that help to transport the polar backbone across the hydrophobic lipid bilayer...
  6. Inhibitors of Fatty Acid Amide Hydrolase (FAAH)
    Dale L Boger; Fiscal Year: 2013
    ..The discovery and characterization of new endogenous signaling fatty acid amides and their sites of action would provide a fundamental understanding of their physiological role and new ..
  7. Role of disulfide bridges in the folding of conotoxins
    Balazs Hargittai; Fiscal Year: 2010
    ..The target peptides are a-conotoxins and their analogues;thirteen or fourteen amino acid-containing peptide amides having four cysteine residues...
  8. Total Synthesis of Bioactive Marine Natural Products
    Armen Zakarian; Fiscal Year: 2013
    ..development and application of methods for efficient asymmetric synthesis using readily available chiral lithium amides as recoverable stereodirecting reagents, 2) total synthesis of complex bioactive molecules, and 3) investigating ..
  9. Glycine N-Acyltransferases
    David J Merkler; Fiscal Year: 2013
    ..The NAGs, the lipoamino acids, and the primary fatty acid amides (PFAMs, R-CO-NH2) are members of a larger class of fatty acid amide cell signaling lipids, the fatty acid amides...
  10. New Reactions for Direct, Native Peptide Ligations
    JEFFREY WILLIAM BODE; Fiscal Year: 2010
    ..The basis for this project is the reagent-less reaction of alpha-ketoacids and N-alkylhydroxylamines to give amides via decarboxylation and dehydration...
  11. Amide Acidity Analysis of Intrinsic and Ligand-induced Flexibility and Allostery
    GRISELDA HERNANDEZ; Fiscal Year: 2012
    ..When such a prediction is impractical for the more structurally protected amides, the exchange-competent conformations will be modeled as constrained by reaction chemistry requirements and, as ..
  12. ASYMMETRIC SYNTHESIS OF BIOACTIVE PRIMARY AMINES
    FRANKLIN DAVIS; Fiscal Year: 2006
    ..sulfinimines [N-sulfinyl imines, R1S(O)N=CR2R3] and four sulfinimine-derived building blocks--beta-amino Weinreb amides, delta-amino beta-ketoesters, 3,4-dihydroisoquinolines, and 3,5-dihydro-1(2H)-isoquinolones--in new methodology ..
  13. REDOX GLYCOSIDATION
    ANTHONY BARRETT; Fiscal Year: 1992
    ..Additionally aldonic acid amides will be condensed with carbohydrate alcohols to produce aldonic thion esters...
  14. THE ROLE OF PIN1 IN MITOSIS WITH DESIGNED INHIBITORS
    FELICIA ETZKORN; Fiscal Year: 2002
    ..1, a newly discovered regulator of mitosis signal transduction, is an enzyme that acts on phosphoserine-proline amides. The unique phosphorylation dependent peptidyl-prolyl isomerase activity of Pin1 in regulating mitosis makes it a ..
  15. Development of Polydepsipeptides as Biomimetic Materials
    Laura J Suggs; Fiscal Year: 2012
    ..The peptide mimics of interest for this proposal are polydepsipeptides (PDPs), also known as polyester amides. These polymers have properties characteristic of proteins by virtue of the ability to control the chemistry of ..
  16. Studies in Amide and Peptide Synthesis
    JEFFREY NICHOLAS JOHNSTON; Fiscal Year: 2013
    ..The concise preparation of amides derived from nonnatural amino acids, common constituents of biologically active linear and cyclic peptides that ..
  17. BIOCHEMICAL TOXICOLOGY OF CARBOXYESTERASES
    Andrew Parkinson; Fiscal Year: 1992
    ..the purified carboxyesterases will be tested for their ability to hydrolyze selected carboxylic acid esters and amides. In addition, the purified carboxyesterases will be tested for their ability to hydrolyze or covalently bind ..
  18. BIOSYNTHESIS OF HUMAN PLATELET GLYCOSPHINGOLIPIDS
    CHENG TEH WANG; Fiscal Year: 1980
    ..g., amides of 1-phenyl-2-amino-1,3-propandiol. The effect of inhibitors on the platelet functions will also be determined...
  19. BIOSYNTHESIS OF OLEAMIDE AND OTHER FATTY ACID AMIDES
    DAVID MERKLER; Fiscal Year: 1999
    ..of primary fatty-acid amide messengers is illustrated by the clinical effectiveness of several primary fatty-acid amides as anxiolytics and antipsychotics...
  20. Asymmetric Synthesis of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2007
    ..a-Substituted ([unreadable]-amino Weinreb amides, prepared by addition of prochiral Weinreb amides to sulfinimines, on reaction with Grignard reagents, represent a ..
