title: Novel Kv1.3 blockers for immunosuppression: WO2012155199.
abstract: A recent patent application from Bionomics/Merck Serono describes novel compounds as blockers of the voltage-gated Kv1.3 ion channel. The blockade of this channel shows great promise as a new therapeutic target for the treatment of autoimmune disorders such as multiple sclerosis, psoriasis, diabetes and rheumatoid arthritis. The generic claim of this patent refers to a new chemotype of Kv1.3 blockers based on an amide core with potent IC50's which are potentially within the nanomolar range. This article briefly reviews the chemistry and biology found in the patent and compares it with previous discoveries in the field.
authors: The Scripps Research Institute, Department of Molecular Therapeutics , 130 Scripps Way, Jupiter, FL , USA +1 561 228 2210 ; +1 561 228 3092 ; wnguyen@scripps.edu.
authors: William
authors: W
authors: Nguyen
mesh_terms: D000818:Animals; D001327:Autoimmune Diseases / Q000188:drug therapy; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D007166:Immunosuppressive Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D051664:Kv1.3 Potassium Channel / Q000037:antagonists & inhibitors*; D010330:Patents as Topic; D026902:Potassium Channel Blockers / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D007166:Immunosuppressive Agents; D051664:Kv1.3 Potassium Channel; D026902:Potassium Channel Blockers