Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis
ACS Medicinal Chemistry Letters2013Vol. 4(12), pp. 1238–1243
Citations Over TimeTop 10% of 2013 papers
Philip A. Harris, Deepak Bandyopadhyay, Scott B. Berger, Nino Campobasso, Carol A. Capriotti, Julie A. Cox, Lauren Dare, Joshua N. Finger, Sandra J. Hoffman, Kirsten M. Kahler, Ruth Lehr, John D. Lich, Rakesh Nagilla, Robert T. Nolte, Michael T. Ouellette, Christina Pao, Michelle C. Schaeffer, Angela Smallwood, Helen H. Sun, Barbara A. Swift, Rachel D. Totoritis, Paris Ward, Robert W. Marquis, John Bertin, Peter J. Gough
Abstract
Potent inhibitors of RIP1 kinase from three distinct series, 1-aminoisoquinolines, pyrrolo[2,3-b]pyridines, and furo[2,3-d]pyrimidines, all of the type II class recognizing a DLG-out inactive conformation, were identified from screening of our in-house kinase focused sets. An exemplar from the furo[2,3-d]pyrimidine series showed a dose proportional response in protection from hypothermia in a mouse model of TNFα induced lethal shock.
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