  21. Hydrophobic Polyamine Amides as Anti-Endotoxin Agents
    Sunil David; Fiscal Year: 2007
    ..The toxicity of the compounds will be systematically determined in a panel of in vitro assays. These studies will serve to generate data for anticipated IND submissions. [unreadable] [unreadable]..
  22. FATTY ACID AND PEPTIDE AMIDATION--A SHARED MECHANSIM
    Gregory Mueller; Fiscal Year: 2003
    ..Primary fatty-acid amides represent a new class of receptor-active signaling molecules whose biogenesis is unknown...
  23. High Efficiency Screening of Bioactive Lipids
    MITCHELL JOHNSON; Fiscal Year: 2009
    DESCRIPTION (provided by applicant): Fatty acid amides comprise a class of bioactive lipids that are frequently found in mammalian systems at very low concentrations. Function and metabolism are largely unknown...
  24. ALCOHOL METABOLISM--ROLE OF P450 OXYGENASES
    Minor Coon; Fiscal Year: 2000
    ..P450 oxygenases (rabbit liver microsomal isozymes 2E1 and 2E2) in the oxidative cleavage of esters and amides, with the eventual goal of finding physiologically important substrates for the reaction...
  25. Designed Inhibitors of Pin1 in Mitosis
    FELICIA ETZKORN; Fiscal Year: 2009
    Pin1 is an enzyme that catalyzes isomerization of phosphoserine/threonine-proline (pSer/Thr-Pro) amides. Pin1 is hypothesized to regulate signal transduction leading to mitosis by a conformational switch, isomerizing specific prolyl ..
  26. NEW CLASS OF ANTITUBERCULOSIS AMIDES:PRECLINICAL DEVELOP
    Leonid Heifets; Fiscal Year: 2001
    ..Introduction of improved PZA analogs should result in more rapid sterilization of Mtb in a murine model of tuberculosis and therefore potentially lead to a shorter course therapy when tested in humans...
  27. High Throughout Assay to Probe UCH-L1 Ligase Inhibitors
    Peter Lansbury; Fiscal Year: 2005
    ..degradation pathway and it is an ubiquitin C terminal hydrolase (UCH-L 1) that hydrolyzes C-terminal ester and amides of ubiquitin and is believed to play a key role in processing polyubiquitin and/or ubiquity lated proteolytic ..
  28. THE CHEMISTRY OF LITHIUM AMIDES
    David B Collum; Fiscal Year: 2013
    Lithium amides are some of the most important reagents in organic synthesis. The pharmaceutical industry uses these reagents frequently and on very large scales...
  29. Mapping the M2 Proton Channel by H/D-LC-MS
    Patrick Griffin; Fiscal Year: 2003
    ..2) The methods will then be used to map the solvent accessibility of amides and sidechains within the M2 proton channel...
  30. STUDIES OF SYNTHETIC METALLOENZYME MIMICS
    CYNTHIA BURROWS; Fiscal Year: 1991
    ..spheres are well-defined will provide information about the use of two metal ions to promote hydrolysis of amides (e.g., peptides), esters (e.g., phosphodiesters) or ureas...
  31. Trimming of Amyloid Peptides by Gamma-Secretase
    Michael S Wolfe; Fiscal Year: 2013
    ..To test this hypothesis, we will examine the ability of C-terminal amides of long A[unreadable] peptides to serve as substrates...
  32. Development of an Asymmetric Amination Process of Unactivated Olefins
    JOHN ROBBINS DEBERGH; Fiscal Year: 2012
    ..the addition of nitrile nucleophiles to 1-alkenes to form a variety of highly functionalized products, such as amides, secondary amines, and nitrogen heterocycles...
  33. METABOLISM OF ACETYLAMINOFLOURENE BY RAINBOW TROUT
    HARISH SIKKA; Fiscal Year: 1993
    ..extensively used model compounds in studies of the metabolism and mechanism of action of carcinogenic aromatic amides and amines...
  34. Asymmetric Synthesis of Nitrogen Heterocycles
    Tomislav Rovis; Fiscal Year: 2013
    ..1) develop temporary tethering strategies for [2+2+2] cycloadditions;2) Investigate the oxidative coupling of amides and alkene/alkyne ? systems to assemble piperidines by a catalyzed/oxidative protocol;3) Exploit readily available ..
  35. New Methodology for the Synthesis of Highly Functionalized Nitrogen Heterocycles
    ERIN PELKEY; Fiscal Year: 2009
    ..the nitrogen heterocycle early in the sequence and can be described as follows: (1) synthesis of pyrrole Weinreb amides followed by their two-step conversion to 3-pyrrolin-2-ones;(2) cross-coupling reactions of tetramic acid ..
