GKL003 is a bacterial transcription inhibitor that targets the RNAP-σ interaction interface, with a K i of 5.79 nM. GKL003 specifically binds to the RNAP β' clamp helix region at the σ A factor binding site, blocks the formation of RNAP holoenzyme, and inhibits the formation of bacterial transcription initiation complexes. GKL003 inhibits the growth of both Gram-positive and Gram-negative bacterial cells, and also exhibits activity against drug-resistant strains.
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