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

A Lew; A R Chamberlin

doi:10.1016/s0960-894x(99)00601-0

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

Bioorg Med Chem Lett. 1999 Dec 6;9(23):3267-72. doi: 10.1016/s0960-894x(99)00601-0.

Authors

A Lew¹, A R Chamberlin

Affiliation

¹ Department of Chemistry, University of California, Irvine 92697, USA.

PMID: 10612582
DOI: 10.1016/s0960-894x(99)00601-0

Abstract

Blockers of the human Kv1.3 potassium channel were designed using Biosym/MSI's ligand design program LUDI. Parallel combinatorial synthesis of the resultant substituted phenyl-stilbenes on solid phase, followed by 125I Charybdotoxin (125I ChTx) screening, yielded 12 Kv1.3 channel blockers with modest activity.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Combinatorial Chemistry Techniques*
Humans
Kv1.3 Potassium Channel
Ligands
Potassium Channel Blockers*
Potassium Channels*
Potassium Channels, Voltage-Gated*
Stilbenes / chemical synthesis*
Stilbenes / pharmacology

Substances

KCNA3 protein, human
Kv1.3 Potassium Channel
Ligands
Potassium Channel Blockers
Potassium Channels
Potassium Channels, Voltage-Gated
Stilbenes