Cited 6 times in
Combination of Type I and Type II MET Tyrosine Kinase Inhibitors as Therapeutic Approach to Prevent Resistance
DC Field | Value | Language |
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dc.contributor.author | 심태보 | - |
dc.date.accessioned | 2022-05-09T17:24:42Z | - |
dc.date.available | 2022-05-09T17:24:42Z | - |
dc.date.issued | 2022-02 | - |
dc.identifier.issn | 1535-7163 | - |
dc.identifier.uri | https://ir.ymlib.yonsei.ac.kr/handle/22282913/188552 | - |
dc.description.abstract | MET-targeted therapies are clinically effective in MET-amplified and MET exon 14 deletion mutant (METex14) non-small cell lung cancers (NSCLCs), but their efficacy is limited by the development of drug resistance. Structurally distinct MET tyrosine kinase inhibitors (TKIs) (type I/II) have been developed or are under clinical evaluation, which may overcome MET-mediated drug resistance mechanisms. In this study, we assess secondary MET mutations likely to emerge in response to treatment with single-agent or combinations of type I/type II MET TKIs using TPR-MET transformed Ba/F3 cell mutagenesis assays. We found that these inhibitors gave rise to distinct secondary MET mutant profiles. However, a combination of type I/II TKI inhibitors (capmatinib and merestinib) yielded no resistant clones in vitro The combination of capmatinib/merestinib was evaluated in vivo and led to a significant reduction in tumor outgrowth compared with either MET inhibitor alone. Our findings demonstrate in vitro and in vivo that a simultaneous treatment with a type I and type II MET TKI may be a clinically viable approach to delay and/or diminish the emergence of on target MET-mediated drug-resistance mutations. | - |
dc.description.statementOfResponsibility | restriction | - |
dc.language | English | - |
dc.publisher | American Association for Cancer Research | - |
dc.relation.isPartOf | MOLECULAR CANCER THERAPEUTICS | - |
dc.rights | CC BY-NC-ND 2.0 KR | - |
dc.subject.MESH | Animals | - |
dc.subject.MESH | Drug Resistance, Neoplasm / drug effects* | - |
dc.subject.MESH | Female | - |
dc.subject.MESH | High-Throughput Nucleotide Sequencing / methods* | - |
dc.subject.MESH | Humans | - |
dc.subject.MESH | Mice | - |
dc.subject.MESH | Molecular Docking Simulation / methods* | - |
dc.subject.MESH | Protein Kinase Inhibitors / pharmacology | - |
dc.subject.MESH | Protein Kinase Inhibitors / therapeutic use* | - |
dc.title | Combination of Type I and Type II MET Tyrosine Kinase Inhibitors as Therapeutic Approach to Prevent Resistance | - |
dc.type | Article | - |
dc.contributor.college | College of Medicine (의과대학) | - |
dc.contributor.department | BioMedical Science Institute (의생명과학부) | - |
dc.contributor.googleauthor | Magda Bahcall | - |
dc.contributor.googleauthor | Cloud P Paweletz | - |
dc.contributor.googleauthor | Yanan Kuang | - |
dc.contributor.googleauthor | Luke J Taus | - |
dc.contributor.googleauthor | Taebo Sim | - |
dc.contributor.googleauthor | Nam Doo Kim | - |
dc.contributor.googleauthor | Kshiti H Dholakia | - |
dc.contributor.googleauthor | Christie J Lau | - |
dc.contributor.googleauthor | Prafulla C Gokhale | - |
dc.contributor.googleauthor | Pratik R Chopade | - |
dc.contributor.googleauthor | Fangxin Hong | - |
dc.contributor.googleauthor | Zihan Wei | - |
dc.contributor.googleauthor | Jens Köhler | - |
dc.contributor.googleauthor | Paul T Kirschmeier | - |
dc.contributor.googleauthor | Jiannan Guo | - |
dc.contributor.googleauthor | Sujuan Guo | - |
dc.contributor.googleauthor | Stephen Wang | - |
dc.contributor.googleauthor | Pasi A Jänne | - |
dc.identifier.doi | 10.1158/1535-7163.MCT-21-0344 | - |
dc.contributor.localId | A05926 | - |
dc.relation.journalcode | J02254 | - |
dc.identifier.eissn | 1538-8514 | - |
dc.identifier.pmid | 34789563 | - |
dc.identifier.url | https://aacrjournals.org/mct/article/21/2/322/678522/Combination-of-Type-I-and-Type-II-MET-Tyrosine | - |
dc.contributor.alternativeName | Sim, Taebo | - |
dc.contributor.affiliatedAuthor | 심태보 | - |
dc.citation.volume | 21 | - |
dc.citation.number | 2 | - |
dc.citation.startPage | 322 | - |
dc.citation.endPage | 335 | - |
dc.identifier.bibliographicCitation | MOLECULAR CANCER THERAPEUTICS, Vol.21(2) : 322-335, 2022-02 | - |
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