具有环五肽骨架的CXCR4拮抗剂的构效关系研究
Structure-activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds.
作者信息
Tamamura Hirokazu, Esaka Ai, Ogawa Teppei, Araki Takanobu, Ueda Satoshi, Wang Zixuan, Trent John O, Tsutsumi Hiroshi, Masuno Hiroyuki, Nakashima Hideki, Yamamoto Naoki, Peiper Stephen C, Otaka Akira, Fujii Nobutaka
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. 2005 Dec 21;3(24):4392-4. doi: 10.1039/b513145f. Epub 2005 Nov 15.
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.
对先前通过使用环五肽文库发现的CXCR4拮抗剂进行了构效关系研究，以优化侧链官能团，其中涉及构象受限类似物。此外，还开发了一种引入新型药效团的环五肽新先导物。
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