Zobrazeno 1 - 10
of 86
pro vyhledávání: '"Sevgi B, Rodan"'
Autor:
W. Cameron Black, Jean-François Lévesque, Denis Riendeau, Jean-Pierre Falgueyret, Kevin P. Bateman, M. David Percival, Elise Isabel, Tammy LeRiche, Vouy Linh Truong, Jacques Yves Gauthier, Michel Therien, Robert Zamboni, Sevgi B. Rodan, Sylvie Desmarais, Christophe Mellon, Deborah A. Nicoll-Griffith, Renata Oballa, Gregg Wesolowski, Sonia Lamontagne, Carmai Seto, Nathalie Chauret, Chun Sing Li, Robert N. Young, Frédéric Massé, Wanda Cromlish, Daniel J. McKay, Le T. Duong, Cheuk K. Lau, Serge Leger, Joel Robichaud, Gideon A. Rodan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:887-892
MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat K. It is orally bioavailable and exhibits long half-life in pre-clinical species. In vivo st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04ce075aa9949065722c92768a34c9f4
https://doi.org/10.1016/j.bmcl.2009.12.083
https://doi.org/10.1016/j.bmcl.2009.12.083
Publikováno v:
Journal of Bone and Mineral Research. 1:213-220
This study compares the metabolism of [14C]-arachidonic acid between PGE2 synthesizing (ROS 17/2.8) and nonsynthesizing (ROS 25/1) osteosarcoma cell lines. In both cell lines: (a) 90% of [14C]-arachidonic acid was taken up at 24 h. (b) More than 90%
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a873f2aff9fc563e6cfcefabb673fc85
https://doi.org/10.1002/jbmr.5650010208
https://doi.org/10.1002/jbmr.5650010208
Autor:
Sevgi B Rodan, Le T. Duong
Publikováno v:
IBMS BoneKEy. 5:16-24
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c9a8aa8fd6d9edf556dcb4e8bcc517a7
https://doi.org/10.1138/20080294
https://doi.org/10.1138/20080294
Publikováno v:
Journal of Bone and Mineral Metabolism. 25:337-344
Integrins are heterodimeric adhesion receptors that mediate cell-matrix interaction. Osteoclast exhibits high expression of the alpha(v)beta(3) integrin, which binds to a variety of extracellular matrix proteins including vitronectin, osteopontin, an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::634c707c007e873c6f958f3b32645ad4
https://doi.org/10.1007/s00774-007-0773-9
https://doi.org/10.1007/s00774-007-0773-9
Autor:
Serge Leger, Denis Deschenes, Chun Sing Li, Donald B. Kimmel, M. David Percival, Michel Therien, Mary E. McGrath, Robert Zamboni, Daniel J. McKay, Sevgi B. Rodan, Gregg Wesolowski, Denis Riendeau, W. Cameron Black, Jean-Pierre Falgueyret, Sylvie Desmarais, Frédéric Massé, Jacques Yves Gauthier, Vouy-Linh Truong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1985-1989
Based on our previous study with trifluoroethylamine as a P2–P3 amide isostere of cathepsin K inhibitor, further optimization led to identification of compound 22 (L-873724) as a potent and selective non-basic cathepsin K inhibitor. This compound s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2b9a7db3c203cc3793f6b7504ed555a
https://doi.org/10.1016/j.bmcl.2005.12.071
https://doi.org/10.1016/j.bmcl.2005.12.071
Autor:
Peppi Prasit, James T. Palmer, Robert G. Strickley, M. David Percival, Liang Liu, Dan-Xiong Wang, Rohan Mendonca, Donald B. Kimmel, Leland C. Ii Burrill, Oballa Renata Marcella, Denis Riendeau, Colena Johnson, Tobee Chung, Young Robert N, Mary E. McGrath, John McCarter, Gregg Wesolowski, Michael C. Venuti, Eric B. Springman, Sevgi B. Rodan, Robert M. Rydzewski, James W. Janc, Bryant Clifford M, Z. Walter Yu, Harry Cheung, Eduardo L. Setti, Tian Zong-Qiang, Dana E. Davis, Jean-Pierre Falgueyret, Philip Enriquez, John R. Somoza, Gideon A. Rodan, Shankar Venkatraman
