The voltage-gated potassium channel Kv1.3 is a crucial player in maintaining the activation signal within T-cells and is evaluated as a promising target for the treatment of autoimmune diseases like multiple sclerosis, rheumatoid arthritis, diabetes and psoriasis. Our Lead Optimization program resulted in a set of potent Kv1.3 inhibitors with tunable selectivity, solubility and stability. Selected representatives displayed highly encouraging ameliorative effects in several different animal models relevant in the context of autoimmune diseases, like pristane-induced arthritis and allergic contact dermatitis, comparable or even slightly favourable over positive controls methotrexate, betamethasone or tacrolimus.

Kv1.3: A promising target for the treatment of autoimmune diseases

244th National Meeting (2012)

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