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ID: ALA1157603

Journal: J Med Chem

Title: Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1.

Authors: Bernardo PH, Sivaraman T, Wan KF, Xu J, Krishnamoorthy J, Song CM, Tian L, Chin JS, Lim DS, Mok HY, Yu VC, Tong JC, Chai CL.

Abstract: The screening of a small focused library of rhodanine derivatives as inhibitors of Bcl-2 proteins led to the discovery of two structurally related compounds with different binding profiles against the Bcl-XL and the Mcl-1 proteins. Subsequent NMR studies with mutant proteins and in silico docking studies provide a possible rationale for the observed specificity.

CiteXplore: 20158203

DOI: 10.1021/jm901469p