Zobrazeno 1 - 10
of 100
pro vyhledávání: '"Gary L, Schieven"'
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:
Viktor Martyanov, Grace-Hyun J Kim, Wendy Hayes, Shuyan Du, Bishu J Ganguly, Oumar Sy, Sun Ku Lee, Galina S Bogatkevich, Gary L Schieven, Elena Schiopu, Roberta Gonçalves Marangoni, Jonathan Goldin, Michael L Whitfield, John Varga
Publikováno v:
PLoS ONE, Vol 12, Iss 11, p e0187580 (2017)
There are no effective treatments or validated clinical response markers in systemic sclerosis (SSc). We assessed imaging biomarkers and performed gene expression profiling in a single-arm open-label clinical trial of tyrosine kinase inhibitor dasati
Externí odkaz:
https://doaj.org/article/b49406860f2e4ce4bd0ac1f6f423b6ac
Autor:
Shana L. Posy, David A Critton, Stefan Ruepp, Ratna Kumar Sreekantha, Laxman Pasunoori, Dharmpal S. Dodd, Murali Subramanian, Andrew Watson, Percy H. Carter, Honghe Wan, Debarati Mazumder Tagore, Paul Davies, Shailesh Dudhgaonkar, Gary L. Schieven, Ratika Srivastava, Luisa Salter-Cid, Michael A. Poss, Alaric J. Dyckman, Mussari Christopher P
Publikováno v:
ACS Med Chem Lett
[Image: see text] The toll-like receptor (TLR) family is an evolutionarily conserved component of the innate immune system, responsible for the early detection of foreign or endogenous threat signals. In the context of autoimmunity, the unintended re
Autor:
Rachael Siegel, Venu Bommireddy, Paget Steven, Albert J. Uveges, Rukiye-Nazan Eraslan, Lee Pellegrino, Krista Saufler, Chia-yu Huang, Eli Mordechai, Haihua Zheng, Gary L. Schieven, Jason Trama, Michael McQueney, Miglena Prabagar, Ku Lu, Axel Metzger, Martin E. Adelson, David Diller, Grant Gallagher, Brian F. Mcguinness, Stanley P. Nawoschik, James R. Beasley
Publikováno v:
Cancer Research. 81:524-524
Introduction: Bacillus Calmette-Guerin (BCG) unresponsive non-muscle invasive bladder cancer (NMIBC) patients are in great need of effective immunotherapies. STING (Stimulator of Interferon Genes) plays a central role in mounting innate and adaptive
Autor:
Sidney Pitt, John S. Sack, Vicky Tang, William J. Pitts, Steven H. Spergel, Jonathan Lippy, Junqing Guo, Michael Galella, Mertzman Michael E, Sylwia Stachura, Steven G. Nadler, Aberra Fura, Percy H. Carter, Gary L. Schieven, Luisa Salter-Cid, Kim W. McIntyre, James Kempson, Javed Khan, Lauren Haque, Rosemary Zhang, John S. Tokarski, Guoxiang Shen, Kathleen M. Gillooly, Stephen T. Wrobleski, Joel C. Barrish
[Image: see text] The four members of the Janus family of nonreceptor tyrosine kinases play a significant role in immune function. The JAK family kinase inhibitor, tofacitinib 1, has been approved in the United States for use in rheumatoid arthritis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee1a959ab8edd802fd477e946d59e0fb
https://europepmc.org/articles/PMC6421541/
https://europepmc.org/articles/PMC6421541/
Autor:
Hong Wu, Gary L. Schieven, Joel C. Barrish, Bei Wang, Bang Chi Chen, Sam T. Chao, Gerry Everlof, Jung Hui Sun, Chunjian Liu, John H. Dodd, Murray McKinnon, Kathleen M. Gillooly, Katerina Leftheris, John Hynes, Tracy L. Taylor, Vivekananda M. Vrudhula, T. G. Murali Dhar, Stephen T. Wrobleski, Hongjian Zhang, David J. Shuster, Shuqun Lin, Kim W. McIntyre, Rulin Zhao, Christoph Gesenberg, James Lin, Punit Marathe
Publikováno v:
Journal of Medicinal Chemistry. 58:7775-7784
