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Preparation and biological properties of biotinylated PhTX derivatives.

Abstract：

:We report the synthesis of several highly functionalized biotinylated philanthotoxin (PhTX) analogues (7, 8, 10, 13-16) designed on the basis of earlier structure-activity 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 bifunctional photoaffinity probe (BPP), represent a new type of probe which should find use in photo-crosslinking studies of ligand receptor interactions.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Hashimoto M,Liu Y,Fang K,Li HY,Campiani G,Nakanishi K

doi

10.1016/s0968-0896(99)00054-1

subject

Has Abstract

pub_date

1999-06-01 00:00:00

pages

1181-94

issue

6

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(99)00054-1

journal_volume

7

pub_type

杂志文章

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