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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Main Authors: Angeles C. Tecalco-Cruz, Jesús Zepeda-Cervantes, Josué O. Ramírez-Jarquín, Alberto Rojas-Ochoa
Format: Article
Language:English
Published: Open Exploration Publishing Inc. 2021-12-01
Series:Exploration of Targeted Anti-tumor Therapy
Subjects:
Online Access:https://www.explorationpub.com/Journals/etat/Article/100260
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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
collection DOAJ
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.
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spelling doaj.art-cde825929f7b48548b8659148429155f2022-12-21T18:44:55ZengOpen Exploration Publishing Inc.Exploration of Targeted Anti-tumor Therapy2692-31142021-12-012649651010.37349/etat.2021.00060Proteolysis-targeting chimeras and their implications in breast cancerAngeles C. Tecalco-Cruz0https://orcid.org/0000-0001-9199-3834Jesús Zepeda-Cervantes1https://orcid.org/0000-0003-2069-2027Josué O. Ramírez-Jarquín2https://orcid.org/0000-0001-7574-8724Alberto Rojas-Ochoa3https://orcid.org/0000-0002-7115-9882Programa en Ciencias Genómicas, Universidad Autónoma de la Ciudad de México (UACM), CDMX, Mexico City 03100, MexicoDepartamento de Microbiología e Inmunología, Facultad de Medicina Veterinaria y Zootecnia, Universidad Nacional Autónoma de México (UNAM), CDMX, Mexico City 04510, MexicoInstituto de Fisiología Celular, Universidad Nacional Autónoma de México (UNAM), CDMX, Mexico City 04500, MexicoInstituto Nacional de Pediatría (INP), CDMX, Mexico City 04530, MexicoBreast 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.https://www.explorationpub.com/Journals/etat/Article/100260estrogen receptor alphabreast cancerdegradation via the ubiquitin-proteasome systemproteolysis-targeting chimeras
spellingShingle Angeles C. Tecalco-Cruz
Jesús Zepeda-Cervantes
Josué O. Ramírez-Jarquín
Alberto Rojas-Ochoa
Proteolysis-targeting chimeras and their implications in breast cancer
Exploration of Targeted Anti-tumor Therapy
estrogen receptor alpha
breast cancer
degradation via the ubiquitin-proteasome system
proteolysis-targeting chimeras
title 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_short Proteolysis-targeting chimeras and their implications in breast cancer
title_sort proteolysis targeting chimeras and their implications in breast cancer
topic estrogen receptor alpha
breast cancer
degradation via the ubiquitin-proteasome system
proteolysis-targeting chimeras
url https://www.explorationpub.com/Journals/etat/Article/100260
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AT jesuszepedacervantes proteolysistargetingchimerasandtheirimplicationsinbreastcancer
AT josueoramirezjarquin proteolysistargetingchimerasandtheirimplicationsinbreastcancer
AT albertorojasochoa proteolysistargetingchimerasandtheirimplicationsinbreastcancer