Protein arginine methyltransferase 5: A novel therapeutic target for triple‐negative breast cancers

Abstract TNBC is a highly heterogeneous and aggressive breast cancer subtype associated with high relapse rates, and for which no targeted therapy yet exists. Protein arginine methyltransferase 5 (PRMT5), an enzyme which catalyzes the methylation of arginines on histone and non‐histone proteins, has...

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Main Authors: Mathilde Vinet, Samyuktha Suresh, Virginie Maire, Clarisse Monchecourt, Fariba Némati, Laetitia Lesage, Fabienne Pierre, Mengliang Ye, Auriane Lescure, Amélie Brisson, Didier Meseure, André Nicolas, Guillem Rigaill, Elisabetta Marangoni, Elaine Del Nery, Sergio Roman‐Roman, Thierry Dubois
Format: Article
Language:English
Published: Wiley 2019-05-01
Series:Cancer Medicine
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Online Access:https://doi.org/10.1002/cam4.2114
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author Mathilde Vinet
Samyuktha Suresh
Virginie Maire
Clarisse Monchecourt
Fariba Némati
Laetitia Lesage
Fabienne Pierre
Mengliang Ye
Auriane Lescure
Amélie Brisson
Didier Meseure
André Nicolas
Guillem Rigaill
Elisabetta Marangoni
Elaine Del Nery
Sergio Roman‐Roman
Thierry Dubois
author_facet Mathilde Vinet
Samyuktha Suresh
Virginie Maire
Clarisse Monchecourt
Fariba Némati
Laetitia Lesage
Fabienne Pierre
Mengliang Ye
Auriane Lescure
Amélie Brisson
Didier Meseure
André Nicolas
Guillem Rigaill
Elisabetta Marangoni
Elaine Del Nery
Sergio Roman‐Roman
Thierry Dubois
author_sort Mathilde Vinet
collection DOAJ
description Abstract TNBC is a highly heterogeneous and aggressive breast cancer subtype associated with high relapse rates, and for which no targeted therapy yet exists. Protein arginine methyltransferase 5 (PRMT5), an enzyme which catalyzes the methylation of arginines on histone and non‐histone proteins, has recently emerged as a putative target for cancer therapy. Potent and specific PRMT5 inhibitors have been developed, but the therapeutic efficacy of PRMT5 targeting in TNBC has not yet been demonstrated. Here, we examine the expression of PRMT5 in a human breast cancer cohort obtained from the Institut Curie, and evaluate the therapeutic potential of pharmacological inhibition of PRMT5 in TNBC. We find that PRMT5 mRNA and protein are expressed at comparable levels in TNBC, luminal breast tumors, and healthy mammary tissues. However, immunohistochemistry analyses reveal that PRMT5 is differentially localized in TNBC compared to other breast cancer subtypes and to normal breast tissues. PRMT5 is heterogeneously expressed in TNBC and high PRMT5 expression correlates with poor prognosis within this breast cancer subtype. Using the small‐molecule inhibitor EPZ015666, we show that PRMT5 inhibition impairs cell proliferation in a subset of TNBC cell lines. PRMT5 inhibition triggers apoptosis, regulates cell cycle progression and decreases mammosphere formation. Furthermore, EPZ015666 administration to a patient‐derived xenograft model of TNBC significantly deters tumor progression. Finally, we reveal potentiation between EGFR and PRMT5 targeting, suggestive of a beneficial combination therapy. Our findings highlight a distinctive subcellular localization of PRMT5 in TNBC, and uphold PRMT5 targeting, alone or in combination, as a relevant treatment strategy for a subset of TNBC.
