STUDY OF STEREO-REQUIREMENTS OF SUBSTANCE-P BINDING TO NK1 RECEPTORS USING ANALOGS WITH SYSTEMATIC D-AMINO-ACID REPLACEMENTS

被引:20
作者
WANG, JX
DIPASQUALE, AJ
BRAY, AM
MAEJI, NJ
GEYSEN, HM
机构
[1] Chiron Mimotopes Pty. Ltd., Clayton, Vic. 3168
关键词
D O I
10.1016/S0960-894X(01)80230-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A total of 512 stereoisomers of substance P, generated by systematic D-amino acid replacements, were synthesised by the multipin technique and their binding potencies to central NK1 receptors assessed. These results provide a comprehensive database for molecular modelling and drug design.
引用
收藏
页码:451 / 456
页数:6
相关论文
共 15 条
[1]   GAS-PHASE CLEAVAGE OF PEPTIDES FROM A SOLID SUPPORT WITH AMMONIA VAPOR - APPLICATION IN SIMULTANEOUS MULTIPLE PEPTIDE-SYNTHESIS [J].
BRAY, AM ;
MAEJI, NJ ;
JHINGRAN, AG ;
VALERIO, RM .
TETRAHEDRON LETTERS, 1991, 32 (43) :6163-6166
[2]  
CASCIERI MA, 1983, J BIOL CHEM, V258, P5158
[3]  
CHANG MM, 1970, J BIOL CHEM, V245, P4784
[4]   PREFERENTIAL CONFORMATION OF SUBSTANCE-P IN SOLUTION [J].
CHASSAING, G ;
CONVERT, O ;
LAVIELLE, S .
EUROPEAN JOURNAL OF BIOCHEMISTRY, 1986, 154 (01) :77-85
[5]   CONFORMATIONALLY RESTRICTED CYCLIC ANALOGS OF SUBSTANCE-P - INSIGHT INTO THE RECEPTOR-BINDING PROCESS [J].
DARMAN, PS ;
LANDIS, GC ;
SMITS, JR ;
HIRNING, LD ;
GULYA, K ;
YAMAMURA, HI ;
BURKS, TF ;
HRUBY, VJ .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1985, 127 (02) :656-662
[6]   BIOLOGICAL EVALUATION OF SUBSTANCE-P ANTAGONISTS [J].
FOLKERS, K ;
HAKANSON, R ;
HORIG, J ;
CHENG, XJ ;
LEANDER, S .
BRITISH JOURNAL OF PHARMACOLOGY, 1984, 83 (02) :449-456
[7]   THE CONFORMATIONAL-ANALYSIS OF SUBSTANCE-P ANALOGS USING HIGH-FIELD NMR TECHNIQUES [J].
KAWAKI, H ;
OTTER, A ;
BEIERBECK, H ;
KOTOVYCH, G ;
STEWART, JM .
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 1986, 3 (04) :795-803
[8]   EFFECTS OF SUBSTANCE-P AND OTHER PEPTIDES ON SPINAL NEURONS OF FROG [J].
KONISHI, S ;
OTSUKA, M .
BRAIN RESEARCH, 1974, 65 (03) :397-410
[9]  
MANAVALAN P, 1982, INT J PEPT PROT RES, V20, P351
[10]   INTERACTION OF TACHYKININS WITH THEIR RECEPTORS STUDIED WITH CYCLIC ANALOGS OF SUBSTANCE-P AND NEUROKININ-B [J].
PLOUX, O ;
LAVIELLE, S ;
CHASSAING, G ;
JULIEN, S ;
MARQUET, A ;
DORLEANSJUSTE, P ;
DION, S ;
REGOLI, D ;
BEAUJOUAN, JC ;
BERGSTROM, L ;
TORRENS, Y ;
GLOWINSKI, J .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1987, 84 (22) :8095-8099