Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Jason Shaoyun Xiang"'
Autor:
Jason Shaoyun Xiang, Xiaobing Deng, Qingqing Zhou, Youzi Tong, Yang He, Liandong Ma, Chunyun Chen, Qianxiang Zhou, Karl Zhou, Jie Chen, Luhua Lai
Publikováno v:
Cancer Research. 79:3861-3861
Reactivation of androgen receptor (AR) plays a key role in prostate cancer growth, especially in castration-resistant prostate cancer (CRPC) progression. Accumulated data have demonstrated that the AR reactivation is resulted from AR amplification, A
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:
Jason Shaoyun Xiang, Jianyao Wang, Seung Hahm, Louis Leung, Nicole Houvig, Mengmeng Wang, Eddine Saiah, Xin Xu, Vipin Suri, Xianbin Tian
Publikováno v:
Drug Metabolism Letters. 5:55-63
Diet-induced obese (DIO) mice have been commonly used as an animal model in the efficacy assessment for new drug candidates. Although high-fat feeding has been reported to cause profound physiological changes, including the expression of drug-metabol
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:
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:
Xuemei Du, Thomas S. Rush, Tam Steve Yik-Kai, Yonghan Hu, Dianne DeVincentis, Jennifer R. Thomason, Kristina Cunningham, Jason Shaoyun Xiang, Jeremy I. Levin, Jianchang Li, Elisabeth A. Morris, Wei Li, Jerauld S. Skotnicki, Priya S. Chockalingam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4961-4966
The structure-based design and synthesis of a series of novel biphenyl sulfonamide carboxylic acids as potent MMP-13 inhibitors with selectivity over MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-14, Aggrecanase 1, and TACE are described.
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