BACKBONE MODIFIED FORMYL-METHIONYL TRIPEPTIDE CHEMOATTRACTANTS

被引:24
作者
FORMAGGIO, F
PANTANO, M
CRISMA, M
TONIOLO, C
BOESTEN, WHJ
SCHOEMAKER, HE
KAMPHUIS, J
BECKER, EL
机构
[1] UNIV PADUA,CNR,DEPT ORGAN CHEM,BIOPOLYMER RES CTR,I-35131 PADUA,ITALY
[2] DSM RES & PATENTS,BIOORGAN CHEM SECT,6160 MD GELEEN,NETHERLANDS
[3] UNIV CONNECTICUT,CTR HLTH,DEPT PATHOL,FARMINGTON,CT 06032
关键词
D O I
10.1016/S0960-894X(00)80699-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The conformationally restricted tripeptides HCO-L-Met-Xxx-L-Phe-OMe [where Xxx is L (D)-Iva, -(alphaMe)Val or -(alphaMe)Phe] were synthesized and tested for their beta-glucosaminidase release activity. The [L-(alphaMe)Val]2- and [L-(alphaMe)Leu]2- analogues turned out to be the most active compounds examined. The positive effects induced by increasing side-chain hydrophobicity and by the L-chirality of the Xxx residue on peptide-receptor interactions are discussed.
引用
收藏
页码:953 / 956
页数:4
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