Thiazolyl peptides are natural products with a wide range of biological activities, including anticancer, antiplasmodial, and antibacterial. Although the natural compounds are not suitable drug because of poor solubility, many synthetic derivatives are currently in clinical trials. An understanding of the enzymes that convert peptide substrates into thiazolyl peptides will significantly aid in producing molecules with better drug-like properties. We seek to carry out biochemical, and structural biological studies on several of these enzymes to help guide the production of improved versions of these bioactive compounds.