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The anti-tuberculosis (TB) agent IMB-T130 was speculated to be a multi-target compound. In this research, we found that IMB-T130 inhibits the catalytic activity of  Mycobacterium tuberculosis  3-dehydroquinate synthase ( Mt DHQS), the enzyme in the second step of the shikimate pathway. IMB-T130 was identified as a selective inhibitor of  Mt DHQS with an IC 50  value of 0.87 μg/mL. The interaction between the compound and protein was analysed by surface plasmon resonance and circular dichroism. Based on the  in silico  molecular docking results, the essential amino acids in the binding pocket were then confirmed by site-directed mutagenesis. Overexpression of DHQS reduced the antibacterial activity of IMB-T130 in cells, verifying that DHQS is the target of IMB-T130. IMB-T130 inhibited standard and drug-resistant  M. tuberculosis  strains by targeting DHQS. Our findings improve our understanding of  Mt DHQS and make it to be a potential target for new anti-TB drug discovery.

IMB-T130 targets 3-dehydroquinate synthase and inhibits Mycobacterium tuberculosis