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ARTICLE | Preclinical News

Paper: GRK2 inhibitors could treat heart failure

July 20, 2017 12:36 AM UTC

In a paper published in the Journal of Medicinal Chemistry, researchers with Takeda Pharmaceutical Co. Ltd. (Tokyo:4502) described a new class of small molecule G protein-coupled receptor kinase 2 (GRK2; GPRK2) inhibitors that could help treat heart failure.

Previous studies had shown reduced GRK2 activity improved outcomes in mouse models of heart failure. Using high-throughput screening, Takeda identified inhibitors of GRK2 kinase activity, then produced a lead compound that bound to GRK2 and the closely related GRK3, but no other GRK family members...