Synthesis and preliminary analysis of a P-glycoprotein-specific [3H]-benzophenone photoaffinity label based on (-)-stipiamide

被引：12

作者：

Andrus, MB

Turner, TM

Sauna, ZE

Ambudkar, SV

机构：

[1] Brigham Young Univ, Dept Chem & Biochem, Provo, UT 84602 USA

[2] NCI, NIH, Cell Biol Lab, Div Basic Sci, Bethesda, MD 20878 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(00)00439-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A benzophenone photoaffinity label 9 based on the polyene natural product (-)-stipiamide has been constructed using a diaminoethane spacer and the radioactive agent [H-3]-BZDC (N-succinimidyl p-benzoyl-(2,3-H-3)-dehydrocinnamate). Photoaffinity experiments show specific binding to human P-glycoprotein (Pgp) in the presence of cis-flupentixol but not with cyclosporin A. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2275 / 2278

页数：4

共 18 条

[11]

GREENBERGER LM, 1993, J BIOL CHEM, V268, P11417

[12]

MORRIS DI, 1994, MOL PHARMACOL, V46, P329

[13] TETHERED BENZOPHENONE REAGENTS FOR THE SYNTHESIS OF PHOTOACTIVATABLE LIGANDS [J].