Structure-activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds

Hirokazu Tamamura; Ai Esaka; Teppei Ogawa; Takanobu Araki; Satoshi Ueda; Zixuan Wang; John O Trent; Hiroshi Tsutsumi; Hiroyuki Masuno; Hideki Nakashima; Naoki Yamamoto; Stephen C Peiper; Akira Otaka; Nobutaka Fujii

doi:10.1039/b513145f

Structure-activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds

Org Biomol Chem. 2005 Dec 21;3(24):4392-4. doi: 10.1039/b513145f. Epub 2005 Nov 15.

Authors

Hirokazu Tamamura¹, Ai Esaka, Teppei Ogawa, Takanobu Araki, Satoshi Ueda, Zixuan Wang, John O Trent, Hiroshi Tsutsumi, Hiroyuki Masuno, Hideki Nakashima, Naoki Yamamoto, Stephen C Peiper, Akira Otaka, Nobutaka Fujii

Affiliation

¹ Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan. tamamura.mr@tmd.ac.jp

PMID: 16327900
DOI: 10.1039/b513145f

Abstract

Structure-activity relationship studies on CXCR4 antagonists, which were previously found by using cyclic pentapeptide libraries, were performed to optimize side-chain functional groups, involving conformationally constrained analogues. In addition, a new lead of cyclic pentapeptides with the introduction of a novel pharmacophore was developed.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Inhibitory Concentration 50
Molecular Structure
Peptides, Cyclic / chemistry*
Peptides, Cyclic / pharmacology*
Receptors, CXCR4 / antagonists & inhibitors*
Receptors, CXCR4 / metabolism*
Structure-Activity Relationship

Substances

Peptides, Cyclic
Receptors, CXCR4
cyclo(tyrosyl-arginyl-arginyl-3-(2-naphthyl)alanyl-glycyl)