Proteolysis-targeting chimeras and their implications in breast cancer

Breast cancer (BC) is a highly heterogeneous neoplasm of the mammary tissue, causing the deaths of a large number of women worldwide. Nearly 70% and 20% of BC cases are estrogen receptor alpha positive (ERα+) and human epidermal growth factor receptor 2-positive (HER2+), respectively; therefore, ER...

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Autores principales: Angeles C. Tecalco-Cruz, Jesús Zepeda-Cervantes, Josué O. Ramírez-Jarquín, Alberto Rojas-Ochoa
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Publicado: Open Exploration Publishing Inc. 2021
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Acceso en línea:https://doaj.org/article/cde825929f7b48548b8659148429155f
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spelling oai:doaj.org-article:cde825929f7b48548b8659148429155f2021-11-17T01:48:03ZProteolysis-targeting chimeras and their implications in breast cancer10.37349/etat.2021.000602692-3114https://doaj.org/article/cde825929f7b48548b8659148429155f2021-11-01T00:00:00Zhttps://www.explorationpub.com/Journals/etat/Article/100260https://doaj.org/toc/2692-3114Breast cancer (BC) is a highly heterogeneous neoplasm of the mammary tissue, causing the deaths of a large number of women worldwide. Nearly 70% and 20% of BC cases are estrogen receptor alpha positive (ERα+) and human epidermal growth factor receptor 2-positive (HER2+), respectively; therefore, ER and HER2 targeted therapies have been employed in BC treatment. However, resistance to these therapies has been reported, indicating a need for developing novel therapeutic strategies. Proteolysis-targeting chimeras (PROTACs) are new, promising therapeutic tools designed with a bimodular structure: one module allows specific binding to target proteins, and the other module allows efficient degradation of these target proteins. In this paper, PROTACs and their potential in controlling the progression of ERα and HER2+ BC are discussed.Angeles C. Tecalco-CruzJesús Zepeda-CervantesJosué O. Ramírez-JarquínAlberto Rojas-OchoaOpen Exploration Publishing Inc.articleestrogen receptor alphabreast cancerdegradation via the ubiquitin-proteasome systemproteolysis-targeting chimerasInternal medicineRC31-1245ENExploration of Targeted Anti-tumor Therapy, Vol 2, Iss 6 (2021)
institution DOAJ
collection DOAJ
language EN
topic estrogen receptor alpha
breast cancer
degradation via the ubiquitin-proteasome system
proteolysis-targeting chimeras
Internal medicine
RC31-1245
spellingShingle estrogen receptor alpha
breast cancer
degradation via the ubiquitin-proteasome system
proteolysis-targeting chimeras
Internal medicine
RC31-1245
Angeles C. Tecalco-Cruz
Jesús Zepeda-Cervantes
Josué O. Ramírez-Jarquín
Alberto Rojas-Ochoa
Proteolysis-targeting chimeras and their implications in breast cancer
description Breast cancer (BC) is a highly heterogeneous neoplasm of the mammary tissue, causing the deaths of a large number of women worldwide. Nearly 70% and 20% of BC cases are estrogen receptor alpha positive (ERα+) and human epidermal growth factor receptor 2-positive (HER2+), respectively; therefore, ER and HER2 targeted therapies have been employed in BC treatment. However, resistance to these therapies has been reported, indicating a need for developing novel therapeutic strategies. Proteolysis-targeting chimeras (PROTACs) are new, promising therapeutic tools designed with a bimodular structure: one module allows specific binding to target proteins, and the other module allows efficient degradation of these target proteins. In this paper, PROTACs and their potential in controlling the progression of ERα and HER2+ BC are discussed.
format article
author Angeles C. Tecalco-Cruz
Jesús Zepeda-Cervantes
Josué O. Ramírez-Jarquín
Alberto Rojas-Ochoa
author_facet Angeles C. Tecalco-Cruz
Jesús Zepeda-Cervantes
Josué O. Ramírez-Jarquín
Alberto Rojas-Ochoa
author_sort Angeles C. Tecalco-Cruz
title Proteolysis-targeting chimeras and their implications in breast cancer
title_short Proteolysis-targeting chimeras and their implications in breast cancer
title_full Proteolysis-targeting chimeras and their implications in breast cancer
title_fullStr Proteolysis-targeting chimeras and their implications in breast cancer
title_full_unstemmed Proteolysis-targeting chimeras and their implications in breast cancer
title_sort proteolysis-targeting chimeras and their implications in breast cancer
publisher Open Exploration Publishing Inc.
publishDate 2021
url https://doaj.org/article/cde825929f7b48548b8659148429155f
work_keys_str_mv AT angelesctecalcocruz proteolysistargetingchimerasandtheirimplicationsinbreastcancer
AT jesuszepedacervantes proteolysistargetingchimerasandtheirimplicationsinbreastcancer
AT josueoramirezjarquin proteolysistargetingchimerasandtheirimplicationsinbreastcancer
AT albertorojasochoa proteolysistargetingchimerasandtheirimplicationsinbreastcancer
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