Zobrazeno 1 - 10
of 91
pro vyhledávání: '"John S, Sack"'
Autor:
Emily C. Cherney, Liping Zhang, Julian Lo, Tram Huynh, Donna Wei, Vijay Ahuja, Claude Quesnelle, Gary L. Schieven, Alan Futran, Gregory A. Locke, Zeyu Lin, Laura Monereau, Charu Chaudhry, Jordan Blum, Sha Li, Mark Fereshteh, Bifang Li-Wang, Sanjeev Gangwar, Chin Pan, Colin Chong, Xiao Zhu, Shana L. Posy, John S. Sack, Ping Zhang, Max Ruzanov, Mary Harner, Fahad Akhtar, Gretchen M. Schroeder, Gregory Vite, Brian Fink
Publikováno v:
Journal of Medicinal Chemistry. 65:3518-3538
Autor:
Chunhong, Yan, John S, Sack
Publikováno v:
Acta Crystallogr F Struct Biol Commun
The X-ray crystal structure of a human cardiac muscle troponin C/troponin I chimera has been determined in two different crystal forms and shows a conformation of the complex that differs from that previously observed by NMR. The chimera consists of
Autor:
Aberra Fura, Shiuhang Yip, Georgia Cornelius, Hai-Yun Xiao, Qingjie Liu, Sha Li, Ning Li, Nicholas A. Meanwell, Shailesh Dudhgaonkar, Max Ruzanov, Jenny Xie, Zili Xiao, Purnima Khandelwal, Carolyn A. Weigelt, David J. Shuster, Dauh-Rurng Wu, T. G. Murali Dhar, Tara Sherry, Yang Michael G, Kevin Stefanski, Jignesh Nagar, Rex Denton, Qihong Zhao, Peng Li, Silvi A. Chacko, Arun Govindarajan, Robert M. Borzilleri, John S. Sack, Yeheng Zhu, Yunling Song, Dawn Sun, Anjuman Rudra, Mary T. Obermeier, Jinhong Wang, Douglas G. Batt, Venkata Murali
Publikováno v:
ACS Med Chem Lett
[Image: see text] Structure–activity relationship studies directed toward the replacement of the fused phenyl ring of the lead hexahydrobenzoindole RORγt inverse agonist series represented by 1 with heterocyclic moieties led to the identification
Autor:
Tara Sherry, John E. Macor, Jinhong Wang, Georgia Cornelius, Shiuhang Yip, Luisa Salter-Cid, Qingjie Liu, Purnima Khandelwal, Carolyn A. Weigelt, Max Ruzanov, John S. Sack, Kevin Stefanski, Jenny Xie, T. G. Murali Dhar, Sha Li, Melissa Yarde, Joseph A. Tino, Qihong Zhao, Dauh-Rurng Wu, Mary T. Obermeier, David J. Shuster, Aberra Fura, Douglas G. Batt, Rex Denton
Publikováno v:
ACS Med Chem Lett
[Image: see text] Employing a virtual screening approach, we identified the pyroglutamide moiety as a nonacid replacement for the cyclohexanecarboxylic acid group which, when coupled to our previously reported conformationally locked tricyclic core,
Autor:
Joel C. Barrish, John Hynes, Ajay Saxena, Natesan Murugesan, Dianlin Xie, Anjaneya Chimalakonda, Stefan Ruepp, Mitalee Das, Richard Rampulla, Durgarao Kantheti, Chunhong Yan, Julie Carman, Jignesh Nagar, Siva Subramani, Qian Ruan, William J. Pitts, Rajeev S. Bhide, Paul A. Elzinga, Venkatram Reddy Paidi, John S. Sack, Mark Fereshteh, Thangavel Soodamani, Amrita Jha Mukherjee, T. Thanga Mariappan, Ramesh Kumar Sistla, Kaushik Ghosh, Debarati Mazumder, Kamalavenkatesh Palanisamy, Deborah A. Holloway, Susan E. Kiefer, John A. Newitt, Satheesh Kesavan Nair, Polimera Subba Rao, Shailesh Dudhgoankar, Percy H. Carter, Xin Li, Srinivas Maddi, S. Pon Saravanakumar, Sreekantha Ratna Kumar, Sucharita Bose
Publikováno v:
ACS Med Chem Lett
[Image: see text] IRAK4 is an attractive therapeutic target for the treatment of inflammatory conditions. Structure guided optimization of a nicotinamide series of inhibitors has been expanded to explore the IRAK4 front pocket. This has resulted in t
Autor:
