Sclerotiorin inhibits protein kinase G from Mycobacterium tuberculosis and impairs mycobacterial growth in macrophages

As a eukaryotic-like Ser/Thr protein kinase, Mycobacterium tuberculosis virulent effector protein kinase G (PknG) mediates mycobacterial survival by regulating bacterial cell metabolic processes and preventing phagosome-lysosome fusion in host macrophages. Targeting PknG is an effective strategy for development of anti-tuberculosis (TB) drugs. In the study, we found that sclerotiorin, derived from marine fungi from the South China Sea, exhibited moderately strong inhibitory effects on recombinant PknG, with an IC50 value of 76.5  μM, and acted as a non-competitive inhibitor.

Source: Tuberculosis - January 13, 2017 Category: Respiratory Medicine Authors: Dongni Chen, Shuangshuang Ma, Lei He, Peibo Yuan, Zhigang She, Yongjun Lu Source Type: research