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The first small molecules capable of strongly suppressing proliferation of cancer cells harboring BRAF class I/II/III mutations

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dc.contributor.author심태보-
dc.date.accessioned2020-12-01T17:32:21Z-
dc.date.available2020-12-01T17:32:21Z-
dc.date.issued2020-11-
dc.identifier.issn0006-291X-
dc.identifier.urihttps://ir.ymlib.yonsei.ac.kr/handle/22282913/180321-
dc.description.abstractBRAF mutants are categorized into three classes according to dependency on RAS signaling and RAF dimerization-dependency. Class I BRAF V600 mutants (RAS-independent monomer) are sensitive to vemurafenib. In contrast, both class II mutants (RAS-independent dimer) and class III mutants (RAS-dependent heterodimer) are insensitive to vemurafenib. It is not likely that BRAF inhibitors capable of inhibiting all classes of BRAF mutants are currently available. Herein, we report GNF-7 and its novel derivative, SIJ1227 as the first BRAF inhibitors capable of inhibiting all classes of BRAF mutants. Compared with vemurafenib and PLX8394, both GNF-7 and SIJ1227 possess much more strong anti-proliferative activities on melanoma (A375 and C8161) and lung cancer cells (H1755 and H1666) harboring BRAF V600E (class I mutant), BRAF G464E/G469A (class II mutant) and BRAF G466V (class III mutant), respectively. Also, both GNF-7 and SIJ1227 are capable of inhibiting more strongly colony formation than vemurafenib and PLX8394 in 3D soft agar assay using C8161 melanoma cells. In addition, GNF-7 and SIJ1227 suppress more strongly migration/invasion of these cancer cells than vemurafenib and PLX8394. Taken together, both GNF-7 and SIJ1227 are much superior to vemurafenib and PLX8394 in terms of capability to inhibit all classes of BRAF mutants.-
dc.description.statementOfResponsibilityrestriction-
dc.languageEnglish-
dc.publisherElsevier-
dc.relation.isPartOfBIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS-
dc.rightsCC BY-NC-ND 2.0 KR-
dc.titleThe first small molecules capable of strongly suppressing proliferation of cancer cells harboring BRAF class I/II/III mutations-
dc.typeArticle-
dc.contributor.collegeCollege of Medicine (의과대학)-
dc.contributor.departmentBioMedical Science Institute (의생명과학부)-
dc.contributor.googleauthorSeung-Hye Choi-
dc.contributor.googleauthorInjae Shin-
dc.contributor.googleauthorNamdoo Kim-
dc.contributor.googleauthorYunju Nam-
dc.contributor.googleauthorTaebo Sim-
dc.identifier.doi10.1016/j.bbrc.2020.07.110-
dc.contributor.localIdA05926-
dc.relation.journalcodeJ00281-
dc.identifier.eissn1090-2104-
dc.identifier.pmid32873393-
dc.identifier.urlhttps://www.sciencedirect.com/science/article/pii/S0006291X20315072-
dc.subject.keywordGNF-7-
dc.subject.keywordPan-classes BRAF inhibitor-
dc.subject.keywordType II kinase inhibitor-
dc.contributor.alternativeNameSim, Taebo-
dc.contributor.affiliatedAuthor심태보-
dc.citation.volume532-
dc.citation.number2-
dc.citation.startPage315-
dc.citation.endPage320-
dc.identifier.bibliographicCitationBIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, Vol.532(2) : 315-320, 2020-11-
Appears in Collections:
1. College of Medicine (의과대학) > BioMedical Science Institute (의생명과학부) > 1. Journal Papers

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