A nonpeptidic agonist ligand of the human C5a receptor: Synthesis, binding affinity optimization and functional characterization.

被引:19
作者
deLaszlo, SE [1 ]
Allen, EE [1 ]
Li, B [1 ]
Ondeyka, D [1 ]
Rivero, R [1 ]
Malkowitz, L [1 ]
Molineaux, C [1 ]
Siciliano, SJ [1 ]
Springer, MS [1 ]
Greenlee, WJ [1 ]
Mantlo, N [1 ]
机构
[1] MERCK RES LABS,DEPT IMMUNOL RES,RAHWAY,NJ 07065
关键词
D O I
10.1016/S0960-894X(96)00606-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The structural optimization for binding affinity and attempted modification of agonist function of a nonpeptide ligand of the human C5a receptor is described. (C) 1997, Elsevier Science Ltd.
引用
收藏
页码:213 / 218
页数:6
相关论文
共 14 条
[1]   THE STEREOSPECIFIC SYNTHESIS OF ALAHOPCIN [J].
BALDWIN, JE ;
ADLINGTON, RM ;
GODFREY, CRA ;
GOLLINS, DW ;
SCHOFIELD, CJ .
TETRAHEDRON, 1991, 47 (30) :5835-5840
[2]  
DEMARTINO JA, 1994, J BIOL CHEM, V269, P14446
[3]  
FLANAGAN KL, 1995, 210 ACS NAT M CHIC I
[4]  
GOLDSTEIN IM, 1988, INFLAMMATION BASIC P, P55
[5]  
HAGMANN WK, 1992, ANNU REP MED CHEM, V27, P199
[6]  
KAWAI M, WO9212168A WORLD INT
[7]  
KIM D, 1995, 210 ACS NAT M CHIC I
[8]  
KONTEATIS ZD, 1994, J IMMUNOL, V153, P4200
[9]   SUBSTITUTED 4,6-DIAMINOQUINOLINES AS INHIBITORS OF C5A RECEPTOR-BINDING [J].
LANZA, TJ ;
DURETTE, PL ;
ROLLINS, T ;
SICILIANO, S ;
CIANCIARULO, DN ;
KOBAYASHI, SV ;
CALDWELL, CG ;
SPRINGER, MS ;
HAGMANN, WK .
JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (02) :252-258
[10]  
MOLLISON KW, 1992, FASEB J, V6, pA2058