Format:
xix, 402 Seiten
,
Illustrationen
,
24 cm
ISBN:
9781782628897
,
1782628894
Series Statement:
Drug discovery series 60
Content:
I. Appraisal of Leishmaniasis Chemotherapy, Current Status and Pipeline Strategies. Chapter 1. Leishmaniasis, Impact and Therapeutic Needs. The Natural History of Leishmaniasis ; Control Measures ; Existing Treatment Options, Recent Advances and Unmet Needs ; Conclusion. Development of an Elimination Tool -- Chapter 2. Anti-leishmanial Drug Discovery: Past, Present and Future Perspectives. Introduction ; Current Drugs for Leishmaniasis ; Medicinal Chemistry Challenges and Strategies to Discover New Anti-leishmanial Drugs ; Future Perspectives -- Chapter 3. From Bench to Bedside: Development and Optimization of Clinical Therapies for Visceral Leishmaniasis. Introduction ; The Role of Preclinical Models in Preclinical to Clinical Translation ; Challenges and Opportunities to Optimize Therapies for Leishmaniasis: The Case of Miltefosine ; Final Remarks
Content:
II. Methodologies and Medicinal Chemistry Strategies to Discover and Develop New Treatments. Chapter 4. Drug Assay Methodology in Leishmaniasis: From the Microplate to Image Analysis. Introduction ; Drug Assay Methods ; Models of Infection ; Detection ; Technological Innovations and Developments ; Summary -- Chapter 5. The Pursuit of Novel Anti-leishmanial Agents by High-throughput Screening (HTS) of Chemical Libraries. New Chemical Entities (NCEs) are an Unmet Need for Therapeutics of Kinetoplastid Diseases ; The Challenge of Choosing the Right Screening Tactics and Assays ; Case Studies of HTS Campaigns for Anti-Leishmanials ; Conclusions -- Chapter 6. Omics and Their Impact on the Development of Chemotherapy Against Leishmania. Introduction ; Genomics ; Transcriptomics ; Proteomics ; Metabolomics ; Concluding Remarks -- Chapter 7. In silico Tools for Target Identification and Drug Molecular Docking in Leishmania. Introduction ; Leishmania Targets Identification ; Anti-leishmanial Drug Development ; Target Databases ; Concluding Remarks and Outlook -- Chapter 8. Medicinal Chemistry Strategies to Discover New Leishmanicidal Drugs. Introduction ; Functional Scaffolds for Drug Discovery Against Leishmania ; Targets for Leishmaniasis Drug Discovery ; Conclusions -- Chapter 9. Natural Products as a Source of New Drugs Against Leishmania ; Leishmania, A Challenging Parasite ; The Interest in Natural Products as Scaffolds: Using a Rational Approach for Drug Discovery ; From a Crude Extract to a Pure Compound -- Aspects of Bioactive Compounds Isolation and Chemical Identification ; The Anti-leishmanial Potential of Natural Products in Animal Models ; Conclusions -- Chapter 10. Organometallic Compounds in Chemotherapy Against Leishmania. Introduction ; History and Clinical Use of Antimony-based Drugs ; Organoantimonial Compounds ; Organobismuth Compounds ; Organotin(iv) Compounds ; Organotellurium(iv) Compounds ; Iron- and Ruthenium-based Organometallic Compounds ; Palladium, Rhodium and Iridium-based Organometallic Compounds ; Conclusion -- Chapter 11. New Avenues for Drug Delivery in Leishmania: Using Treatment of Visceral Leishmaniasis with Amphotericin B as an Exemplar. Introduction ; Drug Delivery Systems (DDS) ; Parenteral Administration ; Oral Administration ; Pulmonary Administration ; Summary
Content:
III. The Quest for Achille's Heel of Leishmania. Singular Targets as New Avenues for Drug Development. Chapter 12. Addressing the Molecular Biology of Leishmania for Drug Development. Introduction ; The Leishmania Genome ; The Leishmania Transcriptome ; Post-transcriptional Regulation of Gene Expression ; Perspectives -- Chapter 13. The Physical Matrix of the Plasma Membrane as a Target: The Charm of Drugs with Low Specificity. Outline for an Antimicrobial Peptide-based Chemotherapy against Leishmaniasis ; General Appraisal of Peptide-based Therapies ; Natural History of AMPs ; Mechanism of Action of Antimicrobial Peptides ; Natural AMPs as Leishmanicidal Agents ; Assessment of Plasma Membrane Permeabilisation by AMPs in Leishmania ; Intracellular Targets ; Induction of Programmed Cell Death of Leishmania by Antimicrobial Peptides ; Structure-Activity Relationship of Leishmanicidal Antimicrobial Peptides ; Antimicrobial Peptides in Animal Models of Leishmaniasis ; Immunomodulation by Leishmanicidal AMPs ; The Outlook for AMP-based Therapies for Leishmaniasis ; Conclusions -- Chapter 14. Nutrient Transport and Sensing as Pharmacological Targets for Leishmaniasis. Introduction ; The Metabolic Environment Inside the Vector and Host ; Amino Acid Transport and Homeostasis ; Glucose Transport ; Purine, Pyrimidine and Nucleoside Transport ; Nutrient Sensing Has a Role in Virulence ; Can Nutrient Transporters Deliver Drugs into Leishmania Cells? ; Concluding Remarks -- Chapter 15. Carbon Metabolism as a Drug Target in Leishmania. Introduction ; Carbon Metabolic Network of Leishmania ; Drug Targets of Carbon Metabolism in Leishmania ; Functional and Structural Properties of Carbon-metabolic Enzymes that are Potential Drug Targets in Leishmania ; Drug Discovery ; Conclusions -- Chapter 16. The Redox Metabolism and Oxidative Stress in Leishmania as a Crossroads for the Lethal Effect of Drugs. Reactive Oxygen and Nitrogen Species and Leishmania ; Elimination of ROS and RNS ; Conclusions -- Chapter 17. DNA Topoisomerases as Promising Targets for Leishmania Chemotherapy. Introduction ; Supercoiled vs. Relaxed DNA. The Need for DNA Topoisomerases ; DNA Topoisomerases in Leishmania ; Other DNA Topoisomerases in Leishmania ; Conclusions -- Chapter 18. Molecular Basis of Drug Resistance in Leishmania. Emerging Drug Resistance ; Methods to Study Resistance ; Molecular Mechanisms of Resistance and Current Limitations ; Conclusions -- Chapter 19. The Macrophage-Parasite Interface as a Chemotherapeutic Target in Leishmaniasis. Introduction ; Phagocytosis and Phagolysosome Biogenesis ; The Membrane Fusion Machinery and the Phagosome ; Leishmania and Phagosome Remodelling ; The Parasitophorous Vacuole as a Potential Target for Drug Development ; Conclusions
Note:
Includes bibliographical references and index
Additional Edition:
ISBN 9781788010177
Additional Edition:
ISBN 9781788012584EPUB
Language:
English
Keywords:
Leishmaniose
;
Protozoozid
;
Arzneimittelforschung
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