Proteolysis Targeting Chimeras (PROTACs) in Breast Cancer Therapy

IF 3.6 4区医学 Q2 CHEMISTRY, MEDICINAL

ChemMedChem Pub Date : 2024-08-13 DOI:10.1002/cmdc.202400267

Yerim Jin, Yeongju Lee

引用次数: 0

Abstract

Breast cancer (BC) accounts for 30 % of cancer cases among women cancer patients globally, indicating the urgent need for the development of selective therapies targeting BCs. Recently, proteolysis-targeting chimera (PROTAC) has emerged as a promising strategy to target breast cancer. PROTAC is a chimeric molecule consisting of a target protein ligand, an E3 ligase ligand, and conjugating linkers, enabling it to facilitate the degradation of desired target proteins by recruiting E3 ligase in close proximity. Due to the catalytic behavior and direct degradation of BC-causing proteins, PROTAC could achieve high drug efficacy with low doses, drawing great attention for its potential as therapeutics. This review provides cases of the currently developed PROTACs targeting BCs depending on the type of BCs, limitations, and future perspectives of PROTAC in targeting BCs.

Abstract Image

查看原文本刊更多论文

乳腺癌治疗中的蛋白质分解靶向嵌合体 (PROTAC)。

乳腺癌（BC）占全球女性癌症患者的 30%，这表明迫切需要开发针对乳腺癌的选择性疗法。最近，蛋白水解靶向嵌合体（PROTAC）作为一种有前途的靶向乳腺癌的策略出现了。PROTAC是一种嵌合分子，由靶蛋白配体、E3连接酶配体和共轭连接体组成，能够通过招募E3连接酶近距离降解所需的靶蛋白。由于 PROTAC 具有催化行为并能直接降解 BC 致病蛋白，因此能以低剂量实现高药效，其作为治疗药物的潜力备受关注。本综述根据 BCs 的类型、局限性以及 PROTAC 在靶向 BCs 方面的前景，介绍了目前已开发的靶向 BCs 的 PROTAC 案例。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

ChemMedChem 医学-药学

CiteScore

6.70

自引率

2.90%

发文量

280

审稿时长

1 months

期刊介绍： Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs. Contents ChemMedChem publishes an attractive mixture of: Full Papers and Communications Reviews and Minireviews Patent Reviews Highlights and Concepts Book and Multimedia Reviews.