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Int J Mol Sci. 2019 May 28;20(11). pii: E2618. doi: 10.3390/ijms20112618.

Recent Progress in TRPM8 Modulation: An Update.

Author information

1
Instituto de Química Médica, IQM-CSIC. Juan de la Cierva 3, 28006 Madrid, Spain. rosario.gonzalezmuniz@iqm.csic.es.
2
Instituto de Química Médica, IQM-CSIC. Juan de la Cierva 3, 28006 Madrid, Spain. angelesbonache@hotmail.com.
3
Instituto de Química Médica, IQM-CSIC. Juan de la Cierva 3, 28006 Madrid, Spain. cristinamartinescura@gmail.com.
4
Dipartimento di Farmacia, Università "Federico II" de Napoli, Via D. Montesano 49, 80131 Naples, Italy. imgomez@unina.it.

Abstract

The transient receptor potential melastatin subtype 8 (TRPM8) is a nonselective, multimodal ion channel, activated by low temperatures (<28 °C), pressure, and cooling compounds (menthol, icilin). Experimental evidences indicated a role of TRPM8 in cold thermal transduction, different life-threatening tumors, and other pathologies, including migraine, urinary tract dysfunction, dry eye disease, and obesity. Hence, the modulation of the TRPM8 channel could be essential in order to understand its implications in these pathologies and for therapeutic intervention. This short review will cover recent progress on the TRPM8 agonists and antagonists, describing newly reported chemotypes, and their application in the pharmacological characterization of TRPM8 in health and disease. The recently described structures of the TRPM8 channel alone or complexed with known agonists and PIP2 are also discussed.

KEYWORDS:

TRPM8; agonists; antagonists; structure

PMID:
31141957
DOI:
10.3390/ijms20112618
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