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.
Hirokazu Tamamura  1 ,  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
Affiliations
  • 1. Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan. [email protected]
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.

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