Antibiotics : targets, mechanisms and resistance /

Antibiotics : targets, mechanisms and resistance /

"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. Openin...

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Bibliographic Details
Other Authors: Gualerzi, Claudio O., 1942-
Format: eBook
Language:English
Published: Weinheim, Germany : Wiley-VCH, ©2014.
Subjects:
Antibiotics.
Antibiotics > Physiological effect.
Drug Resistance, Microbial.
Anti-Bacterial Agents.
Electronic books.
Electronic book.
Online Access:Connect to the full text of this electronic book

MARC

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245 0 0 |a Antibiotics :  |b targets, mechanisms and resistance /  |c edited by Claudio O. Gualerzi [and others]. 
260 |a Weinheim, Germany :  |b Wiley-VCH,  |c ©2014. 
300 |a 1 online resource (xxiv, 549 pages) :  |b illustrations (some color) 
336 |a text  |b txt  |2 rdacontent 
337 |a computer  |b c  |2 rdamedia 
338 |a online resource  |b cr  |2 rdacarrier 
504 |a Includes bibliographical references and index. 
588 0 |a Online resource; title from PDF title page (Wiley, viewed November 4, 2013). 
505 0 |6 880-01  |a A chemist's survey of different antibiotic classes -- Antibacterial discovery: problems and possibilities -- Impact of microbial natural products on antibacterial drug discovery -- Antibiotics and resistance: a fatal attraction -- Fitness costs of antibiotic resistance -- Inhibitors of cell-wall synthesis -- Inhibitors of bacetrial cell partitioning -- The membrane as a novel target site for antibiotics to kill persisting bacterial pathogens -- Bacterial membrane, a key for controlling drug influx and efflux -- Interference with bacterial cell-to-cell chemical signaling in development of new anti-infectives -- Recent developments in inhibitors of bacterial type IIA topoisomerases -- Antibiotics targeting bacterial RNA polymerase -- Inhibitors targeting riboswitches and ribozymes -- Targeting ribonuclease P -- Involvement of ribosome biogenesis in antibiotic functions, acquired resistance, and future opportunities in drug discovery -- Aminoacyl-tRNA synthetase inhibitors -- Antibiotics targeting translation initiation in prokaryotes -- Inhibitors of bacterial elongation factor EF-Tu -- Aminoglycoside antibiotics: structural decoding of inhibitors targeting the ribosomal decoding A site -- Reptidyltransferase inhibitors of the bacterial ribosome -- Antibiotics inhibiting the translocation step of protein elongation on the ribosome -- Antibiotics at the ribosomal exit tunnel -- selected structual aspects -- Targeting HSP70 to fight cancer and bad bugs: one and the same battle? 
520 |a "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, riboswitches and bacterial chaperones are covered here, alongside the latest information on the molecular mechanisms of current blockbuster antibiotics. With its broad overview of current and future antibacterial drug development, this unique reference is essential reading for anyone involved in the development and therapeutic application of novel antibiotics"--EBL. 
650 0 |a Antibiotics. 
650 0 |a Antibiotics  |x Physiological effect. 
650 2 2 |a Drug Resistance, Microbial. 
650 1 2 |a Anti-Bacterial Agents. 
650 2 |a Anti-Bacterial Agents. 
655 4 |a Electronic books. 
655 0 |a Electronic book. 
