New insight into enzyme for HIV/Aids drug development
Without the help of a particular enzyme, HIV/Aids cannot replicate itself and take over the body’s cells. Dr Andrew Motsilanyane, a recent PhD graduate from the North-West University (NWU), has been targeting this enzyme, HIV-1 protease, in research that could open up new possibilities for drug development.
His work focuses on the critical role of HIV-1 protease in the virus's life cycle and emphasises the importance of targeting this enzyme in the development of integrase inhibitors. Integrase inhibitors are one of several classes of antiretroviral drugs used to treat HIV as part of antiretroviral therapy.
HIV needs integrase to replicate, but for this to happen, it needs the help of the HIV-1 protease enzyme. Without this enzyme, HIV cannot make integrase and take over CD4 cells to copy itself, which means the virus’s cycle is interrupted.
Dr Motsilanyane’s study provides a comprehensive view of HIV drug targets and recent advancements in antiviral therapeutics. Specifically, it highlights the significance of integrase inhibitors and developments in HIV-1 protease inhibitors. Through meticulous analysis of computer-aided drug design studies, the research offers insights into the molecular mechanisms of HIV-1 protease inhibition.
The study employed various methodologies of computer aided drug design. It also used molecular dynamics simulations to explore potential inhibitors of HIV-1 protease, contributing to the drug discovery process.
A significant finding is the identification of one of the compounds as a promising candidate for further research.
“When applying these computer-aided drug design tools, we were able to analyse them further and some of them passed toxicity tests, indicating its suitability for oral administration,” says Dr Motsilanyane.
Additionally, their molecular weight and other characteristics align with Lipinski's rule of five (which sets out the rules for oral drugs), suggesting its potential for therapeutic development.
This research offers valuable insights and has implications for developing innovative HIV inhibitors. It also lays a solid foundation for future research in this critical area.
More about Dr Andrew Motsilanyane
Dr Motsilanyane enrolled for a BSc degree at the NWU in 2001. He pursued a postgraduate degree in education in 2007, followed by studies in psychology in 2008 and 2009. He obtained an honour's degree in chemistry in 2011 and an MSc degree in chemistry in 2018, also at the NWU.
Dr Motsilanyane worked as a teacher from 2006 to 2019 and was temporarily employed as a junior lecturer at the NWU's Faculty of Education in 2019 and 2020. Thereafter, he started working on his PhD.
