Rational design of Harakiri (HRK)-derived constrained peptides as BCL-xL inhibitors.
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ABSTRACT:
SUBMITTER: Zhang P
PROVIDER: S-EPMC9904277 | biostudies-literature | 2023 Feb
REPOSITORIES: biostudies-literature
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Rational design of Harakiri (HRK)-derived constrained peptides as BCL-x<sub>L</sub> inhibitors.
Zhang Peiyu P Walko Martin M Wilson Andrew J AJ
Chemical communications (Cambridge, England) 20230207 12
Using the HRK BH3 domain, sequence hybridization and <i>in silico</i> methods we show dibromomaleimide staple scanning can be used to inform the design of BCL-x<sub>L</sub> selective peptidomimetic ligands. These HRK-inspired reagents may serve as starting points for the discovery of therapeutics to target BCL-x<sub>L</sub>-overexpressed cancers. ...[more]
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