Linked e-resources
Details
Table of Contents
Intro; Preface; References; Contents; Antibacterial New Target Discovery: Sentinel Examples, Strategies, and Surveying Success; 1 Introduction: An Evolving View of New and Legitimate Antibacterial Targets; 2 Conditional Essentiality: Providing Novel Screens and Cognate Inhibitors to Validate New Druggable Targets; 3 Alternative Approaches to New Target Discovery; 4 Structural Biology Advances Driving Target Discovery; 5 Considering Antibacterial Drug Resistance as Contextual; 6 Target Discovery Parallels Between Gram-positive WTA and Gram-negative OM Biogenesis; 7 Conclusions; References
The Antibiotic Future1 Introduction; 2 Excursion: Alternatives to Antibiotics; 3 The Resistance Problem with Single Targets; 3.1 Measurement of Resistance; 3.2 Overcoming Single-Target Resistance; 3.2.1 Low Fitness; 3.2.2 Dosing above the Mutant Prevention Concentration (MPC); 3.2.3 Avoiding Resistance by Multiple Target-Ligand Interactions; 3.2.4 Narrow Spectrum Agents; 3.3 Leveraging Single Targets by Truly Assessing Combinations; 3.3.1 Problems that could Compromise Combinations; 4 Old Targets new Chemical Matter; 5 The Entry Problem; 5.1 Gram Positives: Cytoplasmic Membrane Transit
3 Inhibition of Target Alteration4 Inhibition of Efflux; 5 Enhancement of Antibiotic Uptake; 6 Interfering with Signaling Systems; 7 Targeting Nonessential Steps in Cell Wall Synthesis; 8 Conclusions; References; Allosteric Inhibition of Bacterial Targets: An Opportunity for Discovery of Novel Antibacterial Classes; 1 Introduction; 2 Allostery: Modern Interpretation and Examples in Therapeutic Discovery; 3 Examples of Allosteric Targeting in Antimicrobial Discovery; 3.1 Aminoglycoside-Modifying Enzymes; 3.2 The PBP2a Enzyme of Methicillin-Resistant Staphylococcus aureus
3.2.1 Antibacterial Quinazolinones Act as Allosteric Modulators of S. aureus PBP2a3.2.2 Other Structures as Possible PBP2a Allosteric Modulators; 4 Allosteric Discovery Opportunities; 5 Allosteric Discovery Methods; 5.1 Virtual Screening; 5.2 Assay Implementation; 6 Conclusion; References; The Clinical Development of Antibacterial Drugs: A Guide for the Discovery Scientist; 1 Introduction; 2 Novel Targets?; 3 Not ``Novel ́́Targets; 4 Nonclinical Development; 5 Clinical Development Considerations; 5.1 Non-inferiority Trials; 5.2 Fixed-Dose Combination Antibacterials
The Antibiotic Future1 Introduction; 2 Excursion: Alternatives to Antibiotics; 3 The Resistance Problem with Single Targets; 3.1 Measurement of Resistance; 3.2 Overcoming Single-Target Resistance; 3.2.1 Low Fitness; 3.2.2 Dosing above the Mutant Prevention Concentration (MPC); 3.2.3 Avoiding Resistance by Multiple Target-Ligand Interactions; 3.2.4 Narrow Spectrum Agents; 3.3 Leveraging Single Targets by Truly Assessing Combinations; 3.3.1 Problems that could Compromise Combinations; 4 Old Targets new Chemical Matter; 5 The Entry Problem; 5.1 Gram Positives: Cytoplasmic Membrane Transit
3 Inhibition of Target Alteration4 Inhibition of Efflux; 5 Enhancement of Antibiotic Uptake; 6 Interfering with Signaling Systems; 7 Targeting Nonessential Steps in Cell Wall Synthesis; 8 Conclusions; References; Allosteric Inhibition of Bacterial Targets: An Opportunity for Discovery of Novel Antibacterial Classes; 1 Introduction; 2 Allostery: Modern Interpretation and Examples in Therapeutic Discovery; 3 Examples of Allosteric Targeting in Antimicrobial Discovery; 3.1 Aminoglycoside-Modifying Enzymes; 3.2 The PBP2a Enzyme of Methicillin-Resistant Staphylococcus aureus
3.2.1 Antibacterial Quinazolinones Act as Allosteric Modulators of S. aureus PBP2a3.2.2 Other Structures as Possible PBP2a Allosteric Modulators; 4 Allosteric Discovery Opportunities; 5 Allosteric Discovery Methods; 5.1 Virtual Screening; 5.2 Assay Implementation; 6 Conclusion; References; The Clinical Development of Antibacterial Drugs: A Guide for the Discovery Scientist; 1 Introduction; 2 Novel Targets?; 3 Not ``Novel ́́Targets; 4 Nonclinical Development; 5 Clinical Development Considerations; 5.1 Non-inferiority Trials; 5.2 Fixed-Dose Combination Antibacterials