The emergence of resistance to antibiotics in bacterial pathogens, and a lack of new antibiotics are of deep concern globally. Traditional paths to discovery have generally failed to deliver a new generation of antibacterial agents. Fragment-based screening offers a promising alternative. We will exploit a unique opportunity to combine innovative, complementary approaches to develop new lead compounds targeted against key bacterial pathogens: fragment based screening by crystallography and electrospray ionization mass spectrometry, followed by medicinal chemistry to develop these hits into leads. The target will be the beta-clamp, an essential part of the bacterial DNA replication machinery.
The emergence of resistance to antibiotics in bacterial pathogens, and a lack of new antibiotics are of deep concern globally. Traditional paths to discovery have generally failed to deliver a new generation of antibacterial agents. Fragment-based screening offers a promising alternative. We will exploit a unique opportunity to combine innovative, complementary approaches to develop new lead compounds targeted against key bacterial pathogens: fragment based screening by crystallography and electrospray ionization mass spectrometry, followed by medicinal chemistry to develop these hits into leads. The target will be the beta-clamp, an essential part of the bacterial DNA replication machinery.