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Campo DC | Valor | Lengua/Idioma |
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dc.contributor.author | Coll-Martínez, Bernat | - |
dc.contributor.author | Delgado Cirilo, Antonio | - |
dc.contributor.author | Crosas, Bernat | - |
dc.date.accessioned | 2020-12-28T14:25:49Z | - |
dc.date.available | 2020-12-28T14:25:49Z | - |
dc.date.issued | 2020 | - |
dc.identifier.citation | Molecules 25(24): 5956 (2020) | - |
dc.identifier.uri | http://hdl.handle.net/10261/225730 | - |
dc.description.abstract | The induction of protein degradation in a highly selective and efficient way by means of druggable molecules is known as targeted protein degradation (TPD). TPD emerged in the literature as a revolutionary idea: a heterobifunctional chimera with the capacity of creating an interaction between a protein of interest (POI) and a E3 ubiquitin ligase will induce a process of events in the POI, including ubiquitination, targeting to the proteasome, proteolysis and functional silencing, acting as a sort of degradative knockdown. With this programmed protein degradation, toxic and disease-causing proteins could be depleted from cells with potentially effective low drug doses. The proof-of-principle validation of this hypothesis in many studies has made the TPD strategy become a new attractive paradigm for the development of therapies for the treatment of multiple unmet diseases. Indeed, since the initial protacs (Proteolysis targeting chimeras) were posited in the 2000s, the TPD field has expanded extraordinarily, developing innovative chemistry and exploiting multiple degradation approaches. In this article, we review the breakthroughs and recent novel concepts in this highly active discipline. | - |
dc.description.sponsorship | Research funded by Consejo Superior de Investigaciones Científicas (Spanish National Research Council) (project 202020E161, CSIC-COV19). Additional partial financial support from Project CTQ2017-85378-R (AEI/FEDER, UE) from the Spanish Ministry of Science, Innovation and Universities, is acknowledged. | - |
dc.language.iso | eng | - |
dc.publisher | Multidisciplinary Digital Publishing Institute | - |
dc.relation | info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/CTQ2017-85378-R | - |
dc.relation | CTQ2017-85378-R/AEI/10.13039/501100011033 | - |
dc.relation.isversionof | Publisher's version | - |
dc.rights | openAccess | - |
dc.subject | Chimeras | - |
dc.subject | Protac | - |
dc.subject | Targeted protein degradation | - |
dc.subject | Ubiquitin | - |
dc.subject | Proteasome | - |
dc.subject | Lysosome | - |
dc.subject | Autophagy | - |
dc.title | The Potential of Proteolytic Chimeras as Pharmacological Tools and Therapeutic Agents | - |
dc.type | artículo | - |
dc.identifier.doi | 10.3390/molecules25245956 | - |
dc.description.peerreviewed | Publisher’s version | - |
dc.relation.publisherversion | https://doi.org/10.3390/molecules25245956 | - |
dc.identifier.e-issn | 1420-3049 | - |
dc.date.updated | 2020-12-28T14:25:50Z | - |
dc.rights.license | http://creativecommons.org/licenses/by/4.0/ | - |
dc.contributor.funder | Agencia Estatal de Investigación (España) | - |
dc.contributor.funder | Ministerio de Ciencia, Innovación y Universidades (España) | - |
dc.contributor.funder | Consejo Superior de Investigaciones Científicas (España) | - |
dc.relation.csic | Sí | - |
dc.identifier.funder | http://dx.doi.org/10.13039/501100011033 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003339 | es_ES |
dc.identifier.pmid | 33339292 | - |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.fulltext | With Fulltext | - |
item.languageiso639-1 | en | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.openairetype | artículo | - |
item.cerifentitytype | Publications | - |
item.grantfulltext | open | - |
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Potential_Coll_Art2020.pdf | 3,51 MB | Adobe PDF | Visualizar/Abrir |
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