Resistance to CDK4/6 Inhibitors in Estrogen Receptor-Positive Breast Cancer

Estrogen receptor-positive (ER+) breast cancer is the most common form of breast cancer. Antiestrogens were the first therapy aimed at treating this subtype, but resistance to these warranted the development of a new treatment option. CDK4/6 inhibitors address this problem by halting cell cycle prog...

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Autores principales:	Erin R. Scheidemann, Ayesha N. Shajahan-Haq
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	ER+ breast cancer antiestrogens CDK4/6 inhibitors palbociclib ribociclib abemaciclib Biology (General) QH301-705.5 Chemistry QD1-999
Acceso en línea:	https://doaj.org/article/0ae9ff9fe7d845f7bf36575b5236b521
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spelling	oai:doaj.org-article:0ae9ff9fe7d845f7bf36575b5236b5212021-11-25T17:55:07ZResistance to CDK4/6 Inhibitors in Estrogen Receptor-Positive Breast Cancer10.3390/ijms2222122921422-00671661-6596https://doaj.org/article/0ae9ff9fe7d845f7bf36575b5236b5212021-11-01T00:00:00Zhttps://www.mdpi.com/1422-0067/22/22/12292https://doaj.org/toc/1661-6596https://doaj.org/toc/1422-0067Estrogen receptor-positive (ER+) breast cancer is the most common form of breast cancer. Antiestrogens were the first therapy aimed at treating this subtype, but resistance to these warranted the development of a new treatment option. CDK4/6 inhibitors address this problem by halting cell cycle progression in ER+ cells, and have proven to be successful in the clinic. Unfortunately, both intrinsic and acquired resistance to CDK4/6 inhibitors are common. Numerous mechanisms of how resistance occurs have been identified to date, including the activation of prominent growth signaling pathways, the loss of tumor-suppressive genes, and noncanonical cell cycle function. Many of these have been successfully targeted and demonstrate the ability to overcome resistance to CDK4/6 inhibitors in preclinical and clinical trials. Future studies should focus on the development of biomarkers so that patients likely to be resistant to CDK4/6 inhibition can initially be given alternative methods of treatment.Erin R. ScheidemannAyesha N. Shajahan-HaqMDPI AGarticleER+ breast cancerantiestrogensCDK4/6 inhibitorspalbociclibribociclibabemaciclibBiology (General)QH301-705.5ChemistryQD1-999ENInternational Journal of Molecular Sciences, Vol 22, Iss 12292, p 12292 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	ER+ breast cancer antiestrogens CDK4/6 inhibitors palbociclib ribociclib abemaciclib Biology (General) QH301-705.5 Chemistry QD1-999
spellingShingle	ER+ breast cancer antiestrogens CDK4/6 inhibitors palbociclib ribociclib abemaciclib Biology (General) QH301-705.5 Chemistry QD1-999 Erin R. Scheidemann Ayesha N. Shajahan-Haq Resistance to CDK4/6 Inhibitors in Estrogen Receptor-Positive Breast Cancer
description	Estrogen receptor-positive (ER+) breast cancer is the most common form of breast cancer. Antiestrogens were the first therapy aimed at treating this subtype, but resistance to these warranted the development of a new treatment option. CDK4/6 inhibitors address this problem by halting cell cycle progression in ER+ cells, and have proven to be successful in the clinic. Unfortunately, both intrinsic and acquired resistance to CDK4/6 inhibitors are common. Numerous mechanisms of how resistance occurs have been identified to date, including the activation of prominent growth signaling pathways, the loss of tumor-suppressive genes, and noncanonical cell cycle function. Many of these have been successfully targeted and demonstrate the ability to overcome resistance to CDK4/6 inhibitors in preclinical and clinical trials. Future studies should focus on the development of biomarkers so that patients likely to be resistant to CDK4/6 inhibition can initially be given alternative methods of treatment.
format	article
author	Erin R. Scheidemann Ayesha N. Shajahan-Haq
author_facet	Erin R. Scheidemann Ayesha N. Shajahan-Haq
author_sort	Erin R. Scheidemann
title	Resistance to CDK4/6 Inhibitors in Estrogen Receptor-Positive Breast Cancer
title_short	Resistance to CDK4/6 Inhibitors in Estrogen Receptor-Positive Breast Cancer
title_full	Resistance to CDK4/6 Inhibitors in Estrogen Receptor-Positive Breast Cancer
title_fullStr	Resistance to CDK4/6 Inhibitors in Estrogen Receptor-Positive Breast Cancer
title_full_unstemmed	Resistance to CDK4/6 Inhibitors in Estrogen Receptor-Positive Breast Cancer
title_sort	resistance to cdk4/6 inhibitors in estrogen receptor-positive breast cancer
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/0ae9ff9fe7d845f7bf36575b5236b521
work_keys_str_mv	AT erinrscheidemann resistancetocdk46inhibitorsinestrogenreceptorpositivebreastcancer AT ayeshanshajahanhaq resistancetocdk46inhibitorsinestrogenreceptorpositivebreastcancer
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Resistance to CDK4/6 Inhibitors in Estrogen Receptor-Positive Breast Cancer

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