Zobrazeno 1 - 10
of 31
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f0dd100bce7c69b23761dd3867587af
https://doi.org/10.1016/j.bmcl.2007.09.058
https://doi.org/10.1016/j.bmcl.2007.09.058
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dcab39529ea123f4382bed76ef1b6068
https://doi.org/10.1016/j.bmcl.2007.07.101
https://doi.org/10.1016/j.bmcl.2007.07.101
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)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa3d177beeb1725aa51e250b5f8f869a
https://doi.org/10.1021/jm060077j
https://doi.org/10.1021/jm060077j
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f89c51cec1e810d8d01e118806d62ae9
https://doi.org/10.1021/jm051099t
https://doi.org/10.1021/jm051099t
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::78f56ad19fec0b970200e58a9a29521e
https://doi.org/10.1016/j.bmcl.2005.06.091
https://doi.org/10.1016/j.bmcl.2005.06.091
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::604dd37478ea992e97a95f15b44ebddf
https://doi.org/10.1016/j.coph.2003.06.003
https://doi.org/10.1016/j.coph.2003.06.003
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62f2dace220e69db7498c481bea96681
https://doi.org/10.1016/s0960-894x(00)00149-9
https://doi.org/10.1016/s0960-894x(00)00149-9
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e072333b45fd50bb0d75fe45a93f76db
https://doi.org/10.1016/s0960-894x(00)00105-0
https://doi.org/10.1016/s0960-894x(00)00105-0
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b91e1934325ea4b3218d31a6b618f98a
https://doi.org/10.1016/s0960-894x(99)00417-5
https://doi.org/10.1016/s0960-894x(99)00417-5
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38f813f44cdc0c9a18a55cd7f0e39c7b
https://doi.org/10.1016/s0960-894x(99)00102-x
https://doi.org/10.1016/s0960-894x(99)00102-x