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http://hdl.handle.net/10261/141704
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Campo DC | Valor | Lengua/Idioma |
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dc.contributor.author | Pérez de Vega, M. Jesús | es_ES |
dc.contributor.author | Gómez-Monterrey, Isabel | es_ES |
dc.contributor.author | Ferrer-Montiel, Antonio | es_ES |
dc.contributor.author | González-Muñiz, Rosario | es_ES |
dc.date.accessioned | 2016-12-20T11:45:59Z | - |
dc.date.available | 2016-12-20T11:45:59Z | - |
dc.date.issued | 2016-07-20 | - |
dc.identifier.citation | Journal of Medicinal Chemistry 59 : 10006−10029 (2016) | es_ES |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | http://hdl.handle.net/10261/141704 | - |
dc.description.abstract | TRPM8 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 | es_ES |
dc.description.sponsorship | We thank Gregorio Fernández-Ballester for the figure of the TRPM8 homology model. Funding from the Ministry of Economy and Competitiveness (BFU 2012-39092-C02; SAF2015-66275-C2-R) and the Generalitat Valenciana (PROMETEO II/2014/011). | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | American Chemical Society | es_ES |
dc.relation.isversionof | Postprint | es_ES |
dc.rights | openAccess | en_EN |
dc.title | Transient Receptor Potential Melastatin 8 Channel (TRPM8) Modulation: Cool Entryway for Treating Pain and Cancer | es_ES |
dc.type | artículo | es_ES |
dc.identifier.doi | 10.1021/acs.jmedchem.6b00305 | - |
dc.description.peerreviewed | Peer reviewed | es_ES |
dc.relation.publisherversion | http://dx.doi.org/10.1021/acs.jmedchem.6b00305 | es_ES |
dc.identifier.e-issn | 1520-4804 | - |
dc.embargo.terms | 2017-08-01 | - |
dc.contributor.funder | Ministerio de Economía y Competitividad (España) | es_ES |
dc.contributor.funder | Generalitat Valenciana | es_ES |
dc.relation.csic | Sí | es_ES |
oprm.item.hasRevision | no ko 0 false | * |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003329 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003359 | es_ES |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairetype | artículo | - |
item.grantfulltext | open | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | With Fulltext | - |
item.languageiso639-1 | en | - |
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Fichero | Descripción | Tamaño | Formato | |
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J Med Chem_Perspective TRPM8_2016_revised _Gonzalez-Muñiz.pdf | 1,45 MB | Adobe PDF | Visualizar/Abrir |
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