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Article: Targeting therapeutic liabilities engendered by PIK3R1 mutations for cancer treatment

TitleTargeting therapeutic liabilities engendered by PIK3R1 mutations for cancer treatment
Authors
KeywordsPIK3R1
PI3K
MAPK
p85
mutation
targeted therapy
Issue Date2016
Citation
Pharmacogenomics, 2016, v. 17, n. 3, p. 297-307 How to Cite?
Abstract© 2016 Future Medicine Ltd. The regulatory subunit of PI3K, p85α (encoded by PIK3R1), binds, stabilizes and inhibits the PI3K p110 catalytic subunit. Functional characterization of PIK3R1 mutations has identified not only hypomorphs with reduced inhibition of p110, but also hypomorphs and dominant negative mutants that disrupt a novel regulatory role of p85α on PTEN or neomorphs that activate unexpected signaling pathways. The diverse phenotypic spectrum of these PIK3R1 driver mutations underscores the need for different treatment strategies targeting tumors harboring these mutations. This article describes the functional consequences of the spectrum of PIK3R1 driver mutations and therapeutic liabilities they may engender.
Persistent Identifierhttp://hdl.handle.net/10722/225073
ISSN
2015 Impact Factor: 2.71
2015 SCImago Journal Rankings: 0.932

 

DC FieldValueLanguage
dc.contributor.authorCheung, Lydia Wt-
dc.contributor.authorMills, Gordon B.-
dc.date.accessioned2016-04-18T11:16:42Z-
dc.date.available2016-04-18T11:16:42Z-
dc.date.issued2016-
dc.identifier.citationPharmacogenomics, 2016, v. 17, n. 3, p. 297-307-
dc.identifier.issn1462-2416-
dc.identifier.urihttp://hdl.handle.net/10722/225073-
dc.description.abstract© 2016 Future Medicine Ltd. The regulatory subunit of PI3K, p85α (encoded by PIK3R1), binds, stabilizes and inhibits the PI3K p110 catalytic subunit. Functional characterization of PIK3R1 mutations has identified not only hypomorphs with reduced inhibition of p110, but also hypomorphs and dominant negative mutants that disrupt a novel regulatory role of p85α on PTEN or neomorphs that activate unexpected signaling pathways. The diverse phenotypic spectrum of these PIK3R1 driver mutations underscores the need for different treatment strategies targeting tumors harboring these mutations. This article describes the functional consequences of the spectrum of PIK3R1 driver mutations and therapeutic liabilities they may engender.-
dc.languageeng-
dc.relation.ispartofPharmacogenomics-
dc.subjectPIK3R1-
dc.subjectPI3K-
dc.subjectMAPK-
dc.subjectp85-
dc.subjectmutation-
dc.subjecttargeted therapy-
dc.titleTargeting therapeutic liabilities engendered by PIK3R1 mutations for cancer treatment-
dc.typeArticle-
dc.description.natureLink_to_subscribed_fulltext-
dc.identifier.doi10.2217/pgs.15.174-
dc.identifier.scopuseid_2-s2.0-84956633350-
dc.identifier.volume17-
dc.identifier.issue3-
dc.identifier.spage297-
dc.identifier.epage307-
dc.identifier.eissn1744-8042-

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