ML267: Inhibitor of Sfp-PPTase that Attenuates Secondary Metabolism and Thwarts Bacterial Growth

National Center For Advancing Translational Sciences

Investigators

Linked publications & trials

Abstract

Project highlights: a first-in-class sfp-PPTase inhibiting probe with good physiochemical properties ML267 has been developed. The inhibitors modulate the activity of bacterial PPTase enzymes without affecting the human ortholog. Coculture of B. subtilis with sublethal doses of ML267 decreased the capacity of the organism to produce surfactin, demonstrating the feasibility of disrupting bacterial PTM pathways to develop new antibacterials. During this period, the NCGC has fostered and maintained over 180 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to over 100 high-throughput screens and nearly 60 medicinal chemistry campaigns, providing our collaborators and the general research community a wealth of publications and promising small molecule leads. In addition, the NCGC has undertaken a number of informatic challenges to make better use of existing drug and disease target information and provide the general public with easily accessible resources, further catalyzing the development of new therapies for human disease.