Carolyn A. Weigelt, Sha Li, David Marcoux, Georgia Cornelius, Qihong Zhao, Mary Ellen Cvijic, John E. Macor, Jingwu Duan, Melissa Yarde, Muthalagu Vetrichelvan, David J. Shuster, Qingjie Liu, Richard Rampulla, Kim W. McIntyre, Mary T. Obermeier, Shiuhang Yip, Purnima Khandelwal, Sureshbabu Vishwakrishnan, Anuradha Gupta, Virna Borowski, Peng Li, Kevin Stefanski, Sridharan Ramlingam, Myra Beaudoin-Bertrand, Nageswara Maddala, Sridhar Vanteru, Percy H. Carter, Arvind Mathur, Aberra Fura, Max Ruzanov, John Hynes, Dauh-Rurng Wu, Jinhong Wang, Luisa Salter-Cid, John S. Sack, Cornelius Lyndon A M, Anurag S. Srivastava, Robert J. Cherney, Kumaravel Selvakumar, Mushkin Basha, Arun Kumar Gupta, Douglas G. Batt, Rex Denton, Sukhen Karmakar, Qing Shi, Ananta Karmakar, Naveen Manjunath, Javed Khan, Jenny Xie, Joseph A. Tino, T. G. Murali Dhar
Publikováno v:
Journal of Medicinal Chemistry. 62:9931-9946
RORγt is an important nuclear receptor that regulates the production of several pro-inflammatory cytokines such as IL-17 and IL-22. As a result, RORγt has been identified as a potential target for the treatment of various immunological disorders su
Autor:
Zhonghui Lu, James J.-W. Duan, Haiyun Xiao, James Neels, Dauh-Rurng Wu, Carolyn A. Weigelt, John S. Sack, Javed Khan, Max Ruzanov, Yongmi An, Melissa Yarde, Ananta Karmakar, Sureshbabu Vishwakrishnan, Venkata Baratam, Harisha Shankarappa, Sridhar Vanteru, Venkatesh Babu, Mushkin Basha, Arun Kumar Gupta, Selvakumar Kumaravel, Arvind Mathur, Qihong Zhao, Luisa M. Salter-Cid, Percy H. Carter, T.G. Murali Dhar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:2265-2269
An X-ray crystal structure of one of our previously discovered RORγt inverse agonists bound to the RORγt ligand binding domain revealed that the cyclohexane carboxylic acid group of compound 2 plays a significant role in RORγt binding, forming fou
Autor:
Doree F. Sitkoff, Alice Y. Chen, Hongwei Zhang, Anne Rose, Xue-Qing Chen, Cailan Wang, Leonard P. Adam, Mimi L. Quan, Nathan L. Cheadle, Zilun Hu, Lisa Zhang, David S. Taylor, Ruth R. Wexler, Songmei Xu, John S. Sack, Joseph E. Myers, Victor R. Guarino, James Hennan, Peter W. Glunz, Chunhong Yan, Julia Li
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(21)
Structure-activity relationship optimization on a series of phenylpyrazole amides led to the identification of a dual ROCK1 and ROCK2 inhibitor (25) which demonstrated good potency, kinome selectivity and favorable pharmacokinetic profiles. Compound
Autor:
Bin Jiang, Sylwia Stachura, T. G. Murali Dhar, Carolyn A. Weigelt, Dauh Rurng Wu, Jingwu Duan, Luisa M. Salter–Cid, Javed Khan, Ding Ren Shen, Melissa Yarde, Qihong Zhao, Zhonghui Lu, Percy H. Carter, John S. Sack, Max Ruzanov
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(19)
In an effort to discover oral inverse agonists of RORγt to treat inflammatory diseases, a new 2,6–difluorobenzyl ether series of cyclopentyl sulfones were found to be surprisingly more potent than the corresponding alcohol derivatives. When combin
Autor:
Yanling Huang, Jingwu Duan, Carolyn A. Weigelt, Cullen L. Cavallaro, Javed Khan, Brian E. Fink, Muthoni G. Kamau, Zheming Ruan, Lan-Ying Qin, Sylwia Stachura, Cliff Chen, Murali Gururajan, Lalgudi S. Harikrishnan, Tram N. Huynh, John S. Sack, Anwar Murtaza, Daniel O'malley, Zhuyin Li, Melissa Yarde, Max Ruzanov, Virna Borowski, Patrice Gill, Huadong Sun, Zhonghui Lu, Jessica J. Wong
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(12)
Substituted benzyloxy aryl compound 2 was identified as an RORγt agonist. Structure based drug design efforts resulted in a potent and selective tricyclic compound 19 which, when administered orally in an MC38 mouse tumor model, demonstrated a desir