Non‐canonical cMet regulation by vimentin mediates Plk1 inhibitor–induced apoptosis

Abstract To address the need for improved systemic therapy for non–small‐cell lung cancer (NSCLC), we previously demonstrated that mesenchymal NSCLC was sensitive to polo‐like kinase (Plk1) inhibitors, but the mechanisms of resistance in epithelial NSCLC remain unknown. Here, we show that cMet was d...

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Main Authors: Ratnakar Singh, Shaohua Peng, Pavitra Viswanath, Vaishnavi Sambandam, Li Shen, Xiayu Rao, Bingliang Fang, Jing Wang, Faye M Johnson
Format: Article
Language:English
Published: Springer Nature 2019-04-01
Series:EMBO Molecular Medicine
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Online Access:https://doi.org/10.15252/emmm.201809960
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author Ratnakar Singh
Shaohua Peng
Pavitra Viswanath
Vaishnavi Sambandam
Li Shen
Xiayu Rao
Bingliang Fang
Jing Wang
Faye M Johnson
author_facet Ratnakar Singh
Shaohua Peng
Pavitra Viswanath
Vaishnavi Sambandam
Li Shen
Xiayu Rao
Bingliang Fang
Jing Wang
Faye M Johnson
author_sort Ratnakar Singh
collection DOAJ
description Abstract To address the need for improved systemic therapy for non–small‐cell lung cancer (NSCLC), we previously demonstrated that mesenchymal NSCLC was sensitive to polo‐like kinase (Plk1) inhibitors, but the mechanisms of resistance in epithelial NSCLC remain unknown. Here, we show that cMet was differentially regulated in isogenic pairs of epithelial and mesenchymal cell lines. Plk1 inhibition inhibits cMet phosphorylation only in mesenchymal cells. Constitutively active cMet abrogates Plk1 inhibitor–induced apoptosis. Likewise, cMet silencing or inhibition enhances Plk1 inhibitor–induced apoptosis. Cells with acquired resistance to Plk1 inhibitors are more epithelial than their parental cells and maintain cMet activation after Plk1 inhibition. In four animal NSCLC models, mesenchymal tumors were more sensitive to Plk1 inhibition alone than were epithelial tumors. The combination of cMet and Plk1 inhibition led to regression of tumors that did not regrow when drug treatment was stopped. Plk1 inhibition did not affect HGF levels but did decrease vimentin phosphorylation, which regulates cMet phosphorylation via β1‐integrin. This research defines a heretofore unknown mechanism of ligand‐independent activation of cMet downstream of Plk1 and an effective combination therapy.
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spelling doaj-art-4246619e4ece41939b17304846962bc42025-08-20T02:11:22ZengSpringer NatureEMBO Molecular Medicine1757-46761757-46842019-04-0111512010.15252/emmm.201809960Non‐canonical cMet regulation by vimentin mediates Plk1 inhibitor–induced apoptosisRatnakar Singh0Shaohua Peng1Pavitra Viswanath2Vaishnavi Sambandam3Li Shen4Xiayu Rao5Bingliang Fang6Jing Wang7Faye M Johnson8Department of Thoracic/Head & Neck Medical Oncology, The University of Texas MD Anderson Cancer CenterDepartment of Thoracic/Head & Neck Medical Oncology, The University of Texas MD Anderson Cancer CenterDepartment of Thoracic/Head & Neck Medical Oncology, The University of Texas MD Anderson Cancer CenterDepartment of Thoracic/Head & Neck Medical Oncology, The University of Texas MD Anderson Cancer CenterDepartment of Bioinformatics and Computational Biology, The University of Texas MD Anderson Cancer CenterDepartment of Bioinformatics and Computational Biology, The University of Texas MD Anderson Cancer CenterDepartment of Thoracic and Cardiovascular Surgery, The University of Texas MD Anderson Cancer CenterThe University of Texas MD Anderson Cancer Center Graduate School of Biomedical SciencesDepartment of Thoracic/Head & Neck Medical Oncology, The University of Texas MD Anderson Cancer CenterAbstract To address the need for improved systemic therapy for non–small‐cell lung cancer (NSCLC), we previously demonstrated that mesenchymal NSCLC was sensitive to polo‐like kinase (Plk1) inhibitors, but the mechanisms of resistance in epithelial NSCLC remain unknown. Here, we show that cMet was differentially regulated in isogenic pairs of epithelial and mesenchymal cell lines. Plk1 inhibition inhibits cMet phosphorylation only in mesenchymal cells. Constitutively active cMet abrogates Plk1 inhibitor–induced apoptosis. Likewise, cMet silencing or inhibition enhances Plk1 inhibitor–induced apoptosis. Cells with acquired resistance to Plk1 inhibitors are more epithelial than their parental cells and maintain cMet activation after Plk1 inhibition. In four animal NSCLC models, mesenchymal tumors were more sensitive to Plk1 inhibition alone than were epithelial tumors. The combination of cMet and Plk1 inhibition led to regression of tumors that did not regrow when drug treatment was stopped. Plk1 inhibition did not affect HGF levels but did decrease vimentin phosphorylation, which regulates cMet phosphorylation via β1‐integrin. This research defines a heretofore unknown mechanism of ligand‐independent activation of cMet downstream of Plk1 and an effective combination therapy.https://doi.org/10.15252/emmm.201809960cMetdrug combinationNSCLCPlk1vimentin
spellingShingle Ratnakar Singh
Shaohua Peng
Pavitra Viswanath
Vaishnavi Sambandam
Li Shen
Xiayu Rao
Bingliang Fang
Jing Wang
Faye M Johnson
Non‐canonical cMet regulation by vimentin mediates Plk1 inhibitor–induced apoptosis
EMBO Molecular Medicine
cMet
drug combination
NSCLC
Plk1
vimentin
title Non‐canonical cMet regulation by vimentin mediates Plk1 inhibitor–induced apoptosis
title_full Non‐canonical cMet regulation by vimentin mediates Plk1 inhibitor–induced apoptosis
title_fullStr Non‐canonical cMet regulation by vimentin mediates Plk1 inhibitor–induced apoptosis
title_full_unstemmed Non‐canonical cMet regulation by vimentin mediates Plk1 inhibitor–induced apoptosis
title_short Non‐canonical cMet regulation by vimentin mediates Plk1 inhibitor–induced apoptosis
title_sort non canonical cmet regulation by vimentin mediates plk1 inhibitor induced apoptosis
topic cMet
drug combination
NSCLC
Plk1
vimentin
url https://doi.org/10.15252/emmm.201809960
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AT shaohuapeng noncanonicalcmetregulationbyvimentinmediatesplk1inhibitorinducedapoptosis
AT pavitraviswanath noncanonicalcmetregulationbyvimentinmediatesplk1inhibitorinducedapoptosis
AT vaishnavisambandam noncanonicalcmetregulationbyvimentinmediatesplk1inhibitorinducedapoptosis
AT lishen noncanonicalcmetregulationbyvimentinmediatesplk1inhibitorinducedapoptosis
AT xiayurao noncanonicalcmetregulationbyvimentinmediatesplk1inhibitorinducedapoptosis
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