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Targeting Oncoproteins for Degradation by Small Molecule-Based Proteolysis-Targeting Chimeras (PROTACs) in Sex Hormone-Dependent Cancers.

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收录情况： ◇ SCIE

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机构： [1]Department of Clinical Pharmacy, Sichuan Cancer Hospital & Institute, Sichuan Cancer Center, School of Medicine, University of Electronic Science and Technology of China, Chengdu, China, [2]Department of Dermatology, The Affiliated Hospital of Southwest Medical University, Luzhou, China, [3]Department of Gynecology, People’s Hospital of Henan University, Henan Provincial People’s Hospital, Zhengzhou, China

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关键词： sex hormone-dependent cancers PROTACs small molecule inhibitors estrogen receptors androgen receptors

摘要：

Sex hormone-dependent cancers, including breast, ovary, and prostate cancer, contribute to the high number of cancer-related deaths worldwide. Steroid hormones promote tumor occurrence, development, and metastasis by acting on receptors, such as estrogen receptors (ERs), androgen receptors (ARs), and estrogen-related receptors (ERRs). Therefore, endocrine therapy targeting ERs, ARs, and ERRs represents the potential and pivotal therapeutic strategy in sex hormone-dependent cancers. Proteolysis-targeting chimeras (PROTACs) are a novel strategy that can harness the potential of the endogenous ubiquitin-proteasome system (UPS) to target and degrade specific proteins, rather than simply inhibiting the activity of target proteins. Small molecule PROTACs degrade a variety of proteins in cells, mice, and humans and are an emerging approach for novel drug development. PROTACs targeting ARs, ERs, ERRs, and other proteins in sex hormone-dependent cancers have been reported and may overcome the problem of resistance to existing endocrine therapy and receptor antagonist treatments. This review briefly introduces the PROTAC strategy and summarizes the progress on the development of small molecule PROTACs targeting oncoproteins in sex hormone-dependent cancers, focusing on breast and prostate cancers.Copyright © 2022 Liu, Shi, Wang, Zeng, Wang, Xiao and Zhu.

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基金编号： grant number YB2021024

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出版当年[2022]版：

大类 | 2 区医学

小类 | 2 区内分泌学与代谢

最新[2023]版：

大类 | 2 区医学

小类 | 2 区内分泌学与代谢

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出版当年[2022]版：

Q1 ENDOCRINOLOGY & METABOLISM

最新[2023]版：

Q2 ENDOCRINOLOGY & METABOLISM

影响因子： 3.9 最新[2023版] 4.9 最新五年平均 5.2 出版当年[2022版] 5.9 出版当年五年平均 6.055 出版前一年[2021版] 3.9 出版后一年[2023版]

第一作者：

第一作者机构： [1]Department of Clinical Pharmacy, Sichuan Cancer Hospital & Institute, Sichuan Cancer Center, School of Medicine, University of Electronic Science and Technology of China, Chengdu, China, [2]Department of Dermatology, The Affiliated Hospital of Southwest Medical University, Luzhou, China,

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Targeting Oncoproteins for Degradation by Small Molecule-Based Proteolysis-Targeting Chimeras (PROTACs) in Sex Hormone-Dependent Cancers.

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