A5074735686- Biochemical and Molecular Research
- Antifungal resistance and susceptibility
- Cancer therapeutics and mechanisms
- Tuberculosis Research and Epidemiology
- Fungal Plant Pathogen Control
- Synthesis and biological activity
- Enzyme Catalysis and Immobilization
- Antibiotic Resistance in Bacteria
- Mycobacterium research and diagnosis
- Microbial Metabolic Engineering and Bioproduction
- Protein Structure and Dynamics
- Microbial Natural Products and Biosynthesis
- Salmonella and Campylobacter epidemiology
- Enzyme Structure and Function
- Helicobacter pylori-related gastroenterology studies
- Synthesis and Biological Evaluation
- Antimicrobial Resistance in Staphylococcus
The University of Queensland
2016-2021
Acetohydroxyacid synthase (AHAS, EC 2.2.1.6), the first enzyme in branched chain amino acid biosynthesis pathway, is target for more than 50 commercially available herbicides, and a promising antimicrobial drug discovery. Herein, we have expressed purified AHAS from Candida auris, newly identified human invasive fungal pathogen. Thirteen inhibiting herbicides Ki values of <2 μM this enzyme, with most potent having <32 nM. Six these compounds exhibited MIC50 <1 against C. auris (CBS10913...
New drugs to treat tuberculosis (TB) are urgently needed combat the increase in resistance observed among current first-line and second-line treatments. Here, we propose ketol-acid reductoisomerase (KARI) as a target for anti-TB drug discovery. Twenty-two analogues of IpOHA, an inhibitor plant KARI, were evaluated antimycobacterial agents. The strongest Mycobacterium (Mt) KARI has Ki value 19.7 nM, fivefold more potent than IpOHA (Ki = 97.7 nM). This four other slow- tight-binding inhibitors...
Abstract New drugs aimed at novel targets are urgently needed to combat the increasing rate of drug‐resistant tuberculosis (TB). Herein, National Cancer Institute Developmental Therapeutic Program (NCI‐DTP) chemical library was screened against a promising new target, ketol–acid reductoisomerase (KARI), second enzyme in branched‐chain amino acid (BCAA) biosynthesis pathway. From this library, 6‐hydroxy‐2‐methylthiazolo[4,5‐ d ]pyrimidine‐5,7(4 H ,6 )‐dione (NSC116565) identified as potent...
Helicobacter pylori (Hp) is a human pathogen that lives in the gastric mucosa of approximately 50% world's population causing gastritis, peptic ulcers, and cancer. An increase resistance to current drugs has sparked search for new Hp drug targets therapeutics. One target disruption nucleic acid production, which can be achieved by impeding synthesis 6-oxopurine nucleoside monophosphates, precursors DNA RNA. These metabolites are synthesized xanthine–guanine–hypoxanthine...