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具有环五肽骨架的人工CXCR4配体的构效关系研究：通过几种芳香族氨基酸的取代探索五肽的氨基酸残基

Structure-activity relationship study on artificial CXCR4 ligands possessing the cyclic pentapeptide scaffold: the exploration of amino acid residues of pentapeptides by substitutions of several aromatic amino acids.

作者信息

Tanaka Tomohiro, Nomura Wataru, Narumi Tetsuo, Esaka Ai, Oishi Shinya, Ohashi Nami, Itotani Kyoko, Evans Barry J, Wang Zi-xuan, Peiper Stephen C, Fujii Nobutaka, Tamamura Hirokazu

机构信息

Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo, 101-0062, Japan.

出版信息

Org Biomol Chem. 2009 Sep 21;7(18):3805-9. doi: 10.1039/b908286g. Epub 2009 Jul 20.

DOI:10.1039/b908286g
PMID:19707686
Abstract

Previously, downsizing of a 14-residue peptidic CXCR4 antagonist has led to the development of a highly potent CXCR4 antagonist [cyclo(-d-Tyr(1)-Arg(2)-Arg(3)-Nal(4)-Gly(5)-)]. In the present study, cyclic pentapeptide libraries that were designed by substitutions of several amino acids for d-Tyr(1) and Arg(2) in peptide were prepared and screened to evaluate binding activity for CXCR4. The above structure-activity relationship study led to the finding of several potent CXCR4 ligands.

摘要

此前，一种14个残基的肽类CXCR4拮抗剂的缩小编导致了一种高效CXCR4拮抗剂[环（-d-酪氨酸（1）-精氨酸（2）-精氨酸（3）-萘丙氨酸（4）-甘氨酸（5）-）]的开发。在本研究中，通过用几种氨基酸替代肽中的d-酪氨酸（1）和精氨酸（2）设计了环状五肽文库，并进行筛选以评估其对CXCR4的结合活性。上述构效关系研究导致发现了几种有效的CXCR4配体。

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Structure-activity relationship study on artificial CXCR4 ligands possessing the cyclic pentapeptide scaffold: the exploration of amino acid residues of pentapeptides by substitutions of several aromatic amino acids.具有环五肽骨架的人工CXCR4配体的构效关系研究：通过几种芳香族氨基酸的取代探索五肽的氨基酸残基
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