K
Kathleen M. Gillooly
Researcher at Bristol-Myers Squibb
Publications - 38
Citations - 2117
Kathleen M. Gillooly is an academic researcher from Bristol-Myers Squibb. The author has contributed to research in topics: Tyrosine kinase 2 & Tyrosine kinase. The author has an hindex of 23, co-authored 38 publications receiving 1718 citations.
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Journal ArticleDOI
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
Jagabandhu Das,Ping Chen,Derek J. Norris,Ramesh Padmanabha,James Lin,Robert V. Moquin,Zhongqi Shen,Lynda S. Cook,Arthur M. Doweyko,Sidney Pitt,Suhong Pang,Ding Ren Shen,Qiong Fang,Henry F. De Fex,Kim W. McIntyre,David J. Shuster,Kathleen M. Gillooly,Kamelia Behnia,Gary L. Schieven,John Wityak,Joel C. Barrish +20 more
TL;DR: Molecular modeling was used to construct a putative binding model for Lck inhibition by Dasatinib and 12m, and the framework of key hydrogen-bond interactions proposed was in agreement with the subsequent, published crystal structure of 2 bound to structurally similar Abl kinase.
Journal ArticleDOI
A highly selective inhibitor of I kappa B kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice.
Kim W. McIntyre,David J. Shuster,Kathleen M. Gillooly,Donna M. Dambach,Mark A. Pattoli,Pin Lu,Xiadi Zhou,Qiu Yuping,F. Christopher Zusi,James R. Burke +9 more
TL;DR: BMS-345541 represents the first example of an inhibitor of IKK that has antiinflammatory activity in vivo, and inhibitors of this enzyme represent a promising target for the development of novel agents to treat rheumatoid arthritis and other inflammatory diseases.
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
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.
Scott H. Watterson,George V. De Lucca,Qing Shi,Charles M. Langevine,Qingjie Liu,Douglas G. Batt,Myra Beaudoin Bertrand,Hua Gong,Jun Dai,Shiuhang Yip,Peng Li,Dawn Sun,Dauh-Rurng Wu,Chunlei Wang,Yingru Zhang,Sarah C. Traeger,Mark A. Pattoli,Stacey Skala,Lihong Cheng,Mary T. Obermeier,Rodney Vickery,Lorell Discenza,Celia D’Arienzo,Yifan Zhang,Elizabeth M. Heimrich,Kathleen M. Gillooly,Tracy L. Taylor,Claudine Pulicicchio,Kim W. McIntyre,Michael Galella,Andy J. Tebben,Jodi K. Muckelbauer,Chiehying Chang,Richard Rampulla,Arvind Mathur,Luisa Salter-Cid,Joel C. Barrish,Percy H. Carter,Aberra Fura,James R. Burke,Joseph A. Tino +40 more
TL;DR: The structure-activity relationships (SAR) leading to a novel series of highly potent and selective carbazole and tetrahydrocarbazole based, reversible inhibitors of BTK are detailed, resulting in enhanced potency and selectivity as well as a reduction in safety liabilities.