GTPase inhibition

FtsZ-targeting Cell Division Inhibitors

FtsZ, a GTPase that regulates bacterial cell division has been a recognised target for novel antibacterial drug discovery for some time. Under Lloyd Czaplewski's direction, Prolysis discovered the first effective inhibitors of bacterial cell division & partnered the project with the Wellcome Trust's Seeding Drug Discovery initiative. An efficient Lead optimisation project delivered best-in-class novel antibacterials that are effective in gold-standard models of infection


Crystal structure of Bacillus FtsZ from Haydon et al. Image prepared using PyMol. Compounds selected from published patents & papers. Left 3-MBA, right PC190723 - the result of a Lead Optimisation programme.


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