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. 2014 Jun 28;12(24):4074-7.
doi: 10.1039/c4ob00742e.

Investigating peptide sequence variations for 'double-click' stapled p53 peptides

Yu Heng Lau  1 , Peterson de Andrade, Niklas Sköld, Grahame J McKenzie, Ashok R Venkitaraman, Chandra Verma, David P Lane, David R Spring
Affiliations

Investigating peptide sequence variations for 'double-click' stapled p53 peptides

Yu Heng Lau et al. Org Biomol Chem. .

Abstract

Stapling peptides for inhibiting the p53/MDM2 interaction is a promising strategy for developing anti-cancer therapeutic leads. We evaluate double-click stapled peptides formed from p53-based diazidopeptides with different staple positions and azido amino acid side-chain lengths, determining the impact of these variations on MDM2 binding and cellular activity. We also demonstrate a K24R mutation, necessary for cellular activity in hydrocarbon-stapled p53 peptides, is not required for analogous 'double-click' peptides.

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