D
David S. Weinstein
Researcher at Bristol-Myers Squibb
Publications - 61
Citations - 4453
David S. Weinstein is an academic researcher from Bristol-Myers Squibb. The author has contributed to research in topics: Signal Transduction Inhibition & Glucocorticoid receptor. The author has an hindex of 20, co-authored 60 publications receiving 4048 citations. Previous affiliations of David S. Weinstein include University of California, San Diego & Scripps Research Institute.
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Journal ArticleDOI
Assay of proteins in the presence of interfering materials.
TL;DR: The Lowry protein assay is a sensitive but highly nonspecific procedure that has been modified so that protein can be assayed in the presence of interfering chemicals.
Journal ArticleDOI
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
Stephen T. Wrobleski,Moslin Ryan M,Shuqun Lin,Yanlei Zhang,Steven H. Spergel,James Kempson,Tokarski John S,Joann Strnad,Adriana Zupa-Fernandez,Lihong Cheng,David J. Shuster,Kathleen M. Gillooly,Xiaoxia Yang,Elizabeth M. Heimrich,Kim W. McIntyre,Charu Chaudhry,Javed Khan,Max Ruzanov,Jeffrey Tredup,Dawn Mulligan,Dianlin Xie,Huadong Sun,Christine Huang,Celia D’Arienzo,Nelly Aranibar,Manoj Chiney,Anjaneya Chimalakonda,William J. Pitts,Louis J. Lombardo,Percy H. Carter,James R. Burke,David S. Weinstein +31 more
TL;DR: The late stage optimization efforts including a structure-guided design and water displacement strategy that led to the discovery of BMS-986165 as a high affinity JH2 ligand and potent allosteric inhibitor of TYK2 are reported.
Journal ArticleDOI
Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain.
James R. Burke,Lihong Cheng,Kathleen M. Gillooly,Joann Strnad,Adriana Zupa-Fernandez,Ian M. Catlett,Yifan Zhang,Elizabeth M. Heimrich,Kim W. McIntyre,Mark D. Cunningham,Julie Carman,Xiadi Zhou,Dana Banas,Charu Chaudhry,Sha Li,Celia D’Arienzo,Anjaneya Chimalakonda,Xiaoxia Yang,Jenny Xie,Jian Pang,Qihong Zhao,Shawn M. Rose,Jinwen Huang,Moslin Ryan M,Stephen T. Wrobleski,David S. Weinstein,Luisa Salter-Cid +26 more
TL;DR: BMS-986165 is a potent oral agent that similarly blocks receptor-stimulated activation of TYK2 allosterically and with high selectivity and potency afforded through optimized binding to a regulatory domain of the protein.
Journal ArticleDOI
Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain *
John S. Tokarski,Adriana Zupa-Fernandez,Jeffrey Tredup,Kristen Pike,Chiehying Chang,Dianlin Xie,Lihong Cheng,Donna L. Pedicord,Jodi K. Muckelbauer,Stephen R. Johnson,Sophie Wu,Suzanne C. Edavettal,Yang Hong,Mark R. Witmer,Lisa Elkin,Yuval Blat,William J. Pitts,David S. Weinstein,James R. Burke +18 more
TL;DR: The results support a model where the pseudokinase domain regulates activation of the catalytic domain by forming receptor-regulated inhibitory interactions, and represent a novel approach to the design of potent and selective agents for the treatment of autoimmunity.
Journal ArticleDOI
Primary induction of metallothionein by dexamethasone in cultured rat hepatocytes
TL;DR: The glucocorticoid induction of metallothionein in primary cultures of rat hepatocytes is not mediated through elevation of Zn++ uptake, and the dexamethasone stimulated increase in Zn ++ uptake is inhibited by cycloheximide.