Development of Tyrphostin Analogues to Study Inhibition of the Mycobacterium tuberculosis Pup Proteasome System**,ChemBioChem

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Development of Tyrphostin Analogues to Study Inhibition of the Mycobacterium tuberculosis Pup Proteasome System**
ChemBioChem ( IF 2.6 ) Pub Date : 2021-08-12 , DOI: 10.1002/cbic.202100333
Guido V Janssen _{1,

2} , Susan Zhang ₃ , Remco Merkx ₂ , Christa Schiesswohl ₄ , Champak Chatterjee ₄ , K Heran Darwin ₃ , Paul P Geurink _{1,

2} , Gerbrand J van der Heden van Noort _{1,

2} , Huib Ovaa _{1,

2}

Affiliation

The Mycobacterium tuberculosis (Mtb) prokaryotic ubiquitin-like (pup) proteasome system is an attractive target for new drug development. In this study a screen was performed identifying Tyrphostins as low micromolar inhibitors of the Mtb protease Dop. To gain insight in the important functional aspects of these inhibitors, 25 new analogues were prepared and validated, in vitro. Several new compounds were able to inhibit both the depupylating activity of Dop as well as the pupylating activity of de pup ligase PafA.

中文翻译：

开发酪氨酸磷酸化抑制剂类似物来研究结核分枝杆菌幼崽蛋白酶体系统的抑制**

结核 分枝杆菌 (Mtb)原核泛素样 (pup) 蛋白酶体系统是新药开发的一个有吸引力的目标。在这项研究中，进行了筛选，将酪氨酸磷酸酶鉴定为 Mtb 蛋白酶 Dop 的低微摩尔抑制剂。为了深入了解这些抑制剂的重要功能，我们在体外制备并验证了 25 种新的类似物。几种新化合物能够抑制 Dop 的去幼虫化活性以及去幼虫连接酶 PafA 的去幼虫化活性。

更新日期：2021-08-12

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