1.

Record Nr.

UNINA9910141811203321

Titolo

Antibiotics : targets, mechanisms and resistance / / edited by Claudio O. Gualerzi [and three others]

Pubbl/distr/stampa

Weinheim : , : Wiley-VCH, , 2013

ISBN

3-527-65970-6

3-527-65968-4

3-527-65971-4

Descrizione fisica

1 online resource (575 p.)

Altri autori (Persone)

GualerziClaudio O. <1942->

Disciplina

615.329

Soggetti

Antibiotics

Anti-infective agents

Lingua di pubblicazione

Inglese

Formato

Materiale a stampa

Livello bibliografico

Monografia

Note generali

Description based upon print version of record.

Nota di bibliografia

Includes bibliographical references and index.

Nota di contenuto

Title Page; Copyright; Contents; Preface; List of Contributors; Chapter 1 A Chemist's Survey of Different Antibiotic Classes; 1.1 Introduction; 1.2 Aminoglycosides; 1.3 β-Lactams; 1.4 Linear Peptides; 1.4.1 Glycopeptides-Dalbaheptides; 1.4.2 Lantibiotics; 1.5 Cyclic Peptides; 1.6 Thiazolylpeptides; 1.7 Macrolactones; 1.7.1 Macrolides; 1.7.2 Difimicin; 1.8 Ansamycins-Rifamycins; 1.9 Tetracyclines; 1.10 Oxazolidinones; 1.11 Lincosamides; 1.12 Pleuromutilins; 1.13 Quinolones; 1.14 Aminocoumarins; References; Chapter 2 Antibacterial Discovery: Problems and Possibilities; 2.1 Introduction

2.2 Why Is Antibacterial Discovery Difficult? The Problems2.3 Target Choice: Essentiality; 2.4 Target Choice: Resistance; 2.5 Cell Entry; 2.6 Screening Strategies; 2.6.1 Empirical Screens; 2.6.2 Phenotypic Whole-Cell Screens; 2.6.3 In Vitro Screens for Single-Target Inhibitors; 2.6.4 Chemicals to Screen; 2.6.4.1 Chemical Collections; 2.7 Natural Products; 2.8 Computational Chemistry, Virtual Screening, Structure- and Fragment-Based Drug Design (SBDD and FBDD); 2.9 Conclusions; References; Chapter 3 Impact of Microbial Natural Products on Antibacterial Drug Discovery; 3.1 Introduction

3.2 Natural Products for Drug Discovery3.3 Microbial Natural Products; 3.4 The Challenge of Finding Novel Antibiotics from New Natural Sources; 3.5 Workflow for Drug Discovery from Microbial Natural



Products; 3.6 Antimicrobial Activities: Targets for Screens; 3.7 Natural Products: A Continuing Source for Inspiration; 3.8 Genome Mining in Natural Product Discovery; 3.9 Conclusions; References; Chapter 4 Antibiotics and Resistance: A Fatal Attraction; 4.1 To Be or Not to Be Resistant: Why and How Antibiotic Resistance Mechanisms Develop and Spread among Bacteria

4.1.1 Horizontal and Vertical Transmission of Resistance Genes4.2 Bacterial Resistance to Antibiotics by Enzymatic Degradation or Modification; 4.2.1 Antibiotic Resistance by Hydrolytic Enzymes; 4.2.1.1 Î2-Lactamases; 4.2.1.2 Macrolide Esterases; 4.2.1.3 Epoxidases; 4.2.1.4 Proteases; 4.2.2 Antibiotic Transferases Prevent Target Recognition; 4.2.2.1 Acyltransfer; 4.2.2.2 Phosphotransferases; 4.2.2.3 Nucleotidyltransferases; 4.2.2.4 ADP-Ribosyltransferases; 4.2.2.5 Glycosyltransferases; 4.2.3 Redox Enzymes; 4.3 Antibiotic Target Alteration: The Trick Exists and It Is in the Genetics

4.3.1 Low-Affinity Homologous Genes4.3.1.1 Rifamycin Low-Affinity RpoB; 4.3.1.2 Mutated Genes Conferring Resistance to Quinolone, Fluoroquinolone and Aminocoumarins; 4.3.1.3 PBP2a: A Low-Affinity Penicillin-Binding Protein; 4.3.1.4 Dihydropteroate Synthases Not Inhibited by Sulfonamide; 4.3.2 Chemical Modification of Antibiotic Target; 4.3.2.1 23S rRNA Modification; 4.3.2.2 16S rRNA Modification; 4.3.2.3 Reprogramming Chemical Composition of a Bacterial Cell-Wall Precursor; 4.3.3 Ribosomal Protection and Tetracycline Resistance

4.3.4 Chromosomal Mutations in Genes Required for Membrane Phospholipid Metabolism: Lipopeptide Resistance

Sommario/riassunto

Most of the antibiotics now in use have been discovered more or less by chance, and their mechanisms of action have only been elucidated after their discovery. To meet the medical need for next-generation antibiotics, a more rational approach to antibiotic development is clearly needed.Opening with a general introduction about antimicrobial drugs, their targets and the problem of antibiotic resistance, this reference systematically covers currently known antibiotic classes, their molecular mechanisms and the targets on which they act. Novel targets such as cell signaling networks, ribo