Designer macrocyclic organo-peptide hybrids inhibit the interaction between p53 and HDM2/X by accommodating a functional α-helix.

ABSTRACT: We report the design of side-chain-to-tail linked organo-peptide hybrids incorporating an α-helical protein-binding motif. Using this strategy, macrocyclic inhibitors of the p53:HDM2 interaction displaying dual specificity against the HDMX homolog as well as increased proteolytic stability could be obtained.

SUBMITTER: Smith JM 

PROVIDER: S-EPMC4480681 | biostudies-literature | 2014 May

REPOSITORIES: biostudies-literature