ADENOSINE-A1-RECEPTOR AND LIGAND MOLECULAR MODELING

被引:28
作者
DUDLEY, MW
PEET, NP
DEMETER, DA
WEINTRAUB, HJR
IJZERMAN, AP
NORDVALL, G
VANGALEN, PJM
JACOBSON, KA
机构
[1] CTR BIOPHARMACEUT SCI,LEIDEN,NETHERLANDS
[2] KAROLINSKA INST,S-10401 STOCKHOLM 60,SWEDEN
[3] NIH,BETHESDA,MD 20892
关键词
ADENOSINE; THEOPHYLLINE; MDL; 100; 991; N6-C8; MODEL; R-PIA;
D O I
10.1002/ddr.430280309
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This symposium provided a forum for presentations by the relevant groups on ligand design and ligand binding on the adenosine A1 receptor. Agreement appears to exist that the ''N6-C-8'' model of ligand binding to the receptor is the preferred mode. A consensus has not yet been reached on the actual placement of the ligand in the receptor and the exact amino acids which interact in its binding. Two viable models exist at present. Both can be tested with selective site-directed mutagenic studies on the A1 receptor as well as with additional designed ligands.
引用
收藏
页码:237 / 243
页数:7
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