Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Huey S. Shieh"'
Autor:
Michael David Rogers, Jeffery N. Carroll, Mark A. Massa, Jeffrey Hitchcock, Peter G. Ruminski, Michelle A. Schmidt, Bruce C. Hamper, Strohbach Joseph Walter, Huey S. Shieh, Laurence O. Whiteley, Katherine E. Palmquist, Joe T. Collins, Grace E. Munie, Hanau Cathleen E, H. Peter Kleine, Mark E. Schnute, T. Sunyer, Nicole Caspers, John E. Baldus, Theresa R. Fletcher, Joseph J. McDonald, Silvia Portolan, Jeffrey A. Scholten, Dean Messing, Margaret L. Grapperhaus, Brandon Collins
Publikováno v:
Journal of Medicinal Chemistry. 59:313-327
Matrix metalloproteinase-13 (MMP-13) is a zinc-dependent protease responsible for the cleavage of type II collagen, the major structural protein of articular cartilage. Degradation of this cartilage matrix leads to the development of osteoarthritis.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b1bf588f2b187240a5d8f4d5ee2e305b
https://doi.org/10.1021/acs.jmedchem.5b01434
https://doi.org/10.1021/acs.jmedchem.5b01434
Autor:
Li Xing, Devadas Balekudru, Jerry Z. Yang, Michael Mao, Elizabeth G. Webb, Joseph B. Monahan, Gary D. Anderson, Brian Samas, Dean Messing, Huey S. Shieh, John K. Walker, Rajesh V. Devraj, Shaun R. Selness
Publikováno v:
ChemMedChem. 7:273-280
PH-797804 ((aS)-3-{3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl}-N,4-dimethylbenzamde) is a diarylpyridinone inhibitor of p38 mitogen-activated protein (MAP) kinase derived from a racemic mixture as the more potent atropisomer (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5687de363aa7e63f5520098e7c45c8b
https://doi.org/10.1002/cmdc.201100439
https://doi.org/10.1002/cmdc.201100439
Autor:
Dean Messing, Brian S. Hickory, Alan G. Benson, Matthew J. Saabye, Jeff Hitchcock, Heather M. Madsen, Devadas Balekudru, Shaun R. Selness, Richard C. Durley, Laura D. Marrufo, Gary D. Anderson, Li Xing, Kevin D. Jerome, Michael Hepperle, Christie Lance Christopher, Rajesh V. Devraj, Elizabeth G. Webb, Thomas Owen, Ravi G. Kurumbail, Edgardo Alvira, Jeffrey L. Hirsch, Joseph B. Monahan, Paul V. Rucker, Boehm Terri L, Blevis-Bal Radhika M, Huey S. Shieh, John K. Walker, John F. Schindler, Michele A. Promo, Win Naing, Sheri L. Bonar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4059-4065
A series of N-aryl pyridinone inhibitors of p38 mitogen activated protein (MAP) kinase were designed and prepared based on the screening hit SC-25028 (1) and structural comparisons to VX-745 (5). The focus of the investigation targeted the dependence
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b57328f6e5ea96fc972d684f2e92281c
https://doi.org/10.1016/j.bmcl.2011.04.120
https://doi.org/10.1016/j.bmcl.2011.04.120
Autor:
Dean Messing, Win Naing, Joseph P. Portanova, Tina Kim, Alan G. Benson, Shaun R. Selness, Daniel L. Flynn, Joseph B. Monahan, Richard Lindmark, Huey S. Shieh, John K. Walker, Syaulan Yang, Ravi Kurambail, Rajesh V. Devraj, Michael Hepperle, Dice Tom
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2634-2638
Starting from an initial HTS screening lead, a novel series of C(5)-substituted diaryl pyrazoles were developed that showed potent inhibition of p38alpha kinase. Key to this outcome was the switch from a pyridyl to pyrimidine at the C(4)-position lea
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c566e95d1288f02e436717a89b88f0f9
https://doi.org/10.1016/j.bmcl.2010.02.047
https://doi.org/10.1016/j.bmcl.2010.02.047
Autor:
Jeffrey L. Hirsch, Robert H. Keith, Loreen Stillwell, Pamela De Ciechi, Jian Zhang, Ravi G. Kurumbail, Richard M. Leimgruber, Shaun R. Selness, Huey S. Shieh, Stephen J. Mnich, Yan Zhang, Barry L. Burnette, Michael Hepperle, Robert P. Compton, Raj Devraj, Gail Jungbluth, Win Naing, Joseph B. Monahan, Joseph Portanova, Gary D. Anderson, Heidi R. Hope
Publikováno v:
Pharmacology. 84:42-60
