He-Wei Jiang, Daniel M Czajkowsky, Tao Wang, Xu-De Wang, Jia-Bin Wang, Hai-Nan Zhang, Cheng-Xi Liu, Fan-Lin Wu, Xiang He, Zhao-Wei Xu, Hong Chen, Shu-Juan Guo, Yang Li, Li-Jun Bi, Jiao-Yu Deng, Jin Xie, Jian-Feng Pei, Xian-En Zhang, Sheng-Ce Tao
Owing to the spread of multidrug resistance (MDR) and extensive drug resistance (XDR), there is a pressing need to identify potential targets for the development of more-effective anti-M. tuberculosis (Mtb) drugs. PafA, as the sole Prokaryotic Ubiquitin-like Protein ligase in the Pup-proteasome System (PPS) of Mtb, is an attractive drug target. Here, we show that the activity of purified Mtb PafA is significantly inhibited upon the association of AEBSF (4-(2-aminoethyl) benzenesulfonyl fluoride) to PafA residue Serine 119 (S119)...
March 27, 2018: EBioMedicine