Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Manus Ipek"'
Autor:
Yonghan Hu, Jennifer R. Thomason, Steve Tam, Priya S. Chockalingam, Erica Reifenberg, Manus Ipek, Jason Shaoyun Xiang, Huan-Qiu Li, Richard Sheldon, Li Xing, Elisabeth A. Morris, Joshua James Sabatini, Katy E. Georgiadis, Satenig Guler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6800-6803
Design, synthesis and structure–activity relationship of a series of biphenylsulfonamido-3-methylbutanoic acid based aggrecanase-1 inhibitors are described. In addition to robust aggrecanase-1 inhibition, these compounds also exhibit potent MMP-13
Autor:
Darrell Panza, Kristine Svenson, Jason Shaoyun Xiang, Xianbin Tian, Christian E. Johnson, Xin Xu, James Tobin, Xiangping Li, Huan-Qiu Li, Mylene Perreault, Joel Bard, Tarek S. Mansour, Seung Hahm, Eddine Saiah, Ariful Qadri, Vipin Suri, Eva Chenail, Zhao-Kui Wan, Manus Ipek, Yuzhe Xing
Publikováno v:
Journal of Medicinal Chemistry. 52:5449-5461
Cortisol and the glucocorticoid receptor signaling pathway have been implicated in the development of diabetes and obesity. The reduction of cortisone to cortisol is catalyzed by 11beta-hydroxysteroid dehydrogenase type I (11beta-HSD1). 2,4-Disubsitu
Autor:
Darrin William Hopper, Elisabeth A. Morris, David Brian How, Manus Ipek, Erica Reifenberg, Phaik-Eng Sum, Matthew D. Vera, Eric Feyfant, Katy E. Georgiadis, Jerauld S. Skotnicki, Manas K. Majumdar, Jennifer R. Thomason, Qin Wang, Joshua James Sabatini, Cristin C. Keohan, Richard Sheldon, Jason Shaoyun Xiang, Yonghan Hu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2487-2491
The prevention of aggrecan (a key component of cartilage) cleavage via the inhibition of aggrecanase-1 may provide a unique opportunity to stop the progression of cartilage degradation in osteoarthritis. The evaluation of a series of biphenylsulfonam
Autor:
Bruce Follows, Steve J. Kirincich, Jinbo Lee, Douglas P. Wilson, Diane Joseph-McCarthy, David V. Erbe, James Tobin, Yan-Ling Zhang, Tam Steve Yik-Kai, Zhao-Kui Wan, Eva Binnun, Wei Li, Rajeev Hotchandani, Junjun Wu, Tarek S. Mansour, Weixin Xu, Manus Ipek, May Tam, Alessandro Moretto
Publikováno v:
ChemMedChem. 3:1525-1529
Autor:
Manus Ipek, Zhao-Kui Wan, Eva Binnun, Tarek S. Mansour, Jason Shaoyun Xiang, Seung Hahm, Xiangping Li, Huan-Qiu Li, James Tobin, Eddine Saiah, Vipin Suri, Yuzhe Xing, May Tam, Lihren Chen, John C. McKew, Jill Nunez, Xin Xu
Publikováno v:
Journal of Medicinal Chemistry. 51:4068-4071
11beta-Hydroxysteroid dehydrogenase type 1 (11beta-HSD1) is the enzyme that converts cortisone to cortisol. Evidence suggests that selective inhibition of 11beta-HSD1 could treat diabetes and metabolic syndrome. Presented herein are the synthesis, st
Autor:
Jennifer R. Thomason, Phaik-Eng Sum, Elisabeth A. Morris, Erica Reifenberg, Tam Steve Yik-Kai, Yonghan Hu, Manas K. Majumdar, Thomas S. Rush, Katy E. Georgiadis, Leila Abrous, Jason Shaoyun Xiang, Manus Ipek, Joshua James Sabatini
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:311-316
Aggrecanases are recently discovered enzymes that cleave aggrecan, a key component of cartilage. Aggrecanase inhibitors may provide a unique means to halt the progression of cartilage destruction in osteoarthritis. The synthesis and evaluation of bip
Autor:
Wei Li, Qin Wang, Jason Shaoyun Xiang, Jeremy I. Levin, Leif M. Laakso, Xuemei Du, Thomas S. Rush, Jennifer R. Thomason, Manus Ipek, Tam Steve Yik-Kai, Yonghan Hu, Jerauld S. Skotnicki, Jean Schmid, Martin J. DiGrandi, Jianchang Li
Publikováno v:
Bioorganic & Medicinal Chemistry. 13:6629-6644
Modification of alpha-biphenylsulfonamidocarboxylic acids led to potent and selective MMP-13 inhibitors. Compound 16 showed 100% oral bioavailability in rats and demonstrated50% inhibition of bovine cartilage degradation at 10 ng/mL.
Autor:
Yuzhe Xing, Walt Massefski, Manus Ipek, Ning Pan, Tam Steve Yik-Kai, Vipin Suri, Xin Xu, May Tam, James Tobin, Ying Ge, Jason Shaoyun Xiang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2865-2869
The design, synthesis, and biological evaluation of arylsulfonamidooxazoles as 11beta-HSD1 inhibitors and the serendipitous discovery of beta-keto sulfones as potent 11beta-HSD1 inhibitors are described here. These two classes of compounds are not ac
Autor:
Tarek S. Mansour, Mylene Perreault, Joel Bard, Eva Chenail, Xianbin Tian, James F. Tobin, Xiangping Li, Jason Shaoyun Xiang, Zhao-Kui Wan, Xin Xu, Manus Ipek, Darrell Panza, Kristine Svenson, Huan-Qiu Li, Eddine Saiah, Ariful Qadri, Vipin Suri, Mengmeng Wang, Christian E. Johnson, Seung Hahm
11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the conversion of inactive glucocorticoid cortisone to its active form, cortisol. The glucocorticoid receptor (GR) signaling pathway has been linked to the pathophysiology of diabetes and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac55ea3454d8d6acc241eb07df394729
https://europepmc.org/articles/PMC4027441/
https://europepmc.org/articles/PMC4027441/
Autor:
Lih-Ling Lin, Ariamala Gopalsamy, Derek C. Cole, J. Perry Hall, Manus Ipek, Rajiah Aldrin Denny, Yonghan Hu, Julie Liu, Yike Ni, Julie Lee, Jean-Baptiste Telliez, Michael Luong
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(19)
We report here the synthesis and SAR of a new series of thieno[3,2-d]pyrimidines as potent Tpl2 kinase inhibitors. The proposed binding mode suggests the potential flipped binding mode depending on the substitution. Biacore studies show evidence of b