SD0006 is a diarylpyrazole that was prepared as an inhibitor of p38 kinase-alpha (p38alpha). In vitro, SD0006 was selective for p38alpha kinase over 50 other kinases screened (including p38gamma and p38delta with modest selectivity over p38beta). Cry
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::417af8711e84292fd44a13daf8ddc013
https://doi.org/10.1159/000227286
https://doi.org/10.1159/000227286
Autor:
Huey S. Shieh, John J. Likos, Gary A. De Crescenzo, William C. Stallings, Dean Welsch, Yiqing Feng, Leiming Zhu, Anna M. Stevens, Grace E. Munie, Joseph J. McDonald, Harold Woodward, Carol Pearcy Howard
Publikováno v:
Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics. 1598:10-23
MMP-2 is a member of the matrix metalloproteinase family that has been implicated in tumor cell metastasis and angiogenesis. Here, we describe the solution structure of a catalytic domain of MMP-2 complexed with a hydroxamic acid inhibitor (SC-74020)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::013dd0950a2875164a51575f576376b7
https://doi.org/10.1016/s0167-4838(02)00307-2
https://doi.org/10.1016/s0167-4838(02)00307-2
Autor:
Rajesh V. Devraj, Heather M. Madsen, Heidi M. Morgan, Laura D. Marrufo, Gary D. Anderson, Shaun R. Selness, Dean Messing, Elizabeth G. Webb, Joseph B. Monahan, Jian Zhang, Devadas Balekudru, Jerry Z. Yang, Huey S. Shieh, Li Xing
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(13)
A novel series of highly potent and selective p38 MAP kinase inhibitors was developed originating from a substituted N-aryl-6-pyrimidinone scaffold. SAR studies coupled with in vivo evaluations in rat arthritis model culminated in the identification
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c50bfd334c3732636cf4d80aaa2300c
https://pubmed.ncbi.nlm.nih.gov/21620699
https://pubmed.ncbi.nlm.nih.gov/21620699
Autor:
Brandon Collins, W. Howard Roark, Katherine E. Palmquist, Grace E. Munie, Mark E. Schnute, Olga V. Nemirovskiy, Patrick Michael Ann Arbor La Ann Arbor O'brien, Jeffrey A. Scholten, Karl W. Aston, Jeffery N. Carroll, Lillian E. Vickery, T. Sunyer, Steven L. Settle, Joe Nahra, Hanau Cathleen E, Bruce C. Hamper, Peter G. Ruminski, Patt William Chester, Jeffrey Hitchcock, Mark Morris, Huey S. Shieh, Theresa R. Fletcher, Chiu-Fai Man, Joseph J. McDonald, Adam R. Johnson, Michael David Rogers, Arthur J. Wittwer, Alexander Pavlovsky, Richard D. Dyer, Arun Agawal
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(2)
Potent, highly selective and orally-bioavailable MMP-13 inhibitors have been identified based upon a (pyridin-4-yl)-2H-tetrazole scaffold. Co-crystal structure analysis revealed that the inhibitors bind at the S(1)(') active site pocket and are not l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7d21a6adaf1297782797ee424c48361
https://pubmed.ncbi.nlm.nih.gov/20005097
https://pubmed.ncbi.nlm.nih.gov/20005097
Publikováno v:
Current pharmaceutical design. 15(20)
The a disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS) family of metalloproteases consists of 19 members. These enzymes play an important role in the turnover of extracellular matrix proteins in various tissues and their altered
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc3fa2ad1eeec8083997735786511aab
https://pubmed.ncbi.nlm.nih.gov/19601837
https://pubmed.ncbi.nlm.nih.gov/19601837
Autor:
Jennifer M. Williams, Li Xing, Ravi G. Kurumbail, Devadas Balekudru, Jeffrey L. Hirsch, Alan G. Benson, Heidi R. Hope, Roderick A. Stegeman, Zara Walden, Joseph B. Monahan, Shaun R. Selness, Rajesh V. Devraj, Richard M. Broadus, Huey S. Shieh, John K. Walker, Robert P. Compton, John F. Schindler
Publikováno v:
Biochemistry. 48(27)
PH-797804 is a diarylpyridinone inhibitor of p38alpha mitogen-activated protein (MAP) kinase derived from a racemic mixture as the more potent atropisomer (aS), first proposed by molecular modeling and subsequently confirmed by experiments. On the ba
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2167645ed381b042a0fce22befe0bfe1
https://pubmed.ncbi.nlm.nih.gov/19496616
https://pubmed.ncbi.nlm.nih.gov/19496616