نتایج جستجو برای: protein kinase inhibitors

تعداد نتایج: 1436831  

Journal: :Chemistry 2021

Quinoline-3-carboxamides are an essential class of drug-like small molecules that known to inhibit the phosphatidylinositol 3-kinase-related kinases (PIKK) family kinases. The quinoline nitrogen is shown bind hinge region kinases, making them competitive inhibitors adenosine triphosphate (ATP). We have previously designed and synthesized quinoline-3-carboxamides as potential ataxia telangiectas...

2010
O.B. Bekker M.G. Alekseeva D.I. Osolodkin V.A. Palyulin S.M. Elizarov N.S. Zefirov V.N. Danilenko

An efficient test system for serine/threonine protein kinase inhibitors screening has been developed based on theE. coliprotein system APHVIII/Pk25. Phosphorylation of aminoglycoside phosphotransferase VIII (APHVIII) by protein kinases enhances resistance of the bacterial cell to aminoglycoside antibiotics, e.g. kanamycin. Addition of protein kinase inhibitors prevents phosphorylation and incre...

2014
Bryan R. Lanning Landon R. Whitby Melissa M. Dix John Douhan Adam M. Gilbert Erik C. Hett Theodore O. Johnson Chris Joslyn John C. Kath Sherry Niessen Lee R. Roberts Mark E. Schnute Chu Wang Jonathan J. Hulce Baoxian Wei Laurence O. Whiteley Matthew M. Hayward Benjamin F. Cravatt

Kinases are principal components of signal transduction pathways and the focus of intense basic and drug discovery research. Irreversible inhibitors that covalently modify non-catalytic cysteines in kinase active sites have emerged as valuable probes and approved drugs. Many protein classes, however, have functional cysteines, and therefore understanding the proteome-wide selectivity of covalen...

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