利用 PROTACs 靶向可逆的翻译后修饰：以修饰蛋白质赖氨酸和精氨酸残基的酶为重点。
Targeting reversible post-translational modifications with PROTACs: a focus on enzymes modifying protein lysine and arginine residues.
机构信息
Institute of Molecular and Industrial Biotechnology, Lodz University of Technology, Łódź, Poland.
Institute of Organic Chemistry, Lodz University of Technology, Łódź, Poland.
出版信息
J Enzyme Inhib Med Chem. 2023 Dec;38(1):2254012. doi: 10.1080/14756366.2023.2254012.
PROTACs represent an emerging field in medicinal chemistry, which has already led to the development of compounds that reached clinical studies. Posttranslational modifications contribute to the complexity of proteomes, with 2846 disease-associated sites. PROTAC field is very advanced in targeting kinases, while its use for enzymes mediating posttranslational modifications of the basic amino acid residues, started to be developed recently. Therefore, we bring together this less popular class of PROTACs, targeting lysine acetyltransferases/deacetylases, lysine and arginine methyltransferases, ADP-ribosyltransferases, E3 ligases, and ubiquitin-specific proteases. We put special emphasis on structural aspects of PROTAC elements to facilitate the lengthy experimental endeavours directed towards developing PROTACs. We will cover the period from the inception of the field, 2017, to April 2023.
PROTACs 代表了药物化学领域的一个新兴领域，已经有化合物进入临床研究。翻译后修饰导致蛋白质组的复杂性增加，其中有 2846 个与疾病相关的位点。PROTAC 领域在靶向激酶方面非常先进，而其用于介导碱性氨基酸残基翻译后修饰的酶的应用最近才开始发展。因此，我们将这一不太受欢迎的 PROTAC 类别聚集在一起，针对赖氨酸乙酰基转移酶/去乙酰基酶、赖氨酸和精氨酸甲基转移酶、ADP-核糖基转移酶、E3 连接酶和泛素特异性蛋白酶。我们特别强调 PROTAC 元件的结构方面，以促进针对开发 PROTAC 的漫长实验努力。我们将涵盖该领域的起始时间，即 2017 年，到 2023 年 4 月。
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