Structure-binding relation of philanthotoxins from nicotinic acetylcholine receptor binding assay

被引:34
作者
Nakanishi, K [1 ]
Huang, XF [1 ]
Jiang, H [1 ]
Liu, Y [1 ]
Fang, K [1 ]
Huang, DW [1 ]
Choi, SK [1 ]
Katz, E [1 ]
Eldefrawi, M [1 ]
机构
[1] UNIV MARYLAND, SCH MED, DEPT PHARMACOL & EXPT THERAPEUT, BALTIMORE, MD 21201 USA
关键词
D O I
10.1016/S0968-0896(97)00137-5
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Philanthotoxins are noncompetitive inhibitors of the nicotinic acetylcholine receptor and the Various glutamate receptors. Analogues carrying photoaffinity labels, fluorine atoms for solid-state NMR studies of ligand/receptor interaction, and large head groups such as porphyrins and planar bulky aromatic rings (BIG analogues) for clarifying mode of entry and orientation of analogues in receptors have been synthesized, assayed against the nicotinic acetylcholine receptor, and brief comments are given for the assay results. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:1969 / 1988
页数:20
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