  36. SXR--A TARGET FOR BREAST CANCER PREVENTION AND TREATMENT
    Bruce Blumberg; Fiscal Year: 2001
    ..However, other compounds such as phytoestrogens, fatty amides such as anandamide and retinoid X receptor (RXR) agonists have also demonstrated effectiveness against breast ..
  37. Potential sedative mechanism for Humulus lupulus L.
    CASSIA OVERK; Fiscal Year: 2006
    ..is not completely understood, recent experiments implicate a new class of signaling lipids, the fatty-acid amides (FAAs). Anandamide and oleamide are two FAAs that have been shown to induce physiological sleep in mammals...
  38. A Biocatalytic Route to Nitrile Reduction
    Dirk Iwata Reuyl; Fiscal Year: 2006
    ..and chemical industries, where they often serve as intermediates in the synthesis of commercially important acids, amides and amines...
  39. STRUCTURE-FUNCTION STUDIES ON NITRILE HYDRATASE MODELS
    PRADIP MASCHARAK; Fiscal Year: 2003
    Success in use of the enzyme nitrile hydratase (NHase) in commercial production of amides and other useful organic compounds has drawn much attention to the structure and function of this enzyme in recent years...
  40. FACTORS MODIFYING THE REACTION PROPERTIES OF HB S
    John Taylor; Fiscal Year: 1980
    ..These include treatment with substituted amides, cyanate, amino acids (e.g., phenylalanine, tryptophan, arginine) and peptides containing them (e.g...
  41. NEW METHODOLOGY FOR THE SYNTHESIS OF ANTITUMOR AGENTS
    Jeffrey Winkler; Fiscal Year: 1992
    ..the synthesis of natural products using intramolecular (2+2) photocycloadditions of dioxolenones and vinylogous amides has counterparts in the Diels-Alder reaction, cationic polyene cyclization, and arene- olefin cycloaddition...
  42. Flexibility vs Thermal Stability in Rubredoxin Proteins
    GRISELDA HERNANDEZ; Fiscal Year: 2005
    ..furiosus and Clostridium pasteurianum offer a good model system in which the amide exchange for all backbone amides can be monitored over a wide range of pH, temperature and denaturant in a fashion which distinguishes ..
  43. STRUCTURAL ANALYSIS OF PROTEIN FOLDING INTERMEDIATES
    Robert Fox; Fiscal Year: 2000
    ..Three kinetic phases are inferred. Modest protection of amides in the early refolding intermediate composed to two beta-sheets formed by local sequence interactions is observed ..
  44. CATALYZED AMIDE ISOMERIZATION: SYNTHETIC ROTAMASES
    Thomas Lectka; Fiscal Year: 2001
    ..macroporous polymers and template molecules are removed to leave beha=ind rigid cavities able to recognize amides which resemble the template in terms of shape, or more recognize amides which resemble the template in terms of ..
  45. NOVEL PEPTIDE DERIVED SWEETENERS
    Murray Goodman; Fiscal Year: 1993
    ..Stereoisomeric retro and dipeptide amides were studied by NMR and flexible geometry energy minimizations...
  46. SOLVENT EFFECTS ON AMIDE ROTATION USING 'TWISTED' AMIDES
    KATHLEEN MORGAN; Fiscal Year: 2000
    ..Several stable amides are known in which structural features partially or completely prevent the lone pair on nitrogen from delocalizing ..
  47. CATALYTIC ANTIBODIES
    Alfonso Tramontano; Fiscal Year: 1993
    ..The hydrolysis of aryl amides that are relatively reactive may be approached with suitable phosphomamidates as haptins...
  48. CHEMISTRY OF LITHIUM AMIDES
    DAVID COLLUM; Fiscal Year: 2003
    We will investigate structure-reactivity relationships in N-lithiated species by focussing upon three lithium amides: lithium 2,2,6,6-tetramethylpiperidide (LiTMP), lithium hexamethyldisilazide (LiHMDS), and lithium diisopropylamide (LDA)...
  49. NEW RHODIUM-CATALYZED ALLYLIC ALKYLATION REACTIONS
    P Evans; Fiscal Year: 2006
    ..The specific areas of interest are summarized as follows: New Allylic Amination Reactions with Cyclic Vinylogous Amides and Ureas: the development of new allylic amination reactions with vinylogous amides and ureas for the total ..
