relationship studies. Despite the extensive modifications, the binding to nicotinic acetylcholine receptor (nAChR) is in the low micromolar range according to an inhibition assay using 3H-thienylcyclohexyl-piperidine (TCP). A patch clamp functional assay gave comparable results. Compounds exemplified by 16, which consists of a biotinylated ligand linked to a bifunctionalphotoaffinityprobe (BPP), represent
A novel and non-radioactive bifunctionalphotoaffinityprobe (BPP) for the study of paclitaxel–microtubules interactions is designed and synthesized. This new BPP-taxoid bears a 3-nitro-5-trifluoromethyldiazirinyl-phenoxyacetyl group at C-3′N for photoaffinity/photocleavage and a biotin subunit at C-7 for affinity chromatography.
orthogonally. To three of the labels, moenomycin was conjugated with the aim to provide tools for the identification of the moenomycin binding site within the transglycosylase domain of the enzyme PBP 1b. Some preliminary photoaffinity-labeling experiments were carried out.
A Bifunctional Photoaffinity Probe for Ligand/Receptor Interaction Studies
作者:Kan Fang、Masaru Hashimoto、Steffen Jockusch、Nicholas J. Turro、Koji Nakanishi
DOI:10.1021/ja9817186
日期:1998.8.1
J. Turro, and Koji Nakanishi*Department of Chemistry, Columbia UniVersityNew York, New York 10027ReceiVed May 18, 1998Photoaffinity labeling has become a powerful tool for inves-tigating ligand/receptorinteractions since its introduction byWestheimer.
Kan Fang、Masaru Hashimoto、Steffen Jockusch、Nicholas J. Turro 和 Koji Nakanishi*化学系,哥伦比亚大学纽约,纽约 10027ReceiVed 1998 年 5 月 18 日自从引入配体/受体相互作用以来,光亲和标记已成为研究配体/受体相互作用的有力工具通过韦斯特海默。