title: TRPM8 biology and medicinal chemistry.
abstract: TRPM8 belongs to the TRPM Melastatin subfamily of Transient Receptor Potential (TRP) ion channels. Activated by cool temperatures and mimetic ligands, such as menthol and icilin, TRPM8 has been shown to play a role in thermoreception and is expressed in peripheral nerves. TRPM8 is also expressed in other tissues which are not exposed to temperature fluctuations, such as the prostate. The recent advancement of a TRPM8 agonist into the clinic for the treatment of prostate cancer suggests that the channel plays a role in some human pathologies. As more drug-like and selective agonists and antagonists of TRPM8 become available, in vivo pharmacology studies will complement already published knockout data to further our understanding of the role of TRPM8 in human disease.
authors.affiliation: Renovis, Inc., Two Corporate Drive, South San Francisco, CA, USA (a wholly owned subsidiary of Evotec, AG). jeff.defalco@envoytherapeutics.com
authors.forename: Jeff
authors.initials: J
authors.lastname: DeFalco
authors.forename: Matthew A J
authors.initials: MA
authors.lastname: Duncton
authors.forename: Daniel
authors.initials: D
authors.lastname: Emerling
mesh_terms: D002626:Chemistry, Pharmaceutical; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D050053:TRPM Cation Channels / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D008024:Ligands; D050053:TRPM Cation Channels