Blockers of human T cell Kv1.3 potassium channels using de novo ligand design and solid-phase parallel combinatorial chemistry.
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.
Lew
A
A
Department of Chemistry, University of California, Irvine 92697, USA.
Chamberlin
A R
AR
D020650:Combinatorial Chemistry Techniques; D006801:Humans; D051664:Kv1.3 Potassium Channel; D008024:Ligands; D026902:Potassium Channel Blockers; D015221:Potassium Channels; D024642:Potassium Channels, Voltage-Gated; D013267:Stilbenes / Q000138:chemical synthesis* / Q000494:pharmacology
C496973:KCNA3 protein, human; D051664:Kv1.3 Potassium Channel; D008024:Ligands; D026902:Potassium Channel Blockers; D015221:Potassium Channels; D024642:Potassium Channels, Voltage-Gated; D013267:Stilbenes