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Article: Functional characterization of CFI-400945, a polo-like kinase 4 inhibitor, as a potential anticancer agent

TitleFunctional characterization of CFI-400945, a polo-like kinase 4 inhibitor, as a potential anticancer agent
Authors
Issue Date2014
Citation
Cancer Cell, 2014, v. 26, n. 2, p. 163-176 How to Cite?
AbstractPLK4 was identified as a promising therapeutic target through a systematic approach that combined RNAi screening with gene expression analysis in human breast cancers and cell lines. A drug discovery program culminated in CFI-400945, a potent and selective PLK4 inhibitor. Cancer cells treated with CFI-400945 exhibit effects consistent with PLK4 kinase inhibition, including dysregulated centriole duplication, mitotic defects, and cell death. Oral administration of CFI-400945 to mice bearing human cancer xenografts results in the significant inhibition of tumor growth at doses that are well tolerated. Increased antitumor activity invivo was observed in PTEN-deficient compared to PTEN wild-type cancer xenografts. Our findings provide a rationale for the clinical evaluation of CFI-400945 in patients with solid tumors, in particular those deficient in PTEN. © 2014 Elsevier Inc.
Persistent Identifierhttp://hdl.handle.net/10722/292840
ISSN
2023 Impact Factor: 48.8
2023 SCImago Journal Rankings: 17.507
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorMason, Jacqueline M.-
dc.contributor.authorLin, Dan Chi Chia-
dc.contributor.authorWei, Xin-
dc.contributor.authorChe, Yi-
dc.contributor.authorYao, Yi-
dc.contributor.authorKiarash, Reza-
dc.contributor.authorCescon, David W.-
dc.contributor.authorFletcher, Graham C.-
dc.contributor.authorAwrey, Donald E.-
dc.contributor.authorBray, Mark R.-
dc.contributor.authorPan, Guohua-
dc.contributor.authorMak, Tak W.-
dc.date.accessioned2020-11-17T14:57:19Z-
dc.date.available2020-11-17T14:57:19Z-
dc.date.issued2014-
dc.identifier.citationCancer Cell, 2014, v. 26, n. 2, p. 163-176-
dc.identifier.issn1535-6108-
dc.identifier.urihttp://hdl.handle.net/10722/292840-
dc.description.abstractPLK4 was identified as a promising therapeutic target through a systematic approach that combined RNAi screening with gene expression analysis in human breast cancers and cell lines. A drug discovery program culminated in CFI-400945, a potent and selective PLK4 inhibitor. Cancer cells treated with CFI-400945 exhibit effects consistent with PLK4 kinase inhibition, including dysregulated centriole duplication, mitotic defects, and cell death. Oral administration of CFI-400945 to mice bearing human cancer xenografts results in the significant inhibition of tumor growth at doses that are well tolerated. Increased antitumor activity invivo was observed in PTEN-deficient compared to PTEN wild-type cancer xenografts. Our findings provide a rationale for the clinical evaluation of CFI-400945 in patients with solid tumors, in particular those deficient in PTEN. © 2014 Elsevier Inc.-
dc.languageeng-
dc.relation.ispartofCancer Cell-
dc.titleFunctional characterization of CFI-400945, a polo-like kinase 4 inhibitor, as a potential anticancer agent-
dc.typeArticle-
dc.description.naturelink_to_OA_fulltext-
dc.identifier.doi10.1016/j.ccr.2014.05.006-
dc.identifier.pmid25043604-
dc.identifier.scopuseid_2-s2.0-84905709109-
dc.identifier.volume26-
dc.identifier.issue2-
dc.identifier.spage163-
dc.identifier.epage176-
dc.identifier.eissn1878-3686-
dc.identifier.isiWOS:000340343800006-
dc.identifier.issnl1535-6108-

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