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

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)...

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Detalles Bibliográficos
Autores principales: Zhang, Peiyu, Walko, Martin, Wilson, Andrew J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2023
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9904277/
https://www.ncbi.nlm.nih.gov/pubmed/36692261
http://dx.doi.org/10.1039/d2cc06029a
Descripción
Sumario: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.

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