Following nearly two decades of development, significant advancements have been achieved in PROTAC technology. As of the end of 2022, more than 20 drugs have entered clinical trials, with ARV-471 targeting estrogen receptor (ER) showing remarkable progress by entering phase III clinical studies. In 2022, significant progress has been made on multiple targets. The first reversible covalent degrader designed to target the KRASG12C mutant protein, based on cyclopropionamide, has been reported. Additionally, the activity HDCA1 degrader surpassed submicromolar levels during the same year. A novel FEM1B covalent ligand called EN106 was also discovered, expanding the range of available ligands. Furthermore, the first PROTAC drug targeting SOS1 was reported. Additionally, the first-in-class degraders that specifically target BRD4 isoforms (BRD4 L and BRD4 S) have recently been reported, providing a valuable tool for further investigating the biological functions of these isoforms. Lastly, a breakthrough was also achieved with the first degrader targeting both CDK9 and Cyclin T1. In this review, we aimed to update the PROTAC degraders as potential anticancer agents covering articles published in 2022. The design strategies, degradation effects, and anticancer activities were highlighted, which might provide an updated sight to develop novel PROTAC degraders with great potential as anticancer agents as well as favorable drug-like properties.

Xiao Wang

Zhao-Long Qin

Na Li

Mei-Qi Jia

Qiu-Ge Liu

Yi-Ru Bai

Jian Song

Shuo Yuan

Sai-Yang Zhang

European journal of medicinal chemistry

《欧洲药物化学杂志》是一本全球性期刊，发表关于药物化学各个方面的研究。它为发表原创论文提供了一个媒介，也欢迎评论性的论文。典型的论文将报告化合物的有机合成、表征和药理学评价。其他感兴趣的主题是药物设计、QSAR、分子建模、药物-受体相互作用、药物代谢的分子方面、前药合成和药物靶向。该杂志希望手稿能够展示研究的合理性，提供对化合物设计或机制理解的洞察力，或阐明目标。

The European Journal of Medicinal Chemistry is a global journal that focuses on various aspects of medicinal chemistry. It provides a platform for the publication of original research papers and also welcomes review articles. Typical research papers report on the organic synthesis, characterization, and pharmacological evaluation of compounds. Other relevant topics include drug design, quantitative structure-activity relationships (QSAR), molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis, and drug targeting. The journal encourages manuscripts that demonstrate the rationale of the research, provide insights into compound design or mechanistic understanding, or clarify the objectives of the study.

《欧洲药物化学杂志》是一本全球性的期刊，专注于药物化学的各个方面。它为原创研究论文提供了一个发表平台，同时也欢迎评论性论文。典型的研究论文通常会报告化合物的有机合成、表征及药理学评估。其他相关主题包括药物设计、定量构效关系（QSAR）、分子建模、药物与受体的相互作用、药物代谢的分子机制、前药合成以及药物靶向。该杂志希望手稿能够展示研究的合理性，提供对化合物设计或机制理解的深刻见解，或阐明研究目标。

European Journal of Medicinal Chemistry

Eur J Med Chem

Annual review of PROTAC degraders as anticancer agents in 2022.

The design strategies, degradation effects, and anticancer activities were highlighted, which might provide an updated sight to develop novel PROTAC degraders with great potential as anticancer agents as well as favorable drug-like properties.

Category	Quartile
医学	2
医学, 药物化学	1

Annual review of PROTAC degraders as anticancer agents in 2022.

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Journal Info

Category	Quartile
CHEMISTRY, MEDICINAL	1