Leukotriene B4 photoaffinity probes:: Design, synthesis and evaluation of new arylazide-1,3-disubstituted cyclohexanes

被引:3
|
作者
Durand, D [1 ]
Hullot, P [1 ]
Vidal, JP [1 ]
Girard, JP [1 ]
Banères, JL [1 ]
Parello, J [1 ]
Muller, A [1 ]
Bonne, C [1 ]
Rossi, JC [1 ]
机构
[1] Fac Pharm Montpellier, UPRESA CNRS 5074, Lab Chim Biomol & Interact Biol, F-34060 Montpellier 2, France
关键词
D O I
10.1016/S0960-894X(00)00103-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and the binding affinities of new leukotriene Bq receptor photoaffinity probes, where a 1,3-disubstitued cyclohexane ring replaces the conjugated Delta(6.7) and Delta(8.9) double bonds of the natural eicosanoid, are described. One enantiomeric componnd, 4b alpha, is specifically cross-linked upon photolysis to the recombinant leukotriene Bq receptor from human origin (h-BLTR) solubilized in a micellar medium. This probe appears as a good candidate for identifying the ligand binding site of this receptor. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:811 / 814
页数:4
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