Please use this identifier to cite or link to this item:
http://hdl.handle.net/2445/190110
Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Pallara, Chiara | - |
dc.contributor.author | Cabot, Débora | - |
dc.contributor.author | Rivas, Josep | - |
dc.contributor.author | Brun, Sonia | - |
dc.contributor.author | Seco, Jesús | - |
dc.contributor.author | Abuasaker, Baraa | - |
dc.contributor.author | Tarragó Clua, Maria Teresa | - |
dc.contributor.author | Jaumot i Pijoan, Montserrat | - |
dc.contributor.author | Prades, Roger | - |
dc.contributor.author | Agell i Jané, Neus | - |
dc.date.accessioned | 2022-10-24T14:31:49Z | - |
dc.date.available | 2022-10-24T14:31:49Z | - |
dc.date.issued | 2022-09-22 | - |
dc.identifier.issn | 2045-2322 | - |
dc.identifier.uri | http://hdl.handle.net/2445/190110 | - |
dc.description.abstract | Oncogenic RAS proteins are important for driving tumour formation, and for maintenance of the transformed phenotype, and thus their relevance as a cancer therapeutic target is undeniable. We focused here on obtaining peptidomimetics, which have good pharmacological properties, to block Ras-effector interaction. Computational analysis was used to identify hot spots of RAS relevant for these interactions and to screen a library of peptidomimetics. Nine compounds were synthesized and assayed for their activity as RAS inhibitors in cultured cells. Most of them induced a reduction in ERK and AKT activation by EGF, a marker of RAS activity. The most potent inhibitor disrupted Raf and PI3K interaction with oncogenic KRAS, corroborating its mechanism of action as an inhibitor of protein-protein interactions, and thus validating our computational methodology. Most interestingly, improvement of one of the compounds allowed us to obtain a peptidomimetic that decreased the survival of pancreatic cancer cell lines harbouring oncogenic KRAS | - |
dc.format.extent | 15 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Nature Publishing Group | - |
dc.relation.isformatof | Reproducció del document publicat a: https://doi.org/10.1038/s41598-022-19703-6 | - |
dc.relation.ispartof | Scientific Reports, 2022, vol. 22, num. 12, p. 15810 | - |
dc.relation.uri | https://doi.org/10.1038/s41598-022-19703-6 | - |
dc.rights | cc-by (c) Pallara, Chiara et al., 2022 | - |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | - |
dc.source | Articles publicats en revistes (Biomedicina) | - |
dc.subject.classification | Càncer | - |
dc.subject.classification | Síntesi de pèptids | - |
dc.subject.classification | Proteïnes ras | - |
dc.subject.classification | Càncer de pàncrees | - |
dc.subject.other | Cancer | - |
dc.subject.other | Peptide synthesis | - |
dc.subject.other | Ras proteins | - |
dc.subject.other | Pancreas cancer | - |
dc.title | Peptidomimetics designed to bind to RAS effector domain are promising cancer therapeutic compounds. | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/publishedVersion | - |
dc.identifier.idgrec | 726101 | - |
dc.date.updated | 2022-10-24T14:31:49Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
dc.identifier.idimarina | 9330814 | - |
dc.identifier.pmid | 36138080 | - |
Appears in Collections: | Articles publicats en revistes (IDIBAPS: Institut d'investigacions Biomèdiques August Pi i Sunyer) Articles publicats en revistes (Biomedicina) |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
726101.pdf | 22.75 MB | Adobe PDF | View/Open |
This item is licensed under a Creative Commons License