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spelling doaj-art-e38d40999951432e94d1e8844dc31f542024-11-15T13:01:04ZengWileyCancer Medicine2045-76342019-05-01852414242810.1002/cam4.2114Protein arginine methyltransferase 5: A novel therapeutic target for triple‐negative breast cancersMathilde Vinet0Samyuktha Suresh1Virginie Maire2Clarisse Monchecourt3Fariba Némati4Laetitia Lesage5Fabienne Pierre6Mengliang Ye7Auriane Lescure8Amélie Brisson9Didier Meseure10André Nicolas11Guillem Rigaill12Elisabetta Marangoni13Elaine Del Nery14Sergio Roman‐Roman15Thierry Dubois16Translational Research Department Institut Curie, PSL Research University Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FrancePlatform of Investigative Pathology, Department of Pathology Institut Curie Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FrancePlatform of Investigative Pathology, Department of Pathology Institut Curie Paris FrancePlatform of Investigative Pathology, Department of Pathology Institut Curie Paris FranceInstitute of Plant Sciences Paris‐Saclay (IPS2), UMR 9213, UMR1403, CNRS, INRA Université Paris‐Sud, Université d'Evry, Université Paris‐Diderot, Sorbonne, Paris‐Cité Orsay FranceTranslational Research Department Institut Curie, PSL Research University Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FranceTranslational Research Department Institut Curie, PSL Research University Paris FranceAbstract TNBC is a highly heterogeneous and aggressive breast cancer subtype associated with high relapse rates, and for which no targeted therapy yet exists. Protein arginine methyltransferase 5 (PRMT5), an enzyme which catalyzes the methylation of arginines on histone and non‐histone proteins, has recently emerged as a putative target for cancer therapy. Potent and specific PRMT5 inhibitors have been developed, but the therapeutic efficacy of PRMT5 targeting in TNBC has not yet been demonstrated. Here, we examine the expression of PRMT5 in a human breast cancer cohort obtained from the Institut Curie, and evaluate the therapeutic potential of pharmacological inhibition of PRMT5 in TNBC. We find that PRMT5 mRNA and protein are expressed at comparable levels in TNBC, luminal breast tumors, and healthy mammary tissues. However, immunohistochemistry analyses reveal that PRMT5 is differentially localized in TNBC compared to other breast cancer subtypes and to normal breast tissues. PRMT5 is heterogeneously expressed in TNBC and high PRMT5 expression correlates with poor prognosis within this breast cancer subtype. Using the small‐molecule inhibitor EPZ015666, we show that PRMT5 inhibition impairs cell proliferation in a subset of TNBC cell lines. PRMT5 inhibition triggers apoptosis, regulates cell cycle progression and decreases mammosphere formation. Furthermore, EPZ015666 administration to a patient‐derived xenograft model of TNBC significantly deters tumor progression. Finally, we reveal potentiation between EGFR and PRMT5 targeting, suggestive of a beneficial combination therapy. Our findings highlight a distinctive subcellular localization of PRMT5 in TNBC, and uphold PRMT5 targeting, alone or in combination, as a relevant treatment strategy for a subset of TNBC.https://doi.org/10.1002/cam4.2114breast cancermolecular biologytargeted therapytranslational research
spellingShingle Mathilde Vinet
Samyuktha Suresh
Virginie Maire
Clarisse Monchecourt
Fariba Némati
Laetitia Lesage
Fabienne Pierre
Mengliang Ye
Auriane Lescure
Amélie Brisson
Didier Meseure
André Nicolas
Guillem Rigaill
Elisabetta Marangoni
Elaine Del Nery
Sergio Roman‐Roman
Thierry Dubois
Protein arginine methyltransferase 5: A novel therapeutic target for triple‐negative breast cancers
Cancer Medicine
breast cancer
molecular biology
targeted therapy
translational research
title Protein arginine methyltransferase 5: A novel therapeutic target for triple‐negative breast cancers
title_full Protein arginine methyltransferase 5: A novel therapeutic target for triple‐negative breast cancers
title_fullStr Protein arginine methyltransferase 5: A novel therapeutic target for triple‐negative breast cancers
title_full_unstemmed Protein arginine methyltransferase 5: A novel therapeutic target for triple‐negative breast cancers
title_short Protein arginine methyltransferase 5: A novel therapeutic target for triple‐negative breast cancers
title_sort protein arginine methyltransferase 5 a novel therapeutic target for triple negative breast cancers
topic breast cancer
molecular biology
targeted therapy
translational research
url https://doi.org/10.1002/cam4.2114
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