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Issue 75, 2017

An in-tether chiral center modulates the proapoptotic activity of the KLA peptide

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Abstract

The helical peptide KLA (KLAKLAKKLAKLAK) is a well-known inducer of cellular apoptosis, acting to disrupt the mitochondrial membrane. However, its weak cellular uptake impedes development of any further applications. Here, we have utilized a novel in-tether chiral center induced helicity strategy (CIH) to develop a potent apoptosis inducer based on this KLA sequence. Notably, for the two resulting epimers of the CIH-KLA peptide, the CIH-KLA-(R) epimer exhibited superior cellular uptakes and special mitochondrial targeting when compared with its S counterpart. This work provides a promising and versatile method to modify the KLA peptide and a proof-of-concept application for the CIH strategy in modifying bioactive peptides.

Graphical abstract: An in-tether chiral center modulates the proapoptotic activity of the KLA peptide

Supplementary files

Article information


Submitted
26 Jun 2017
Accepted
30 Aug 2017
First published
30 Aug 2017

Chem. Commun., 2017,53, 10452-10455
Article type
Communication

An in-tether chiral center modulates the proapoptotic activity of the KLA peptide

J. Li, K. Hu, H. Chen, Y. Wu, L. Chen, F. Yin, Y. Tian and Z. Li, Chem. Commun., 2017, 53, 10452 DOI: 10.1039/C7CC04923D

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