  50. CAMPTOTHECIN ANALOGS AS TUMOR INHIBITORS
    MONORE WALL; Fiscal Year: 1990
    ..as the 21-glycinate esters of 9- or 10-AC, certain water soluble esters of 9- or 10- hydroxy-1a or water soluble amides of 9- or 10 AC...
  51. MOLECULAR TOXICOLOGY OF PLACENTAL CARBOXYLESTRASE
    Bingfang Yan; Fiscal Year: 2001
    ..specificities, the recombinant enzymes will be examined for their ability to hydrolyze selected esters and amides, and their ability to catalyze the transesterification of cocaine and the synthesis of fatty acid ethyl esters...
  52. Synthesis & Evaluation of Lavendamycin Antitumor Agents
    Mohammad Behforouz; Fiscal Year: 2004
    ..Our data also indicate the importance of the C-7 amino and the C-2' amides or esters in enhancing the molecular activity...
  53. SITE-SELECTIVE SEROTONERGIC AGENTS
    RICHARD GLENNON; Fiscal Year: 1990
    ..5-HT1A antagonists), 4-alkylphenalkylamines (5-HT1C agonists and antagonists), aryloxyaminoalkyl amides (5-HT1A agonists and antagonists), and 4-alkyl 2,5-dimethoxyphenalkylamines (5-HT2 antagonists)...
  54. Role of endogenous vanilloids and cannabinoids in pain
    Kenneth Mackie; Fiscal Year: 2009
    ..been the elucidation of the biological effects of a family of lipid signalling molecules referred to as fatty acid amides. The proposed experiments focus on the characterization of N-acyldopamines, a novel group of fatty acid amides ..
  55. New C-C Bond Forming Reactions of Palladium Enolates
    ERIK ALEXANIAN; Fiscal Year: 2007
    ..coupling, which will be studied using a diverse set of substrates including alpha- haloketones, -esters, and -amides. The synthesis of an array of carbocyclic and heterocyclic architectures will be examined...
  56. Use of 2-Amido Substituted Furans for Alkaloid Synthesis
    Mickea Rose; Fiscal Year: 2006
    ..Cyclic amides are widely regarded as useful precursors for N-acyliminium ions...
  57. SYNTHESIS AND TESTING OF A NEW CLASS OF HEPARINOIDS
    Joseph Toce; Fiscal Year: 2000
    ..During the Phase I gram period we synthesized sulfated bis-disaccharide acid amides that have in vitro anticoagulant and antithrombotic activities...
  58. METAL ION CATALYSIS OF AMIDE HYDROLYSIS
    LAWRENCE SAYRE; Fiscal Year: 1990
    ..In preliminary model studies, large rate enhancements by metal ions have been observed for amides bearing aliphatic amine leaving groups...
  59. DE NOVO DESIGN OF PEPTIDE CATALYSTS
    M Ghadiri; Fiscal Year: 2002
    ..at reactions of chemical and biological importance: amide bond formation and hydrolysis of carboxylic esters and amides. The proposed research plan builds on our recent design of an efficient 33-residue synthetic peptide ligase that ..
  60. HYDROLYSIS OF AMIDE AND PEPTIDE BONDS IN PEPTIDES
    JACINTO STEINHARDT; Fiscal Year: 1980
    ..that the 12 carbon anionic detergent dodecyl sulfonate does not appreciable catalyze the hydrolysis of alkylacid amides. On the other hand it is as powerful a catalyst of amide hydrolysis in proteins containing glutamine and ..
  61. Synthetic Analogues of Cysteinate-Ligated Metalloenzymes
    Priscilla Lugo Mas; Fiscal Year: 2005
    ..of NHase in an effort to understand the mechanism of nitrile hydrolysis as well as the role that peptide amides and cysteinate sulfur ligand(s) might play in promoting function; determining whether the oxygenated sulfurs are ..
  62. MECHANISMS OF TRANSMEMBRANE SIGNALING
    LYNMARIE THOMPSON; Fiscal Year: 2005
    ..contacts in the cytoplasmic domain to elucidate the structure of receptor clusters, and measure the orientation of amides throughout the receptor to test the overall structural model (Aim 5)...
  63. Biochemical Investigations of Fatty Acid Amide Hydrolase
    MICHELE MCKINNEY; Fiscal Year: 2006
    Fatty acid amides (FAAs) represent an emerging class of lipid messengers that influence a variety of behavioral responses including pain sensation, anxiety, sleep, and feeding...
  64. PEPTIDES to Imidates and Back-Towards Bioavailibility
    Jeffery Kelly; Fiscal Year: 2003
    ..The cationic masked amides aim to take advantage of a newly discovered active transport system to mediate membrane translocation...