In search for prodrugs to address the issue of pH-dependent solubility and exposure associated with 1 (BMS-582949), a previously disclosed phase II clinical p38α MAP kinase inhibitor, a structurally novel clinical prodrug, 2 (BMS-751324), featuring
Autor:
Joel C. Barrish, Aberra Fura, Guoxiang Shen, Jingwu Duan, David S. Nirschl, Jonathan Lippy, Stephen T. Wrobleski, Rosemary Zhang, Lidia M. Doweyko, Bingwei V. Yang, Lauren Haque, Murray McKinnon, Shuqun Lin, Luisa Salter-Cid, Sidney Pitt, William J. Pitts, Percy H. Carter, John S. Sack, Gary L. Schieven, Bin Jiang, John Hynes, Gregory D. Brown, John S. Tokarski, Zhonghui Lu, Javed Khan, Steven G. Nadler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:5721-5726
A new class of Janus kinase (JAK) inhibitors was discovered using a rationally designed pyrrolo[1,2-b]pyridazine-3-carboxamide scaffold. Preliminary studies identified (R)-(2,2-dimethylcyclopentyl)amine as a preferred C4 substituent on the pyrrolopyr
Autor:
Dezhi Xing, Carolyn A. Weigelt, Luisa Salter-Cid, Pirama Nayagam Arunachalam, Rodney B.W. Smith, Ling Li, Melissa Yarde, Jodi K. Muckelbauer, Jonathan Lippy, Mary Ellen Cvijic, Sidney Pitt, John S. Sack, Thatipamula Rp, Michael A. Poss, Paul Levesque, Robert J. Cherney, Ipsit Kundu, David Marcoux, Gary L. Schieven, Arvind Mathur, Qingjie Liu, Zheming Ruan, Rosemary Zhang, R M Fancher, Shweta Padmanabhan, Scott H. Watterson, Qing Shi, Mary T. Obermeier, Anurag S. Srivastava, Anuradha Gupta, Douglas G. Batt, James Neels, Joseph A. Tino, Kevin Stefanski, Percy H. Carter, Macor John E, John Hynes, Myra Beaudoin-Bertrand, Hao Lu, Kim W. McIntyre, Stacey Skala, Aberra Fura, Lan-Ying Qin, Cornelius Lyndon A M, James Hennan, Richard Rampulla, Bogdan Sleczka, Jenny Xie, Kallem Rajareddy, Jie Pan, Christine B. Goldstine, Hua Gong, Qian Ruan, Kathleen M. Gillooly, Donna L. Pedicord, Jingsong Fan, Rajeev S. Bhide, Stefan Ruepp
Publikováno v:
Journal of medicinal chemistry. 60(12)
PI3Kδ plays an important role controlling immune cell function and has therefore been identified as a potential target for the treatment of immunological disorders. This article highlights our work toward the identification of a potent, selective, a
Autor:
Jingwu Duan, Stephen T. Wrobleski, Joel C. Barrish, Jagabandhu Das, Gary L. Schieven, Steven H. Spergel, Charu Chaudhry, Percy H. Carter, John S. Tokarski, Damaso Ovalle, John S. Sack, Aberra Fura, Zhonghui Lu, James Kempson, Luisa Salter-Cid, William J. Pitts, Junqing Guo, Yuval Blatt, John Hynes, Shuqun Lin, Hong Wu, Bin Jiang, Bingwei V. Yang, Javed Khan
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(20)
A useful and novel set of tool molecules have been identified which bind irreversibly to the JAK3 active site cysteine residue. The design was based on crystal structure information and a comparative study of several electrophilic warheads.
Autor:
Sidney Pitt, Sylwia Stachura, Rosemary Zhang, Steven G. Nadler, Kim W. McIntyre, Hong Wu, James Kempson, Jonathan Lippy, John Hynes, Joel C. Barrish, Zhonghui Lu, Percy H. Carter, Gary L. Schieven, Bin Jiang, Kate Gillooly, William J. Pitts, Javed Khan, Stephen T. Wrobleski, Jingwu Duan, Aberra Fura, Guoxiang Shen, John S. Tokarski, John S. Sack, Luisa Salter-Cid
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(14)
A series of potent dual JAK1/3 inhibitors have been developed from a moderately selective JAK3 inhibitor. Substitution at the C6 position of the pyrrolopyridazine core with aryl groups provided exceptional biochemical potency against JAK1 and JAK3 wh