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

Authors
Andrus, MB Turner, TM Sauna, ZE Ambudkar, SV
Citation
Mb. Andrus et al., Synthesis and preliminary analysis of a P-glycoprotein-specific [H-3]-benzophenone photoaffinity label based on (-)-stipiamide, BIOORG MED, 10(20), 2000, pp. 2275-2278
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
20
Year of publication
2000
Pages
2275 - 2278
Database
ISI
SICI code
0960-894X(20001016)10:20<2275:SAPAOA>2.0.ZU;2-K
Abstract
A benzophenone photoaffinity label 9 based on the polyene natural product ( -)-stipiamide has been constructed using a diaminoethane spacer and the rad ioactive agent [H-3]-BZDC (N-succinimidyl p-benzoyl-(2,3-H-3)-dehydrocinnam ate). Photoaffinity experiments show specific binding to human P-glycoprote in (Pgp) in the presence of cis-flupentixol but not with cyclosporin A. (C) 2000 Elsevier Science Ltd. All rights reserved.