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癌症表观遗传疗法：最新进展、挑战与新机遇

Cancer epigenetic therapy: recent advances, challenges, and emerging opportunities.

作者信息

Vatapalli Rajita, Rossi Alex P, Chan Ho Man, Zhang Jingwen

机构信息

AstraZeneca, Oncology Research and Development, Waltham, MA, USA.

Biology, Flare Therapeutics, Cambridge, MA, USA.

出版信息

Epigenomics. 2025 Jan;17(1):59-74. doi: 10.1080/17501911.2024.2430169. Epub 2024 Nov 27.

DOI:10.1080/17501911.2024.2430169
PMID:39601374
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11702999/
Abstract

Epigenetic dysregulation is an important nexus in the development and maintenance of human cancers. This review provides an overview of how understanding epigenetic dysregulation in cancers has led to insights for novel cancer therapy development. Over the past two decades, significant strides have been made in drug discovery efforts targeting cancer epigenetic mechanisms, leading to successes in clinical development and approval of cancer epigenetic therapeutics. This article will discuss the current therapeutic rationale guiding the discovery and development of epigenetic therapeutics, key learnings from clinical experiences and new opportunities on the horizon.

摘要

表观遗传失调是人类癌症发生和维持过程中的一个重要环节。本综述概述了对癌症表观遗传失调的理解如何为新型癌症治疗方法的开发提供了见解。在过去二十年中，针对癌症表观遗传机制的药物研发取得了重大进展，促成了癌症表观遗传疗法在临床开发和获批方面的成功。本文将讨论指导表观遗传疗法发现和开发的当前治疗原理、临床经验中的关键经验教训以及即将出现的新机遇。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/716e/11702999/6320e25093ff/IEPI_A_2430169_F0002_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/716e/11702999/a65e84193c61/IEPI_A_2430169_F0001_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/716e/11702999/6320e25093ff/IEPI_A_2430169_F0002_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/716e/11702999/a65e84193c61/IEPI_A_2430169_F0001_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/716e/11702999/6320e25093ff/IEPI_A_2430169_F0002_OC.jpg

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Synthetic lethality: targeting the SMARCA2 bromodomain for degradation in SMARCA4-deficient tumors - a review of patent literature from 2019-June 2023.合成致死性：针对 SMARCA4 缺陷肿瘤中的 SMARCA2 溴结构域进行靶向降解——对 2019 年 6 月至 2023 年的专利文献进行综述。
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