Minimization of apoptosis-inducing CPP-Bim peptide

Shengli Zhou; Kazunori Watanabe; Seiichiro Koide; Mizuki Kitamatsu; Takashi Ohtsuki

doi:10.1016/j.bmcl.2021.127811

Minimization of apoptosis-inducing CPP-Bim peptide

Shengli Zhou, Kazunori Watanabe, Seiichiro Koide, Mizuki Kitamatsu, Takashi Ohtsuki

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

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.

Original language	English
Article number	127811
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	36
DOIs	https://doi.org/10.1016/j.bmcl.2021.127811
Publication status	Published - Mar 15 2021

Keywords

Apoptosis
Bim
Cell penetrating peptide
Poly(Arg)
Tat

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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title = "Minimization of apoptosis-inducing CPP-Bim peptide",

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.",

keywords = "Apoptosis, Bim, Cell penetrating peptide, Poly(Arg), Tat",

author = "Shengli Zhou and Kazunori Watanabe and Seiichiro Koide and Mizuki Kitamatsu and Takashi Ohtsuki",

note = "Funding Information: This work was supported by JSPS KAKENHI Grant Number JP18H02090 (to T. O.). Publisher Copyright: {\textcopyright} 2021 Elsevier Ltd",

year = "2021",

month = mar,

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doi = "10.1016/j.bmcl.2021.127811",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - Minimization of apoptosis-inducing CPP-Bim peptide

AU - Zhou, Shengli

AU - Watanabe, Kazunori

AU - Koide, Seiichiro

AU - Kitamatsu, Mizuki

AU - Ohtsuki, Takashi

PY - 2021/3/15

Y1 - 2021/3/15

N2 - 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.

AB - 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.

KW - Apoptosis

KW - Bim

KW - Cell penetrating peptide

KW - Poly(Arg)

KW - Tat

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Minimization of apoptosis-inducing CPP-Bim peptide

Abstract

Keywords

ASJC Scopus subject areas

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