Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Max, Ruzanov"'
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:
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:
Susheel J. Nara, Srinivas Jogi, Srinivas Cheruku, Sarkunam Kandhasamy, Firoz Jaipuri, Pavan Kalyan Kathi, Subba Reddy, Sanket Sarodaya, Erica M. Cook, Tao Wang, Doree Sitkoff, Karen A. Rossi, Max Ruzanov, Susan E. Kiefer, Javed A. Khan, Mian Gao, Satyanarayana Reddy, Sankara Sivaprasad LVJ, Ramola Sane, Kathy Mosure, Xiaoliang Zhuo, Gary G. Cao, Milinda Ziegler, Anthony Azzara, John Krupinski, Matthew G. Soars, Bruce A. Ellsworth, Dean A. Wacker
Publikováno v:
Journal of medicinal chemistry. 65(13)
While several farnesoid X receptor (FXR) agonists under clinical investigation for the treatment of nonalcoholic steatohepatitis (NASH) have shown beneficial effects, adverse effects such as pruritus and elevation of plasma lipids have limited their
Autor:
Jianqing Li, Daniel Smith, John S. Tokarski, Lihong Cheng, John E. Macor, Javed Khan, Adriana Zupa-Fernandez, Anil Thankappan, Chunjian Liu, Charu Chaudhry, David S. Weinstein, Percy H. Carter, Kathleen M. Gillooly, Kim W. McIntyre, Yifan Zhang, Anjaneya Chimalakonda, Joann Strnad, James Lin, James R. Burke, David J. Shuster, Manoj Chiney, Paul A. Elzinga, Max Ruzanov, Louis J. Lombardo, Charles M. Langevine
Publikováno v:
Journal of Medicinal Chemistry. 64:677-694
A search for structurally diversified Tyk2 JH2 ligands from 6 (BMS-986165), a pyridazine carboxamide-derived Tyk2 JH2 ligand as a clinical Tyk2 inhibitor currently in late development for the treatment of psoriasis, began with a survey of six-membere
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:
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(4)
The identification of agonists of the stimulator of interferon genes (STING) pathway has been an area of intense research due to their potential to enhance innate immune response and tumor immunogenicity in the context of immuno-oncology therapy. Ini
Autor:
Jennifer Brown, Karen E. Parrish, Andrew J. Tebben, Jonathan Lippy, Kamalavenkatesh Palanisamy, Todd Kinsella, Chetan Padmakar Darne, Vinay K. Holenarsipur, Anwar Murtaza, Muthalagu Vetrichelvan, Chunhong Yan, Karen Augustine-Rauch, Max Ruzanov, Mark Fereshteh, Upender Velaparthi, Gopal Dhar, Gregory D. Vite, Peiying Liu, Steven Sheriff, Jayakumar Sankara Warrier, Aravind Anandam, Marina Gelman, Arvind Mathur, Barri Wautlet, Robert M. Borzilleri, Hasibur Rahaman, Zheng Yang, Anuradha Gupta, Arun Kumar Gupta, Rajinder Singh, Joseph Fargnoli, Jesse Swanson
Publikováno v:
ACS Med Chem Lett
[Image: see text] Novel imidazole-based TGFβR1 inhibitors were identified and optimized for potency, selectivity, and pharmacokinetic and physicochemical characteristics. Herein, we report the discovery, optimization, and evaluation of a potent, sel
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:
Ilya V. Likhachev, Robert Karisch, Roni D. Gordon, Benjamin G. Neel, Max Ruzanov, Andres Lin, Evgeniy V. Brazhnikov, Kevin P. Battaile, Vladimir Romanov, Nikolay K. Balabaev, Nickolay Y. Chirgadze, Yuri N. Chirgadze, Robert Lam, Emil F. Pai
Publikováno v:
Journal of biomolecular structuredynamics. 40(24)
Protein tyrosine phosphatases constitute a family of cytosolic and receptor-like signal transducing enzymes that catalyze the hydrolysis of phospho-tyrosine residues of phosphorylated proteins. PTP1B, encoded by
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