Journal of medicinal chemistryHumansAnimalsStructure-Activity RelationshipInflammationProtein Kinase Inhibitors
Discovery of Clinical Candidate GDC-8264, a Novel, Potent and Selective RIP1 Inhibitor for Amelioration of Tissue Damage and the Treatment of Inflammatory Diseases.
Snahel Patel, Huifen Chen, Eugene Varfolomeev, Youngsu Kwon, Sreemathy Ramaswamy, Pawan Bir Kohli, John G Quinn, Joshua D Webster, Jialin Mao, Yuan Chen, Rina Fong, F Esra Demircioglu, Patrick Lupardus, Craig Stivala, Gregory L Hamilton
Published: 202510.1021/acs.jmedchem.5c01891
Abstract
Receptor-interacting protein 1 (RIP1) is a critical regulator of inflammatory cell death induced by diverse stimuli including TNF family ligands and ischemic injury. As such, the inhibition of RIP1 with small molecule kinase inhibitors is predicted t…
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