PDF(Pubmed)
Abstract：
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.
摘要：
PROTACs代表了药物化学的一个新兴领域，这已经导致了达到临床研究的化合物的发展。翻译后修饰有助于蛋白质组的复杂性，与2846个疾病相关的地点。PROTAC领域在靶向激酶方面非常先进，虽然它用于介导碱性氨基酸残基翻译后修饰的酶，最近开始开发。因此,我们汇集了这类不那么受欢迎的蛋白质，靶向赖氨酸乙酰转移酶/脱乙酰酶，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要素的结构方面，以促进针对开发PROTAC的冗长实验努力。我们将涵盖从该领域开始的时期，2017年，至2023年4月。
