LEADER 05351nam 22006611 450 001 9910141811203321 005 20220609155255.0 010 $a3-527-65970-6 010 $a3-527-65968-4 010 $a3-527-65971-4 035 $a(CKB)2670000000414477 035 $a(EBL)1380171 035 $a(OCoLC)862821789 035 $a(SSID)ssj0001152667 035 $a(PQKBManifestationID)11682034 035 $a(PQKBTitleCode)TC0001152667 035 $a(PQKBWorkID)11148963 035 $a(PQKB)10165034 035 $a(OCoLC)858657953 035 $a(MiAaPQ)EBC1380171 035 $a(Au-PeEL)EBL1380171 035 $a(CaPaEBR)ebr10763015 035 $a(CaONFJC)MIL516716 035 $a(PPN)175440433 035 $a(EXLCZ)992670000000414477 100 $a20130704d2013 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aAntibiotics $etargets, mechanisms and resistance /$fedited by Claudio O. Gualerzi [and three others] 210 1$aWeinheim :$cWiley-VCH,$d2013. 215 $a1 online resource (575 p.) 300 $aDescription based upon print version of record. 311 $a3-527-33305-3 311 $a1-299-85465-6 320 $aIncludes bibliographical references and index. 327 $aTitle 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 ?-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 327 $a2.2 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 327 $a3.2 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 327 $a4.1.1 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 I?2-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 327 $a4.3.1 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 327 $a4.3.4 Chromosomal Mutations in Genes Required for Membrane Phospholipid Metabolism: Lipopeptide Resistance 330 $aMost 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 606 $aAntibiotics 606 $aAnti-infective agents 615 0$aAntibiotics. 615 0$aAnti-infective agents. 676 $a615.329 701 $aGualerzi$b Claudio O.$f1942-$0905181 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910141811203321 996 $aAntibiotics$92024467 997 $aUNINA