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

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

研究成果: Article査読

13 被引用数 (Scopus)

抄録

Previously, downsizing of a 14-residue peptidic CXCR4 antagonist 1 has led to the development of a highly potent CXCR4 antagonist 2 [cyclo(-d-Tyr 1-Arg2-Arg3-Nal4-Gly5-)]. In the present study, cyclic pentapeptide libraries that were designed by substitutions of several amino acids for d-Tyr1 and Arg2 in peptide 2 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.

本文言語English
ページ(範囲)3805-3809
ページ数5
ジャーナルOrganic and Biomolecular Chemistry
7
18
DOI
出版ステータスPublished - 7 9月 2009

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