Structure-activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds.
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.
Tamamura
Hirokazu
H
Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan. tamamura.mr@tmd.ac.jp
Esaka
Ai
A
Ogawa
Teppei
T
Araki
Takanobu
T
Ueda
Satoshi
S
Wang
Zixuan
Z
Trent
John O
JO
Tsutsumi
Hiroshi
H
Masuno
Hiroyuki
H
Nakashima
Hideki
H
Yamamoto
Naoki
N
Peiper
Stephen C
SC
Otaka
Akira
A
Fujii
Nobutaka
N
D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000494:pharmacology*; D019718:Receptors, CXCR4 / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013329:Structure-Activity Relationship
D010456:Peptides, Cyclic; D019718:Receptors, CXCR4; C496951:cyclo(tyrosyl-arginyl-arginyl-3-(2-naphthyl)alanyl-glycyl)