Development of HER2-antagonistic peptides as novel anti-breast cancer drugs by in silico methods.

Development of HER2-antagonistic peptides as novel anti-breast cancer drugs by in silico methods. Research Abstract Details 

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Development of HER2-antagonistic peptides as novel anti-breast cancer drugs by in silico methods. Abstract Text:

Hiroo Nakajima,Naruhiko Mizuta,Koichi Sakaguchi,Ikuya Fujiwara,Atsushi Yoshimori,Satoshi Takahashi,Ryoko Takasawa,Sei-Ichi Tanuma,

An antagonistic peptide called HRAP that binds to the human HER2 molecule was designed by our computational method. In silico docking study demonstrated the specific interaction of HRAP with the dimerization domain in the HER2 molecule. Interestingly, HRAP inhibited proliferation of HER2-overexpressed human breast cancer cell lines. However, it had little cellular cytotoxicity (apoptosis inducibility). The cell proliferation inhibition was associated with the suppression of phosphorylation of PTEN and Akt. Thus, HRAP is the first HER2-binding small peptide antagonist rationally designed by a computer-aided SBDD method and is useful for the development of peptide mimetics to generate novel anti-breast cancer drugs.

Development of HER2-antagonistic peptides as novel anti-breast cancer drugs by in silico methods. Publishing Authors By Initials

H Nakajima,N Mizuta,K Sakaguchi,I Fujiwara,A Yoshimori,S Takahashi,R Takasawa,S Tanuma,

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Development of HER2-antagonistic peptides as novel anti-breast cancer drugs by in silico methods. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Breast cancer (Tokyo, Japan)

VOLUME: 15

Page Numbers: 65-72

Journal Abbreviation: Breast Cancer

ISSN: 1880-4233

DAY: 28

MONTH: 01

YEAR: 2008

Development of HER2-antagonistic peptides as novel anti-breast cancer drugs by in silico methods. Information

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LANGUAGE: eng

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Grant and Affiliation Information for Development of HER2-antagonistic peptides as novel anti-breast cancer drugs by in silico methods.

AFFILIATION: Department of Endocrine and Breast Surgery, Kyoto Prefectural University of Medicine, Kawaramachi-Hirokoji, Kamikyo-ku, Kyoto, 602-0841, Japan, hiro@koto.kpu-m.ac.jp.

Country: Japan

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MEDLINETA: Breast Cancer

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