Blockers of human T cell Kv1.3 potassium channels using de novo ligand design and solid-phase parallel combinatorial chemistry

Authors
Lew, A Chamberlin, AR
Citation
A. Lew et Ar. Chamberlin, Blockers of human T cell Kv1.3 potassium channels using de novo ligand design and solid-phase parallel combinatorial chemistry, BIOORG MED, 9(23), 1999, pp. 3267-3272
Citations number
28
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
23
Year of publication
1999
Pages
3267 - 3272
Database
ISI
SICI code
0960-894X(199912)9:23<3267:BOHTCK>2.0.ZU;2-D
Abstract
Blockers of the human Kv1.3 potassium channel were designed using Biosym/MS I's ligand design program LUDI. Parallel combinatorial synthesis of the res ultant substituted phenyl-stilbenes on solid phase, followed by I-125 Chary bdotoxin (I-125 ChTx) screening, yielded 12 Kv1.3 channel blockers with mod est activity. (C) 1999 Elsevier Science Ltd. All rights reserved.