Inhibitors of potassium channels KV1.3 and IK-1 as immunosuppressants.
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.
Pegoraro
Stefano
S
4SC AG, Am Klopferspitz 19a, 82152 Planegg-Martinsried, Germany.
Lang
Martin
M
Dreker
Tobias
T
Kraus
Jürgen
J
Hamm
Svetlana
S
Meere
Cathal
C
Feurle
Juliane
J
Tasler
Stefan
S
Prütting
Sylvia
S
Kuras
Zerrin
Z
Visan
Violeta
V
Grissmer
Stephan
S
D000818:Animals; D020013:Calcium Signaling / Q000187:drug effects / Q000502:physiology; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D004195:Disease Models, Animal; D006801:Humans; D006968:Hypersensitivity, Delayed / Q000188:drug therapy / Q000378:metabolism; D007166:Immunosuppressive Agents / Q000138:chemical synthesis* / Q000145:classification / Q000494:pharmacology*; D051660:Intermediate-Conductance Calcium-Activated Potassium Channels / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000502:physiology; D015603:Keratinocytes / Q000187:drug effects / Q000502:physiology; D051664:Kv1.3 Potassium Channel / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000502:physiology; D018408:Patch-Clamp Techniques; D026902:Potassium Channel Blockers / Q000138:chemical synthesis* / Q000145:classification / Q000494:pharmacology*
D007166:Immunosuppressive Agents; D051660:Intermediate-Conductance Calcium-Activated Potassium Channels; C496923:KCNN4 protein, human; D051664:Kv1.3 Potassium Channel; D026902:Potassium Channel Blockers