English   español  
Por favor, use este identificador para citar o enlazar a este item: http://hdl.handle.net/10261/141704
Título

Transient Receptor Potential Melastatin 8 Channel (TRPM8) Modulation: Cool Entryway for Treating Pain and Cancer

AutorPérez de Vega, M. Jesús; Gómez-Monterrey, Isabel; Ferrer-Montiel, Antonio; González-Muñiz, Rosario
Fecha de publicación20-jul-2016
EditorAmerican Chemical Society
CitaciónJournal of Medicinal Chemistry 59 : 10006−10029 (2016)
ResumenTRPM8 ion channels, the primary cold sensors in humans, are activated by innocuous cooling (<28 °C) and cooling compounds (menthol, icilin) and are implicated in sensing unpleasant cold stimuli as well as in mammalian thermoregulation. Overexpression of these thermoregulators in prostate cancer and in other life-threatening tumors, along with their contribution to an increasing number of pathological conditions, opens a plethora of medicinal chemistry opportunities to develop receptor modulators. This Perspective seeks to describe current known modulators for this ion channel because both agonists and antagonists may be useful for the treatment of most TRPM8-mediated pathologies. We primarily focus on SAR data for the different families of compounds and the pharmacological properties of the most promising ligands. Furthermore, we also address the knowledge about the channel structure, although still in its infancy, and the role of the TRPM8 protein signalplex to channel function and dysfunction. We finally outline the potential future prospects of the challenging TRPM8 drug discovery field
Versión del editorhttp://dx.doi.org/10.1021/acs.jmedchem.6b00305
URIhttp://hdl.handle.net/10261/141704
DOI10.1021/acs.jmedchem.6b00305
ISSN0022-2623
E-ISSN1520-4804
Aparece en las colecciones: (IQM) Artículos
Ficheros en este ítem:
Fichero Descripción Tamaño Formato  
J Med Chem_Perspective TRPM8_2016_revised _Gonzalez-Muñiz.pdf1,45 MBAdobe PDFVista previa
Visualizar/Abrir
Mostrar el registro completo
 

Artículos relacionados:


NOTA: Los ítems de Digital.CSIC están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.