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Minimization of apoptosis-inducing CPP-Bim peptide

Authors :
Takashi Ohtsuki
Shengli Zhou
Mizuki Kitamatsu
Kazunori Watanabe
Seiichiro Koide
Source :
Bioorganic & Medicinal Chemistry Letters. 36:127811
Publication Year :
2021
Publisher :
Elsevier BV, 2021.

Abstract

Pro-apoptotic peptides may be promising agents for cancer therapy owing to their ability to induce apoptosis in cancer cells. TatBim, a fusion peptide of Tat cell-penetrating peptide (CPP) and the BH3 domain derived from Bim apoptosis-inducing protein, is a pro-apoptotic peptide. In this study, based on the TatBim sequence, we attempted to minimize the CPP-Bim peptide while retaining apoptosis-inducing activity. The CPP and Bim parts were systematically shortened, and the pro-apoptotic activities of the shortened peptides were examined. We obtained TatBim-N1C2 and R8Bim-N1C2 as minimized peptides with efficient apoptotic activity. These peptides may have potential applications in future biomedical studies, such as cancer therapeutics.

Details

ISSN :
0960894X
Volume :
36
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....938c072f356ffc976607cb57a0f9d068
Full Text :
https://doi.org/10.1016/j.bmcl.2021.127811