Structural basis for producing selective MAP2K7 inhibitors.

ID: ALA4699503

Journal: Bioorg Med Chem Lett

Title: Structural basis for producing selective MAP2K7 inhibitors.

Authors: Murakawa Y,Valter S,Barr H,London N,Kinoshita T

Abstract: Mitogen-activated protein kinase kinase 7 (MAP2K7) in the c-Jun N-terminal kinase signal cascade is an attractive drug target for a variety of diseases. The selectivity of MAP2K7 inhibitors against off-target kinases is a major barrier in drug development. We report a crystal structure of MAP2K7 complexed with a potent covalent inhibitor bearing an acrylamide moiety as an electrophile, which discloses a structural basis for producing selective and potent MAP2K7 inhibitors.

CiteXplore: 32931911

DOI: 10.1016/j.bmcl.2020.127546

Patent ID: ┄