Rational design of Harakiri (HRK)-derived constrained peptides as BCL-xL inhibitors

Peiyu Zhang; Martin Walko; Andrew J. Wilson

doi:10.1039/D2CC06029A

You do not have JavaScript enabled. Please enable JavaScript to access the full features of the site or access our non-JavaScript page.

Rational design of Harakiri (HRK)-derived constrained peptides as BCL-x_L inhibitors†

Peiyu Zhang,

^ab Martin Walko

^ab and Andrew J. Wilson

*^ab

Author affiliations

* Corresponding authors

^a School of Chemistry, University of Leeds, Woodhouse Lane, Leeds, UK
E-mail: a.j.wilson@leeds.ac.uk

^b Astbury Centre for Structural Molecular Biology, University of Leeds, Woodhouse Lane, Leeds, UK

Abstract

Using the HRK BH3 domain, sequence hybridization and in silico methods we show dibromomaleimide staple scanning can be used to inform the design of BCL-x_L selective peptidomimetic ligands. These HRK-inspired reagents may serve as starting points for the discovery of therapeutics to target BCL-x_L-overexpressed cancers.

Download options Please wait...

Supplementary files

Supplementary information PDF (2373K)

Article information

DOI: https://doi.org/10.1039/D2CC06029A
Article type: Communication
Submitted: 08 Nov 2022
Accepted: 13 Jan 2023
First published: 13 Jan 2023
This article is Open Access

Download Citation

Chem. Commun., 2023,59, 1697-1700

Permissions

Request permissions

Rational design of Harakiri (HRK)-derived constrained peptides as BCL-x_L inhibitors

P. Zhang, M. Walko and A. J. Wilson, Chem. Commun., 2023, 59, 1697 DOI: 10.1039/D2CC06029A

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

Social activity

Fetching data from CrossRef.
This may take some time to load.

Chemical Communications