Design and synthesis of novel dual-cyclic RGD peptides for &#945;<sub>v</sub>ß<sub>3</sub> integrin targeting.

Liu, Junjie; Cheng, Xiaozhong; Tian, Xiaobo; Guan, Dongliang; Ao, Jiwei; Wu, Zhimeng; Huang, Wei; Le, Zhiping

Design and synthesis of novel dual-cyclic RGD peptides for α_vß₃ integrin targeting.

Liu, Junjie; Cheng, Xiaozhong; Tian, Xiaobo; Guan, Dongliang; Ao, Jiwei; Wu, Zhimeng; Huang, Wei; Le, Zhiping.

Afiliação

Liu J; Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, PR China; CAS Key Laboratory of Receptor Research, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Pudong, Shanghai 201203, PR
Cheng X; Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, PR China.
Tian X; Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, PR China; CAS Key Laboratory of Receptor Research, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Pudong, Shanghai 201203, PR
Guan D; CAS Key Laboratory of Receptor Research, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Pudong, Shanghai 201203, PR China; University of Chinese Academy of Sciences, No.19A Yuquan Road, Beijing 100049, PR C
Ao J; CAS Key Laboratory of Receptor Research, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Pudong, Shanghai 201203, PR China.
Wu Z; Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, PR China. Electronic address: zwu@jiangnan.edu.cn.
Huang W; CAS Key Laboratory of Receptor Research, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Pudong, Shanghai 201203, PR China; University of Chinese Academy of Sciences, No.19A Yuquan Road, Beijing 100049, PR C
Le Z; Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, PR China. Electronic address: zple@ncu.edu.cn.

Bioorg Med Chem Lett ; 29(7): 896-900, 2019 04 01.

Article em En | MEDLINE | ID: mdl-30732943

ABSTRACT

ABSTRACT

The specific binding of RGD cyclic peptide with integrin αvß3 attracts great research interest for tumor-targeting drug delivery. Herein, we designed and synthesized a series of dual-ring RGD-peptide derivatives as a drug carrier for αvß3 targeting. Three novel peptides showed excellent cell adhesion inhibition effect, in which, P3 exhibited 7-fold enhancement in IC50 compared with cyclo(RGDfK). Drug-loaded cytotoxicity experiment and imaging experiment indicated that such dual-cyclic RGD peptides have good tumor targeting effects. This work provides a new strategy for the design of novel RGD peptides.

Assuntos

Integrina alfaVbeta3/metabolismo; Oligopeptídeos/síntese química; Oligopeptídeos/farmacologia; Sequência de Aminoácidos; Antineoplásicos/síntese química; Antineoplásicos/química; Antineoplásicos/farmacologia; Adesão Celular/efeitos dos fármacos; Linhagem Celular Tumoral; Sobrevivência Celular/efeitos dos fármacos; Desenho de Fármacos; Humanos; Oligopeptídeos/química; Conformação Proteica

Palavras-chave

Adhesion inhibition; Cyclo(RGDfK); RGD cyclic peptide; Tumor-targeting; α(v)ß(3) integrin

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Oligopeptídeos / Integrina alfaVbeta3 Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Porto Rico

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