Inhibitors of potassium channels KV1.3 and IK-1 as immunosuppressants

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2299-304. doi: 10.1016/j.bmcl.2009.02.077. Epub 2009 Feb 25.

Abstract

New structural classes of K(V)1.3 and IK-1 ion channel blockers have been identified based on a virtual high throughput screening approach using a homology model of KcsA. These compounds display inhibitory effects on T-cell and/or keratinocyte proliferation and immunosuppressant activity within a DTH animal model.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Calcium Signaling / drug effects
  • Calcium Signaling / physiology
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Disease Models, Animal
  • Humans
  • Hypersensitivity, Delayed / drug therapy
  • Hypersensitivity, Delayed / metabolism
  • Immunosuppressive Agents / chemical synthesis*
  • Immunosuppressive Agents / classification
  • Immunosuppressive Agents / pharmacology*
  • Intermediate-Conductance Calcium-Activated Potassium Channels / antagonists & inhibitors*
  • Intermediate-Conductance Calcium-Activated Potassium Channels / chemistry
  • Intermediate-Conductance Calcium-Activated Potassium Channels / physiology
  • Keratinocytes / drug effects
  • Keratinocytes / physiology
  • Kv1.3 Potassium Channel / antagonists & inhibitors*
  • Kv1.3 Potassium Channel / chemistry
  • Kv1.3 Potassium Channel / physiology
  • Patch-Clamp Techniques
  • Potassium Channel Blockers / chemical synthesis*
  • Potassium Channel Blockers / classification
  • Potassium Channel Blockers / pharmacology*

Substances

  • Immunosuppressive Agents
  • Intermediate-Conductance Calcium-Activated Potassium Channels
  • KCNN4 protein, human
  • Kv1.3 Potassium Channel
  • Potassium Channel Blockers