700 1 |a Gualerzi, Claudio O.,  |d 1942- 
776 0 8 |i Print version:  |t Antibiotics.  |d Weinheim : Wiley-VCH, 2013  |z 9783527333059 
856 4 0 |u http://proxy.library.tamu.edu/login?url=https://onlinelibrary.wiley.com/book/10.1002/9783527659685  |z Connect to the full text of this electronic book  |t 0 
880 0 0 |6 505-00  |g 1.  |t A Chemist's Survey of Different Antibiotic Classes / Sonia Ilaria Maffioli --  |g 1.1.  |t Introduction --  |g 1.2.  |t Aminoglycosides --  |g 1.3.  |t β Lactams --  |g 1.4.  |t Linear Peptides --  |g 1.4.1.  |t Glycopeptides-Dalbaheptides --  |g 1.4.2.  |t Lantibiotics --  |g 1.5.  |t Cyclic Peptides --  |g 1.6.  |t Thiazolylpeptides --  |g 1.7.  |t Macrolactones --  |g 1.7.1.  |t Macrolides --  |g 1.7.2.  |t Difimicin --  |g 1.8.  |t Ansamycins --  |g 1.9.  |t Tetracyclines --  |g 1.10.  |t Oxazolidinones --  |g 1.11.  |t Lincosamides --  |g 1.12.  |t Pleuromutilins --  |g 1.13.  |t Quinolones --  |g 1.14.  |t Aminocoumarins -- --  |g 2.  |t Antibacterial Discovery: Problems and Possibilities / Lynn L. Silver --  |g 2.1.  |t Introduction --  |g 2.2.  |t Why Is Antibacterial Discovery DifficultThe Problems --  |g 2.3.  |t Target Choice: Essentiality --  |g 2.4.  |t Target Choice: Resistance --  |g 2.5.  |t Cell Entry --  |g 2.6.  |t Screening Strategies --  |g 2.6.1.  |t Empirical Screens --  |g 2.6.2.  |t Phenotypic Whole-Cell Screens --  |g 2.6.3.  |t In Vitro Screens for Single-Target Inhibitors --  |g 2.6.4.  |t Chemicals to Screen --  |g 2.6.4.1.  |t Chemical Collections --  |g 2.7.  |t Natural Products --  |g 2.8.  |t Computational Chemistry, Virtual Screening, Structure- and Fragment-Based Drug Design (SBDD and FBDD) --  |g 2.9.  |t Conclusions -- --  |g 3.  |t Impact of Microbial Natural Products on Antibacterial Drug Discovery / Gabriella Molinari --  |g 3.1.  |t Introduction --  |g 3.2.  |t Natural Products for Drug Discovery --  |g 3.3.  |t Microbial Natural Products --  |g 3.4.  |t The Challenge of Finding Novel Antibiotics from New Natural Sources --  |g 3.5.  |t Workflow for Drug Discovery from Microbial Natural Products --  |g 3.6.  |t Antimicrobial Activities: Targets for Screens --  |g 3.7.  |t Natural Products: A Continuing Source for Inspiration --  |g 3.8.  |t Genome Mining in Natural Product Discovery --  |g 3.9.  |t Conclusions -- --  |g 4.  |t Antibiotics and Resistance: A Fatal Attraction / Anna Maria Puglia --  |g 4.1.  |t To Be or Not to Be Resistant: Why and How Antibiotic Resistance Mechanisms Develop and Spread among Bacteria --  |g 4.1.1.  |t Horizontal and Vertical Transmission of Resistance Genes --  |g 4.2.  |t Bacterial Resistance to Antibiotics by Enzymatic Degradation or Modification --  |g 4.2.1.  |t Antibiotic Resistance by Hydrolytic Enzymes --  |g 4.2.1.1.  |t β-Lactamases --  |g 4.2.1.2.  |t Macrolide Esterases --  |g 4.2.1.3.  |t Epoxidases --  |g 4.2.1.4.  |t Proteases --  |g 4.2.2.  |t Antibiotic Transferases Prevent Target Recognition --  |g 4.2.2.1.  |t Acyltransfer --  |g 4.2.2.2.  |t Phosphotransferases --  |g 4.2.2.3.  |t Nucleotidyltransferases --  |g 4.2.2.4.  |t ADP-Ribosyltransferases --  |g 4.2.2.5.  |t Glycosyltransferases --  |g 4.2.3.  |t Redox Enzymes --  |g 4.3.  |t Antibiotic Target Alteration: The Trick Exists and It Is in the Genetics --  |g 4.3.1.  |t Low-Affinity Homologous Genes --  |g 4.3.1.1.  |t Rifamycin Low-Affinity RpoB --  |g 4.3.1.2.  |t Mutated Genes Conferring Resistance to Quinolone, Fluoroquinolone and Aminocoumarins --  |g 4.3.1.3.  |t PBP2a: A Low-Affinity Penicillin-Binding Protein --  |g 4.3.1.4.  |t Dihydropteroate Synthases Not Inhibited by Sulfonamide --  |g 4.3.2.  |t Chemical Modification of Antibiotic Target --  |g 4.3.2.1.  |t 23S rRNA Modification --  |g 4.3.2.2.  |t 16S rRNA Modification --  |g 4.3.2.3.  |t Reprogramming Chemical Composition of a Bacterial Cell-Wall Precursor --  |g 4.3.3.  |t Ribosomal Protection and Tetracycline Resistance --  |g 4.3.4.  |t Chromosomal Mutations in Genes Required for Membrane Phospholipid Metabolism: Lipopeptide Resistance --  |g 4.3.5.  |t Covalent Modifications on Lipopolysaccharide Core Conferring Polymixine Resistance --  |g 4.4.  |t Efflux Systems --  |g 4.4.1.  |t The ATP-Binding Cassette (ABC) Superfamily --  |g 4.4.2.  |t The Major Facilitator Superfamily (MSF) --  |g 4.4.3.  |t The Small Multidrug-Resistance Family (SMR) --  |g 4.4.4.  |t The Resistance-Nodulation-Division (RND) Superfamily --  |g 4.4.5.  |t The Multidrug and Toxic Compound Extrusion (MATE) Family --  |g 4.5.  |t The Case Stories of Intrinsic and Acquired Resistances --  |g 4.5.1.  |t β-Lactam Resistome of P. aeruginosa: Intrinsic Resistance Is Genetically Determined --  |g 4.5.2.  |t Acquired Antibiotic Resistance in S. aureus --  |g 4.5.2.1.  |t Acquired Resistance to β-Lactams and Glycopeptides --  |g 4.5.2.2.  |t Acquired Resistance to Fluoroquinolones --  |g 4.6.  |t Strategies to Overcome Resistance. 
880 0 0 |6 505-01  |g 12.  |t Antibiotics Targeting Bacterial RNA Polymerase / Konstantin Brodolin --  |g 12.1.  |t Introduction --  |g 12.2.  |t Antibiotics Blocking Nascent RNA Extension --  |g 12.2.1.  |t Ansamycins (Rifamycins) --  |g 12.2.2.  |t Sorangicin --  |g 12.3.  |t Antibiotics Targeting RNAP Active Center --  |g 12.3.1.  |t Streptolydigin and Other Acyl-Tetramic Acid Family Antibiotics --  |g 12.3.2.  |t Lasso Peptides: Microcin j25 and Capistruin --  |g 12.3.3.  |t CBR703 Series --  |g 12.4.  |t Antibiotics Blocking Promoter Complex Formation --  |g 12.4.1.  |t Myxopyronin --  |g 12.4.2.  |t Corallopyronin --  |g 12.4.3.  |t Ripostatin --  |g 12.4.4.  |t Lipiarmycin --  |g 12.5.  |t Inhibitors Hindering σ-Core Interactions --  |g 12.5.1.  |t SB2 and Analogs (Phenyl-Furanyl-Rodanines) --  |g 12.6.  |t Inhibitors with Unknown Mechanisms and Binding Sites --  |g 12.6.1.  |t GE23077 --  |g 12.6.2.  |t Ureidothiophene --  |g 12.7.  |t Conclusions and Perspectives --  |g 12.7.1.  |t Bacterial RNA Polymerase Inhibitors are a Valid Source of Clinical Drugs --  |g 12.7.2.  |t The σ Subunit of RNAP Modulates Antibiotics Activity -- --  |g 13.  |t Inhibitors Targeting Riboswitches and Ribozymes / Claudio O. Gualerzi --  |g 13.1.  |t Introduction --  |g 13.2.  |t Riboswitches as Antibacterial Drug Targets --  |g 13.2.1.  |t Purine Riboswitches --  |g 13.2.2.  |t c-di-GMP (Bis-3'-5'-Cyclic Dimeric Guanosine Monophosphate) Riboswitch --  |g 13.2.3.  |t FMN Riboswitches --  |g 13.2.4.  |t Thiamine Pyrophosphate (TPP) Riboswitch --  |g 13.2.5.  |t Lysine Riboswitch --  |g 13.2.6.  |t SAM (S-Adenosylmethionine) Riboswitches --  |g 13.3.  |t Ribozymes as Antibacterial Drug Targets --  |g 13.4.  |t Concluding Remarks and Future Perspectives -- --  |g 14.  |t Targeting Ribonuclease P / Denis Drainas --  |g 14.1.  |t Introduction --  |g 14.2.  |t Targeting RNase P with Antisense Strategies --  |g 14.3.  |t Aminoglycosides --  |g 14.4.  |t Peptidyltransferase Inhibitors --  |g 14.5.  |t Substrate Masking by Synthetic Inhibitors --  |g 14.6.  |t Peculiar Behavior of Macrolides on Bacterial RNase P --  |g 14.7.  |t Antipsoriatic Compounds --  |g 14.8.  |t Conclusions and Future Perspectives -- --  |g 15.  |t Involvement of Ribosome Biogenesis in Antibiotic Function, Acquired Resistance, and Future Opportunities in Drug Discovery / Jason P. Rife --  |g 15.1.  |t Introduction --  |g 15.2.  |t Ribosome Biogenesis --  |g 15.3.  |t Antibiotics and Ribosome Biogenesis --  |g 15.4.  |t Methyltransferases --  |g 15.5.  |t Methyltransferase Integration into the Ribosome Biogenesis Pathway --  |g 15.6.  |t Ribosome Biogenesis Factors, Virulence, and Vaccine Development -- --  |g 16.  |t Aminoacyl-tRNA Synthetase Inhibitors / Thale C. Jarvis --  |g 16.1.  |t Introduction --  |g 16.2.  |t Enzymatic Mechanism of Action of aaRS --  |g 16.2.1.  |t Condensation of Amino Acid and Cognate tRNA --  |g 16.2.2.  |t Classification of aaRS --  |g 16.2.3.  |t Fidelity and Proof Reading --  |g 16.2.4.  |t Transamidation Pathway --  |g 16.2.5.  |t aaRSs as Targets for Antimicrobial Agents: General Modes of Inhibition --  |g 16.3.  |t aaRS Inhibitors --  |g 16.3.1.  |t Mupirocin, a Paradigm --  |g 16.3.2.  |t Old and New Compounds with aaRS Inhibitory Activity --  |g 16.3.2.1.  |t Natural Products That Inhibit aaRS --  |g 16.3.2.2.  |t AaRS Inhibitors Identified in Screening Programs --  |g 16.3.3.  |t Novel aaRS Inhibitors in Clinical Development --  |g 16.3.3.1.  |t CRS3123, a Fully Synthetic MetRS Inhibitor --  |g 16.3.3.2.  |t AN2690 (Tavaborole) and AN3365 (GSK2251052), Boron-Containing LeuRS Inhibitors --  |g 16.4.  |t Considerations for the Development of aaRS Inhibitors --  |g 16.4.1.  |t Resistance Development --  |g 16.4.2.  |t Selectivity over Eukarvotic and Mitochondrial Counterparts --  |g 16.4.3.  |t Spectrum of Activity --  |g 16.4.4.  |t Amino Acid Antagonism --  |g 16.5.  |t Conclusions -- --  |g 17.  |t Antibiotics Targeting Translation Initiation in Prokaryotes / Claudio O. Gualerzi --  |g 17.1.  |t Introduction --  |g 17.2.  |t Mechanism of Translation Initiation --  |g 17.3.  |t Inhibitors of Folate Metabolism --  |g 17.4.  |t Methionyl-tRNA Formyltransferase --  |g 17.5.  |t Inhibitors of Peptide Deformylase --  |g 17.6.  |t Inhibitors of Translation Initiation Factor IF2 --  |g 17.7.  |t PpGpp Analogs as Potential Translation Initiation Inhibitors --  |g 17.8.  |t Translation Initiation Inhibitors Targeting the P-Site. 
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