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

Peiyu Zhang; Martin Walko; Andrew J. Wilson

doi:10.1039/d2cc06029a

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

Peiyu Zhang, Martin Walko, Andrew J. Wilson^*

^*Corresponding author for this work

Chemistry

Research output: Contribution to journal › Article › peer-review

1 Citation (Scopus)

15 Downloads (Pure)

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.

Original language	English
Pages (from-to)	1697-1700
Number of pages	4
Journal	Chemical Communications
Volume	59
Issue number	12
Early online date	13 Jan 2023
DOIs	https://doi.org/10.1039/d2cc06029a
Publication status	Published - 11 Feb 2023

Bibliographical note

Publisher Copyright:
© 2023 The Royal Society of Chemistry.

ASJC Scopus subject areas

Catalysis
Electronic, Optical and Magnetic Materials
Ceramics and Composites
General Chemistry
Surfaces, Coatings and Films
Metals and Alloys
Materials Chemistry

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Access to Document

10.1039/d2cc06029aLicence: Creative Commons: Attribution (CC BY)

ZhangP2023RationalFinal published version, 918 KBLicence: Creative Commons: Attribution (CC BY)

Cite this

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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-xL selective peptidomimetic ligands. These HRK-inspired reagents may serve as starting points for the discovery of therapeutics to target BCL-xL-overexpressed cancers.",

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