Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Susan Y. Tamura"'
Autor:
Huong T. Dang, Philip J. Skinner, Graeme Semple, Martin C. Cherrier, Peter J. Webb, Ruoping Chen, Susan Y. Tamura, Carleton R. Sage, Daniel T. Connolly, Cameron Pride, Jeremy G. Richman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6619-6622
A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high
Autor:
Philip J. Skinner, Tawfik Gharbaoui, Vu Hong, Ruoping Chen, Graeme Semple, Huong T. Dang, Martin C. Cherrier, Jeremy G. Richman, Young-Jun Shin, Cameron Pride, Peter J. Webb, Andrew K. Lindstrom, Daniel T. Connolly, Susan Y. Tamura
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5620-5623
A series of 5-alkyl pyrazole-3-carboxylic acids were prepared and found to act as potent and selective agonists of the human GPCR, GPR109a, the high affinity nicotinic acid receptor. No activity was observed at the highly homologous low affinity niac
Autor:
Odile E. Levy, Susan Y. Tamura, Andrew Prongay, Robert Chase, Sumei Ruan, Rong Liu, Bahige Baroudy, Paul Ingravallo, Kemp Scott Jeffrey, Viyyoor Girijavallabhan, Kevin Chen, John Pichardo, Bennett Frank, Tony Y. Hsieh, F. George Njoroge, Weidong Pan, Raymond G. Lovey, Kuo-Chi Cheng, Ashok Arasappan, Edwin Jao, Lim-Wilby Marguerita, Jean-Marc Brisson, Tajel Parekh, Russel E. Pike, Srikanth Venkatraman, Stephane L. Bogen, Sony Agrawal, Yi-Tsung Liu, Anil K. Saksena
Publikováno v:
Journal of Medicinal Chemistry. 49:2750-2757
Introduction of various modified prolines at P(2) and optimization of the P(1) side chain led to the discovery of SCH6 (24, Table 2), a potent ketoamide inhibitor of the HCV NS3 serine protease. In addition to excellent enzyme potency (K(i)*= 3.8 nM)
Autor:
Peter J. Webb, Martin C. Cherrier, Graeme Semple, Carleton R. Sage, Philip J. Skinner, Jeremy G. Richman, Ruoping Chen, Susan Y. Tamura, Daniel T. Connolly
Publikováno v:
Journal of Medicinal Chemistry. 49:1227-1230
1-Substituted benzotriazole carboxylic acids have been identified as the first reported examples of selective small-molecule agonists of the human orphan G-protein-coupled receptor GPR109b (HM74), a low-affinity receptor for the HDL-raising drug niac
Autor:
Levy Odile Esther, B. Marten, Ashit K. Ganguly, Andrew Prongay, Patrick Pinto, Bruce A. Malcolm, Tin-Yau Chan, Parekh Tejal N, Santhanam Bama, Lim-Wilby Marguerita, Z. Zhu, Vincent Madison, Liwu Hong, Ashok Arasappan, Edwin Jao, Stephane L. Bogen, Hongwu Wang, Kemp Scott Jeffrey, F. G. Njoroge, Srikanth Venkatraman, Nanhua Yao, Kevin X. Chen, Nancy Butkiewicz, Mckittrick Brian A, John Pichardo, Henry M. Vaccaro, Liu Yi-Tsung, V. Girijavallabhan, Anil K. Saksena, Raymond G. Lovey, Richard N. Ingram, Haining Gu, Russell E. Pike, Frank Bennett, Xiaozheng Yang, Susan Y. Tamura
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4180-4184
We have discovered that introduction of appropriate amino acid derivatives at P 2 ′ position improved the binding potency of P3-capped α-ketoamide inhibitors of HCV NS3 serine protease. X-ray crystal structure of one of the inhibitors (43) bound t
Publikováno v:
Current Opinion in Pharmacology. 3:530-543
Recent advances in the development of potent and selective peptide and non-peptide ligands for peptidergic receptors are anticipated to help further unravel the roles of class I and II G-protein-coupled receptors in the pathogenesis of human diseases
Autor:
Susanne M Anderson, Michael G Ma, Michael I. Weinhouse, Erick A. Goldman, Vernon T Bernardino, Christopher A Roberts, Cheryl R. Cohen, Kevin Masukawa, Thomas G. Nolan, Terence K. Brunck, Susan Y. Tamura, Steven A Dixon, Annette E Bradbury
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:983-987
Solid- and solution-phase synthesis of peptidomimetic inhibitors of urokinase-type plasminogen activator based on the sequence dSerAlaArg-al are described. The biological activities of these unique inhibitors are reported herein. Carbonate prodrugs w
Autor:
Cheryl R. Cohen, Susan Y. Tamura, Terence K. Brunck, John Reiner, Odile E. Levy, Ruth F. Nutt, Erick A. Goldman, Jonathan Z. Ho, J. Edward Semple, Peter W. Bergum, Theresa H. Uong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:745-749
A novel series of rigid P3-guanylpiperidine peptide mimics 3-14 was designed as potential factor Xa and prothrombinase inhibitors. Incorporation into a P2-gly-P1-argininal motif led to highly potent and selective inhibitors. The synthesis and biologi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2573-2578
Rigid benzolactam P3-P2 dipeptide mimics were designed and prepared as potential inhibitors of blood coagulation factor Xa. Methoxy substitution of the tetrahydrobenzazepinone scaffold led to potent and selective inhibitors. The synthesis and biologi
Autor:
Matthew A. Abelman, Erick A. Goldman, J. Edward Semple, Theresa Ha-Uong, Margeurita S. Lim-Wilby, Terence K. Brunck, Susan Y. Tamura, John Reiner, Ruth F. Nutt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:895-900
A novel scaffold for P4-P2 dipeptide mimics containing a rigid pyridone spacer was designed based on a virtual library strategy. Several selected nonpeptidic 4-aralkyl or 4-alkylpyridones incorporating a P1-argininal sequence were prepared. The model