Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.

ABSTRACT: Because of the promise of BCL-2 antagonists in combating chronic lymphocytic leukemia (CLL) and non-Hodgkin's lymphoma (NHL), interest in additional selective antagonists of antiapoptotic proteins has grown. Beginning with a series of selective, potent BCL-XL antagonists containing an undesirable hydrazone functionality, in silico design and X-ray crystallography were utilized to develop alternative scaffolds that retained the selectivity and potency of the starting compounds.

SUBMITTER: Koehler MF 

PROVIDER: S-EPMC4060937 | biostudies-literature | 2014 Jun

REPOSITORIES: biostudies-literature