A5061863935- HIV/AIDS drug development and treatment
- Chemical and Physical Properties in Aqueous Solutions
- Computational Drug Discovery Methods
- Ubiquitin and proteasome pathways
- Phenothiazines and Benzothiazines Synthesis and Activities
- Ionic liquids properties and applications
- Peptidase Inhibition and Analysis
- Thermodynamic properties of mixtures
- Various Chemistry Research Topics
- Bacteriophages and microbial interactions
- Polyamine Metabolism and Applications
- Microbial Natural Products and Biosynthesis
- Cancer therapeutics and mechanisms
- Tuberculosis Research and Epidemiology
- Metabolomics and Mass Spectrometry Studies
- Cancer-related gene regulation
University of Cape Town
2024
North-West University
2023
Rhodes University
2017-2021
Mycobacterium tuberculosis (Mtb) has an impermeable cell wall which gives it inherent ability to resist many antibiotics. DprE1, essential enzyme in Mtb synthesis, been validated as a target for several TB drug candidates. The most potent and developmentally advanced DprE1 inhibitor, PBTZ169, is still undergoing clinical development. With high attrition rate, there need populate the development pipeline. Using scaffold hopping strategy, we imprinted benzenoid ring of PBTZ169 onto quinolone...
The feasibility of achieving anti-HIV activity from the attenuation USP18 was explored for first time. A cheminformatic survey demonstrated that current known isopeptidase inhibitors are derivatives a bis-aryl pyranone scaffold possesses undesirable toxicity profiles. Molecular modelling approaches applied to these active pyranones isolated likely mechanism perturbs USP18. dynamic simulations and free-energy profiling showed induced-fit effects on catalytic triad IBB-1 domain residues drive...
The large chemical space universe can be traversed by screening libraries of compounds that possess novel medicinally relevant chemistries, properties and complexity criteria. These populated with the use exhaustive, de novo approaches or inspired, combinatorial approaches. By assuming natural products within may classified as a source feedstock for populating virtual libraries, they act scaffolds upon which exhaustive used in exploring space. In order to achieve this, we have built...
Eukaryotic initiation factor 5A, eIF5A, isa ubiquitous eukaryotic protein that has been shown to influence the translation of a specific subset mRNAs. It is only known undergo hypusinylation in two-step post translational modification process involving deoxyhypusine synthase (DHS) and deoxyhypusin hydroxylase (DOHH) enzymes. Hypusinylation HIV-1 HTLV-1 nuclear export signals, while involvement active hypusinylated eIF5A induction IRES mediated processes initiate pro-apoptotic have inspired...