Structure-Based Optimization of Pyridoxal 5′-Phosphate-Dependent Transaminase Enzyme (BioA) Inhibitors that Target Biotin Biosynthesis in Mycobacterium tuberculosis

Keyphrases

• Mycobacterium Tuberculosis (M. tb) 100%
• Structure Optimization 100%
• Pyridoxal 5′-phosphate 100%
• Biotin Biosynthesis 100%
• Transaminase Enzyme 100%
• Biotin 75%
• Overexpressing 25%
• Biological Evaluation 25%
• Synthetic Evaluation 25%
• Minimum Inhibitory Concentration 25%
• Bacterial Persistence 25%
• Design Evaluation 25%
• Bacterial Survival 25%
• Structure-based Drug Design 25%
• Structure-activity Relationship 25%
• Free Media 25%
• Transaminases 25%
• Conformationally Constrained 25%
• Drug Design Strategies 25%
• Mycobacterium Tuberculosis Strains 25%
• Essential Enzymes 25%
• Systematic Series 25%
• Off-target Effects 25%
• Teraryl 25%
• Target Engagement 25%
• Constrained Derivatives 25%
• Whole-cell Screening 25%
• Co-crystallization 25%

Biochemistry, Genetics and Molecular Biology

• Anabolism 100%
• Biotin 100%
• Pyridoxal 100%
• Enzyme 100%
• Transaminase 100%
• Mycobacterium Tuberculosis 100%
• Wild Type 20%
• Structure Activity Relation 20%
• Bacterial Survival 20%
• Cell Screening 20%
• Minimum Inhibitory Concentration 20%
• Whole Cell 20%

Pharmacology, Toxicology and Pharmaceutical Science

• Aminotransferase 100%
• Pyridoxal 5 Phosphate 100%
• Biotin 100%
• Mycobacterium Tuberculosis 100%
• Drug Development 20%
• Minimum Inhibitory Concentration 20%
• Structure Activity Relationship 20%
• Target Activity 20%