Transition state analysis as a smart approach to the development of novel tailored therapeutics
Maurice Wilkins Centre scientists are using an approach called transition state analysis to generate potent and selective enzyme inhibitors, several of which have already been tested in preclinical and human trials for their potential as treatments for a variety of infectious diseases, haematological disorders and gout.
Transition state analysis is a rational approach to drug discovery spanning biology, physical chemistry, quantum mechanics and computational modelling, as well as inhibitor design and synthesis.
We will now focus on targeting enzymes that lack effective inhibitors, by applying the experience we have gained over the past two decades through our long-standing collaboration with the Albert Einstein College of Medicine. Our targets will include specific metabolic enzymes involved in cancer, enzymes that confer bacterial resistance, and enzymes that play critical roles in microbial metabolism.
Of note, Wellington-based Maurice Wilkins Centre researchers in this programme helped discover and test novel anti-cancer agent Mundesine, only the second New Zealand-developed drug to be authorised anywhere in the world for use in patients. Mundesine was approved in Japan in 2017 for treating patients with peripheral T-cell lymphoma – a group of aggressive cancers that account for 10 to 15 percent of all cases of non-Hodgkin lymphomas.