文章基本信息

标题：Development of Low Molecular Weight Ligands for Integrin αvβ3
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作者：Akira Makino ; Masahiro Ueda ; Yoshitaka Uematsu 等
期刊名称：Chemical and Pharmaceutical Bulletin
印刷版ISSN：0009-2363
电子版ISSN：1347-5223
出版年度：2022
卷号：70
期号：4
页码：293-299
DOI：10.1248/cpb.c21-01085
语种：English
出版社：The Pharmaceutical Society of Japan
摘要：We designed and synthesized non-peptide organic molecular ligands for integrin αvβ3. Candidate ligands featured amidino analog and carboxy groups as binding sites on either side of a spacer, which consisted of benzophenone or an analog, such as diphenyl sulfide, diphenyl sulfoxide, diphenyl sulfone, or diphenyl ether. Competitive binding assays to integrin αvβ3 with respect to [125I]echistatin were used to determine inhibitory activity of the synthetic ligands. Ligands bearing 2-aminobenzimidazoyl and glycyl groups separated by a benzophenone spacer demonstrated more potent binding than did a linear Arg-Gly-Asp (RGD) tripeptide that represents the native integrin αvβ3 binding motif. Ligands possessing 2-aminobenzimidazoyl and carboxy groups and diphenyl sulfoxide or diphenyl ether spacers inhibited binding of [125I]echistatin with IC50 values similar to that of the linear RGD tripeptide.
关键词：integrin αvβ3;non-peptide;synthetic ligand;[125I]echistatin