NiKem Research, via Zambeletti 25, 20021 Baranzate, Milan, Italy.
ChemMedChem. 2010 Apr 6;5(4):552-8. doi: 10.1002/cmdc.200900409.
High-throughput screening highlighted 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile (1) as an active inhibitor of ubiquitin-specific proteases (USPs), a family of hydrolytic enzymes involved in the removal of ubiquitin from protein substrates. The chemical behavior of compound 1 was examined. Moreover, the synthesis and in vitro evaluation of new compounds, analogues of 1, led to the identification of potent and selective inhibitors of the deubiquitinating enzyme USP8.
高通量筛选突出显示 9-氧代-9H-茚并[1,2-b]吡嗪-2,3-二腈（1）是泛素特异性蛋白酶（USPs）的有效抑制剂，USP 是一组参与从蛋白质底物上去除泛素的水解酶。研究了化合物 1 的化学行为。此外，新化合物的合成和体外评估，1 的类似物，导致鉴定出去泛素化酶 USP8 的有效和选择性抑制剂。
