Bacterial Enzymes as Targets for Drug Discovery: Meeting the Challenges of Antibiotic Resistance addresses the gap between medical microbiology, structural biology, and genomic science in the development of new antibacterial drug development. This book consolidates detailed profiling of bacterial target enzyme families for the drug discovery process and methodologies for use and validation of the potential drug targets. The content covers the foundations of antibiotic drug discovery process and focuses on bacterial enzymes as drug targets, building a bridge between microbiology, structural biology, and genomic science. This is the ideal reference for antibiotic drug discovery researchers in the pharma industry and academia. Biochemists, microbiologists, and medicinal chemists will also benefit from this books’ content.
Table of Contents
Part I Primer of antibiotic discovery process1. Antibacterial drug discovery: An introduction
2. Druggability of a target site
3. Dual inhibition as a novel strategy for antibiotic discovery
4. Conserved enzymes across the bacterial pathogens serves as great drug targets
5. Validation of drug targets using molecular methodologies
6. Selection of Enzymatic activity assays for validation of inhibitory potential
7. Computational tools to identify potential drug targets in bacteria
8. Antimicrobial drug resistance and bypassing strategies
Part II Bacterial enzyme as drug targets
9. Strategic identification of novel enzymes as antibacterial drug targets
10. Inhibiting the replication by targeting topoisomerases
11. Aminoglycoside modifying Enzymes (AMEs)
12. Role of beta lactamases in antibiotic drug discovery
13. Combining efflux pump inhibitory agents for broad spectrum antibacterial activity
14. Ribosomal binding antibacterial agents
15. DNA dependent RNA polymerase as an attractive drug target
16. Polymyxins and their role as next generation inhibitory compounds
17. Arresting the peptidoglycan synthesis to kill the bacteria
18. Bacterial Proteases
19. Targeting lipase enzyme for drug discovery
20. Bacteriophage mechanisms for identification of target enzymes
21. Role of regulatory RNAs as antibacterial drug targets
22. Pathogen specific antibiotic discovery
23. Drug Repurposing: Tackling the antibiotic resistance with existing therapeutics