An article Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors WOS:000503114700006 published article about FAILURE; POTENT; PATHOPHYSIOLOGY; PAROXETINE; PREVENTS; GRKS in [Rowlands, Rachel A.; Waldschmidt, Helen V.; Larsen, Scott D.; White, Andrew D.] Univ Michigan, Vahlteich Med Chem Core, Coll Pharm, 428 Church St, Ann Arbor, MI 48109 USA; [Cato, M. Claire; Bouley, Renee A.] Univ Michigan, Life Sci Inst, Dept Pharmacol, 210 Washtenaw Ave, Ann Arbor, MI 48109 USA; [Cato, M. Claire; Bouley, Renee A.] Univ Michigan, Dept Biol Chem, 210 Washtenaw Ave, Ann Arbor, MI 48109 USA; [Chen, Qiuyan; Avramova, Larisa; Tesmer, John J. G.] Purdue Univ, Dept Biol Sci, 915 W State St, W Lafayette, IN 47907 USA; [Chen, Qiuyan; Avramova, Larisa; Tesmer, John J. G.] Purdue Univ, Dept Med Chem, 915 W State St, W Lafayette, IN 47907 USA; [Chen, Qiuyan; Avramova, Larisa; Tesmer, John J. G.] Purdue Univ, Dept Mol Pharmacol, 915 W State St, W Lafayette, IN 47907 USA in 2019, Cited 38. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Computed Properties of C7H8N2O
The ability of G protein-coupled receptor (GPCR) kinases (GRKs) to regulate desensitization of GPCRs has made GRK2 and GRK5 attractive targets for treating heart failure and other diseases such as cancer. Although advances have been made toward developing inhibitors that are selective for GRK2, there have been far fewer reports of GRK5 selective compounds. Herein, we describe the development of GRK5 subfamily selective inhibitors, 5 and 16d that covalently interact with a nonconserved cysteine (Cys474) unique to this subfamily. Compounds 5 and 16d feature a highly amenable pyrrolopyrimidine scaffold that affords high nanomolar to low micromolar activity that can be easily modified with Michael acceptors with various reactivities and geometries. Our work thereby establishes a new pathway toward further development of subfamily selective GRK inhibitors and establishes Cys474 as a new and useful covalent handle in GRK5 drug discovery.
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Reference:
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