Novel Small Molecules, Targets, and Strategies in Anti-Infective Development

Dove e quando

2017-07-03 | Aula magna DCCI

Il Prof. Jason K. Sello, della Brown University, Providence, RI (USA), il 3 luglio 2017, alle 15.00, terrà, presso il Dipartimento di Chimica e Chimica Industriale, in aula magna, un seminario dal titolo "Novel Small Molecules, Targets, and Strategies in Anti-Infective Development" Abstract: The increasing number of infections caused by multi-drug resistant bacteria portends a public health crisis. Unfortunately, therapeutic options are limited because of a long innovation gap in the last half-century of antibacterial drug development. The gap is reflected in marketed drugs that have closely related structures and act on a few essential phenomena like DNA replication, transcription, translation, and cell envelope homeostasis. This situation is problematic because genetic mutations or genes that confer resistance to one antibacterial drug often compromise the efficacies of others with the same target or mechanism of action. To circumvent this “cross-resistance”, we must identify and validate new antibacterial drug targets. Among the most compelling of today’s antibacterial drug targets are the chaperone-dependent proteases that are known to play critical roles in bacterial physiology and pathogenicity. Interestingly, the accumulation of data that have validated these enzymes as drug targets has been coincident with discoveries of novel small molecules that critically perturb them. This seminar will describe efforts in the Sello group to discover, design, and synthesize small molecules that lethally perturb the structures and functions of enzymes that mediate protein homeostasis in a variety of pathogenic bacteria. Additionally, efforts to develop inhibitors of chaperone-dependent proteases for applications in cancer therapy will be discussed.
Ultimo aggiornamento 29 Giugno 2017