Frontiers in Anti-Infective Drug Discovery, Volume 9

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Title
Copyright
End User License Agreement
Contents
Preface
List of Contributors
Use of Preclinical and Early Clinical Data for Accelerating Antimicrobial Drug Development
Mahesh N. Samtani1,*, Amarnath Sharma1 and Partha Nandy1
INTRODUCTION
Drug, Bug and Host Interactions: Five Critical Factors
METHODOLOGICAL ASPECTS
Model for In-vitro MIC Distributions and Pathogen Frequency of Natural Occurrence
Model for In-vivo PK/PD Target
Population PK Parameters Representing Human Variability
Target Attainment Computation
Assumptions Adopted During Modelling And Simulation
CASE-STUDY RESULTS: APPLICATION OF MONTE-CARLO APPROACH
Target Indication and Patterns of In-vitro Killing
Pathogen Susceptibility and Natural Occurrence
PK/PD Target Based on The Murine Thigh Infection Model
Clinical PK
Monte Carlo Simulation Results
SUMMARY
CONSENT FOR PUBLICATION
CONFLICT OF INTEREST
ACKNOWLEDGEMENTS
APPENDIX 1A
APPENDIX 1B
REFERENCES
Post-Translational Modifications: Host Defence Mechanism, Pathogenic Weapon, and Emerged Target of Anti-Infective Drugs
Maria Amprazi1,2,#, Anastasia Tomatsidou3,4,#, Dimitra Paliogianni5,# and Vasiliki E. Fadouloglou6,*
INTRODUCTION
PTMS IN THE FRONTLINE OF EUKARYOTIC DEFENCE AND PATHOGENIC INVASION
Innate Immunity
Adaptive Immunity: Antibodies
Eukaryotic Regulatory Processes Are Pathogenic Targets
BACTERIAL PATHOGENICITY EMPOWERED BY PTMS
Yersinia Yops Effectors: An Arsenal of Post-Translational Modifiers
Activation of Bacterial Effectors by Host-Mediated Post-Translational Modifications
Localization of Bacterial Effectors to Membranes by Host-Mediated Post Translational Lipidations
Eliminylation: A Particular Case of Dephosphorylation
AMPylation: An Emerging Modification in Bacterial Pathogenicity
ADP-Ribosylation: An Ancient Modification with Huge Potential for Infection
Deamidation: From Biological Clock to Virulence Factor
Bacterial Deamidation of Host G Proteins
Bacterial Deamidation of Transcription Factors Pauses Host Protein Synthesis
Bacterial Deamidation Targets the Ubiquitin/Ubiquitin-Like Protein Signaling Pathways
Bacterial Infection Interferes with the Canonical Ubiquitination
Bacterial Proteins Modify and Disrupt the Host Ubiquitination Network
Bacterial Proteins Are Modified by the Host Ubiquitination Network
Bacteria have Evolved Non-Canonical Ubiquitinases and Deubiquitinases
Phosphoribosyl Ubiquitinases and Deubiquitinases
Ubiquitin Transglutaminases
THE MULTIPLE FACETS OF GLYCOSYLATION IN BACTERIAL PATHOGENICITY
O-Glycosylation of Bacterial Flagella
N-Glycosylation of Bacterial Surface Proteins
O-Glycosylation of Host Proteins by Bacterial Toxins
N-Glycosylation of Host Proteins by Bacterial Effectors
VIRAL PATHOGENICITY THOUGH PTMS
Coronavirus (CoV) Family
PTMS FOUND IN CORONAVIRUS PROTEINS
Glycosylation
Disulfide Bond Formation
Palmitoylation
Phosphorylation
Ubiquitination
How Coronaviruses Induce PTMs to Host Proteins
THE POTENTIAL OF PTMS IN THE NEW ERA OF BIOPHARMACEUTICALS, ANTIBIOTICS AND ANTIVIRALS
The Challenge of Engineering PTMs in Biopharmaceuticals
Potential Anti-Viral Drugs
Promising Antimicrobial Targets
PTMS IN NATURAL ANTIMICROBIAL PEPTIDES AID SEARCH FOR NOVEL THERAPEUTICS
Lasso Peptides
Thiopeptides
Lanthipeptides/lantibiotics
Class I lantibiotics
Class II Lantibiotics
Class III and IV Lantibiotics
CONCLUSION AND FUTURE PERSPECTIVES
CONSENT FOR PUBLICATION
CONFLICT OF INTEREST
ACKNOWLEDGEMENTS
REFERENCES
Scope and Limitations on the Potent Antimicrobial Activities of Hydrazone Derivatives
Jean Michel Brunel1,*
INTRODUCTION
Hydrazones as Potent Antimicrobial Agents
R is a Hydrogen
R is an Aryl Group
R is a Heterocyclic Ring
Sulfonylhydrazones
Ylidene Hydrazide Derivatives
CONCLUDING REMARKS
CONSENT FOR PUBLICATION
CONFLICT OF INTEREST
ACKNOWLEDGEMENTS
REFERENCES
Current Scenario of Anti-Leishmanial Drugs and Treatment
Priyanka H. Mazire1 and Amit Roy1,*
INTRODUCTION
History of Leishmaniasis
Morphology of Leishmania Parasites
Lifecycle of Leishmania Parasite
Classification of Leishmaniasis
Clinical Symptoms
Diagnosis of Leishmaniasis
Diagnosis of Cutaneous and Mucocutaneous leishmaniasis
Treatment for Leishmaniasis
CURRENTLY USED ANTI-LEISHMANIAL DRUGS
Amphotericin B
Mechanism of Action
Treatment Regimen
Miltefosine
Mechanism of Action
Treatment Regimen
Paromomycin (PM)
Mechanism of Action
Treatment Regimen
Pentavalent Antimonials ( SbV )
Mechanism of Action
Treatment Regimen
Pentamidine
Mechanism of Action
Treatment Regimen
Anti-leishmanial Activity of Compounds from Natural Sources
Plants
Marine Macroalgae
Endophytes
CONCLUSION
CONSENT FOR PUBLICATION
CONFLICT OF INTEREST
ACKNOWLEDGEMENTS
REFERENCES
Dengue Hemorrhagic Fever: The Potential Repurposing Drugs
Wattana Leowattana1,*, Pathomthep Leowattana2 and Tawithep Leowattana3
INTRODUCTION
DENV REPLICATION
DRUG REPURPOSING FOR DENGUE
RdRp Inhibitors
Balapiravir
Sofosbuvir
Ribavirin
Antibiotic
Doxycycline
Iminosugars
Celgosivir
UV-4B
Anti-parasitic drugs
Chloroquine (CQ)
Ivermectin
Mast Cell Stabilizers
Cromolyn and Ketotifen
Leukotriene Inhibitor and Platelet-activating Factor (PAF) Inhibitor
Montelukast and Rupatadine
CONCLUDING REMARKS
CONSENT FOR PUBLICATION
CONFLICT OF INTEREST
ACKNOWLEDGEMENTS
REFERENCES
Subject Index
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