Publikováno v:
Journal of Medicinal Chemistry. 48:7520-7534
We have prepared a series of achiral aminoacetonitriles, bearing tri-ring benzamide moieties and an aminocyclohexanecarboxylate residue at P2. This combination of binding elements resulted in sub-250 pM, reversible, selective, and orally bioavailable
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::162e31c572aa51cc7d9a1b06687fc694
https://doi.org/10.1021/jm058198r
https://doi.org/10.1021/jm058198r
Autor:
Paul Tawa, M. David Percival, Wanda Cromlish, Kathryn E. Bass, Sylvie Desmarais, Shankar Venkatraman, Sonia Lamontagne, W. Cameron Black, Gregg Wesolowski, Jean-Pierre Falgueyret, Sevgi B. Rodan, Denis Riendeau, Christophe Mellon
Publikováno v:
Analytical Biochemistry. 335:218-227
We describe a novel diazomethylketone-containing irreversible inhibitor (BIL-DMK) which is specific for a subset of pharmaceutically important cysteine cathepsin proteases. BIL-DMK rapidly inactivates cathepsins B, F, K, L, S, and V in isolated enzym
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a84040a1008f6fba5cc76af2791ce2db
https://doi.org/10.1016/j.ab.2004.09.005
https://doi.org/10.1016/j.ab.2004.09.005
Autor:
Lorraine Lipfert, Gideon A. Rodan, John H. Hutchinson, Bradley P. Feuston, Kara Merkle, Donald B. Kimmel, Thomayant Prueksaritanont, Mark E. Duggan, Carol A. Mcvean, Chih-Tai Leu, Gregg Wesolowski, Brenda L Pennypacker, Michael A. Gentile, Ben C. Askew, Sevgi B. Rodan, Le T. Duong, Karen M. Brashear, Carmen Fernandez-Metzler, Paul J. Coleman, George D. Hartman
Publikováno v:
Journal of Medicinal Chemistry. 47:4829-4837
3-(S)-Pyrimidin-5-yl-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5e) and 3-(S)-(methylpyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5f) were identified as potent and selective antagonists of the alpha(v
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6cde893cb8bee0ba6c34ab12f6498939
https://doi.org/10.1021/jm049874c
https://doi.org/10.1021/jm049874c
Autor:
Michael J. Breslin, Sevgi B. Rodan, Gideon A. Rodan, Chih-Tai Leu, George D. Hartman, John H. Hutchinson, Le T. Duong, Hunt Cecilia, Mark E. Duggan, Paul J. Coleman, Jiabing Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1049-1052
A series of 3-substituted tetrahydro-[1,8]naphthyridine containing α v β 3 antagonists was prepared. A comparison of their in vitro IC 50 values to the electron properties of the 3-substituents revealed a good linear Hammett correlation (ρ=−1.96
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a606a99dad25be7e75818391f5a9866e
https://doi.org/10.1016/j.bmcl.2003.11.036
https://doi.org/10.1016/j.bmcl.2003.11.036
Autor:
Colena Johnson, James T. Palmer, Rohan Mendonca, Jean-Pierre Falgueyret, Renata Oballa, Gregg Wesolowski, M David Percival, Peppi Prasit, Cliff Bryant, Joël Robichaud, Eduardo South San Francisco Setti, Donald B. Kimmel, Shankar Venkatraman, Sevgi B. Rodan
Publikováno v:
Journal of Medicinal Chemistry. 46:3709-3727
A novel series of nonpeptidic biaryl compounds was identified as potent and reversible inhibitors of cathepsin K. The P2-P3 amide bond of a known amino acetonitrile dipeptide 1 was replaced with a phenyl ring, thereby giving rise to this biaryl serie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1f5c0e012974cbbf3c816d4468292a0
https://doi.org/10.1021/jm0301078
https://doi.org/10.1021/jm0301078