–
November 15, 2024
2024 WARF Therapeutics Distinguished Lecture in Drug Discovery
- Jeffrey Aubé, PhD
- University of North Carolina
New Approaches to Tuberculosis Therapeutics
Tuberculosis (TB) continues to be a major worldwide health problem, despite the existence of numerous drugs for its treatment. This is in part due to the long therapeutics times required to administer cocktails of front-line therapeutics and in part due to the emergence of even more challenging long-term strains. For these reasons, new therapeutic agents for the treatment of TB continue to be sought. In collaborative work with the laboratory of Carl Nathan (Weill–Cornell Medicine) and others, we have sought to find new chemotypes as potential anti-TB agents and to identify new biochemical targets for drug treatment. In this talk, I will describe our efforts in this area, beginning with early approaches to explore beta-lactam antibiotics as possible TB agents. More recent efforts have been focused on finding inhibitors of phosphopantetheinyl transferase (PptT). PptT carries out central biochemistry that is essential for mycobacterial survival; for this reason, it has been a long sought-target for antibacterial agent development. This story begins with our team's discovery of the first effective small-molecule inhibitors of PptT, efforts to use bioisostere design to create a new series, and more recent chemotypes of PptT.
Hosted by Jennifer Golden
Jeffrey Aubé, PhD
Esehlman Distinguished Professor
Division of Chemical Biology & Medicinal Chemistry
Eshelman School of Pharmacy, University of North Carolina at Chapel Hill
Jeffrey Aubé attended the University of Miami, where he did undergraduate research with Professor Robert Gawley. He received his Ph.D. in chemistry in 1984 from Duke University, working with Professor Steven Baldwin, and was an NIH postdoctoral fellow at Yale University with Professor Samuel Danishefsky. From 1986 until 2015,he held a faculty position in the Department of Medicinal Chemistry at the University of Kansas. In 2015, he moved to the University of North Carolina, where he is an Eshelman Distinguished Professor in the Division of Chemical Biology and Medicinal Chemistry and holds a joint appointment in the Department of Chemistry.