Design of PAP-1, a selective small molecule Kv1. 3 blocker, for the suppression of effector memory T cells in autoimmune diseases

…, A Sankaranarayanan, P Azam, K Schmidt-Lassen…

Index: Schmitz, Alexander; Sankaranarayanan, Ananthakrishnan; Azam, Philippe; Schmidt-Lassen, Kristina; Homerick, Daniel; Haensel, Wolfram; Wulff, Heike Molecular Pharmacology, 2005 , vol. 68, # 5 p. 1254 - 1270

Full Text: HTML

Citation Number: 138

Abstract

Abstract The lymphocyte K+ channel Kv1. 3 constitutes an attractive pharmacological target for the selective suppression of terminally differentiated effector memory T (T EM) cells in T cell-mediated autoimmune diseases, such as multiple sclerosis and type 1 diabetes. Unfortunately, none of the existing small-molecule Kv1. 3 blockers is selective, and many of them, such as correolide, 4-phenyl-4-[3-(methoxyphenyl)-3-oxo-2-azapropyl] ...