In small molecule drug discovery and development, drugs are normally optimized for hepatic metabolism. However, in tuberculosis (TB) drug discovery, drug metabolism mediated by the causative agent, Mycobacterium tuberculosis (Mtb), needs to be factored in. Mtb-mediated drug metabolism has potential implications both on the efficacy of TB drugs but also on the efficacy of co-administered drugs in patients with co-morbidities. To ensure optimal drug dosages, this warrants the consideration of both hepatic and Mtb-mediated drug metabolism when optimizing small molecule drug candidates as well as in treating patients with co-morbidities.
Plasmodium kinases essential for parasite survival and expressed at multiple stages of the malaria parasite lifecycle have been identified. With knowledge of protein structures/binding site for human kinase inhibitors, human kinase focused libraries being available for screening, and evidence of clinical validation of Plasmodium phosphatidylinositol 4-kinase type III beta – PfPI4KIIIβ, the kinase gene family presents an attractive opportunity for malaria drug discovery through target repurposing.
Kelly Chibale is a Professor of Organic Chemistry at the University of Cape Town (UCT) where he holds the Neville Isdell Chair in African-centric Drug Discovery & Development. He is also a Schmidt Sciences AI2050 Senior Fellow, Full Member of the UCT Institute of Infectious Disease & Molecular Medicine, founding Director of the South African Medical Research Council Drug Discovery & Development Research unit at UCT, Founder & Director of the UCT Holistic Drug Discovery and Development (H3D) Centre and Founder and CEO of the H3D Foundation. Kelly obtained his PhD in Synthetic Organic Chemistry from the University of Cambridge.
This was followed by postdoctoral stints at the University of Liverpool and Scripps Research Institute. Kelly’s research interests are in drug discovery and the development of tools and models to contribute to improving treatment outcomes in people of African descent. He serves as Editor-In-Chief of the American Chemical Society (ACS)’s ACS Medicinal Chemistry Letters.
Kelly Chibale is a Professor of Organic Chemistry at the University of Cape Town (UCT) where he holds the Neville Isdell Chair in African-centric Drug Discovery & Development. He is also a Schmidt Sciences AI2050 Senior Fellow, Full Member of the UCT Institute of Infectious Disease & Molecular Medicine, founding Director of the South African Medical Research Council Drug Discovery & Development Research unit at UCT, Founder & Director of the UCT Holistic Drug Discovery and Development (H3D) Centre and Founder and CEO of the H3D Foundation. Kelly obtained his PhD in Synthetic Organic Chemistry from the University of Cambridge. This was followed by postdoctoral stints at the University of Liverpool and Scripps Research Institute. Kelly’s research interests are in drug discovery and the development of tools and models to contribute to improving treatment outcomes in people of African descent. He serves as Editor-In-Chief of the American Chemical Society (ACS)’s ACS Medicinal Chemistry Letters.