LEADER 02890nam0-2200445---450- 001 990003521920203316 005 20111021133611.0 010 $a978-92-79-15707-3 035 $a000352192 035 $aUSA01000352192 035 $a(ALEPH)000352192USA01 035 $a000352192 100 $a20110414d2010----km-y0itay0103----ba 101 $aeng 102 $aLU 105 $a||||||||001yy 200 1 $aEU research fighting the three major deadly diseases$eHIV/AIDS, malaria and tuberculosis$e1. edition EU projects 2007-2010$fEuropean Commission, Directorate-General for Research 210 $aLuxembourg$cPublications office of the European Union$d2010 215 $a191 p.$cill.$d21 cm 225 2 $aEuropean Research Area. Health & life science 300 $aIn cop.: Project information 330 $aThe global emergency caused by HIV/AIDS, Malaria and Tuberculosis requires new approaches to confront the three major killing diseases around the world that are the origin and the consequence of serious poverty. In response to this emergency, The European Union provides a comprehensive approach in a wide range of policy areas, including trade, development and research. Research on HIV/AIDS, Malaria and Tuberculosis focuses on collaborative research at World level, developing new therapies, diagnostic and preventive tools. The Programme is sponsoring research on the entire spectrum, from basic molecular research through to preclinical tests and proof-of-principle studies. Research efforts confront the three diseases at the global level, but also address specific European aspects. Structures that were successfully built under the FP6 (2002-2006) are reinforced and complemented in the FP7. This catalogue shows the projects currently financed by the European Commission?s Seventh Research Framework Programme (FP7) since 2007 up to 2010, aiming at combating these three major killer diseases: HIV/AIDS, Malaria and Tuberculosis. [abstract tratto dalla pubblicazione] 410 1$12001$aEuropean Research Area. Health & life science 606 0 $aMalattie contagiose$xPrevenzione$yPaesi dell'Unione europea 606 0 $aMalattie infettive$xPrevenzione$yPaesi dell'Unione europea 676 $a616.905 699 $a18.01$bProgetti di ricerca 710 02$aCommissione europea :$bDirezione generale Ricerca$0542713 801 0$aIT$bsalbc$gISBD 856 4 $uhttp://dx.publications.europa.eu/10.2777/47563$4.$zAccesso libero online 912 $a990003521920203316 951 $aCDE 18.01 (XLIX)$bCDE 2639$cCDE 18.01$d00185298 959 $aBK 969 $aCDE 979 $aMARIAS$b90$c20110414$lUSA01$h1123 979 $aMARIAS$b90$c20111021$lUSA01$h1328 979 $aMARIAS$b90$c20111021$lUSA01$h1336 979 $aMARIAS$b90$c20140730$lUSA01$h1439 996 $aEU research fighting the three major deadly diseases$91114711 997 $aUNISA LEADER 10738nam 22004453 450 001 9910590098503321 005 20220806060222.0 010 $a3-527-83058-8 010 $a3-527-83060-X 035 $a(MiAaPQ)EBC7069549 035 $a(Au-PeEL)EBL7069549 035 $a(CKB)24342157200041 035 $a(EXLCZ)9924342157200041 100 $a20220806d2022 uy 0 101 0 $aeng 135 $aurcnu|||||||| 181 $ctxt$2rdacontent 182 $cc$2rdamedia 183 $acr$2rdacarrier 200 10$aDrug Development for Malaria $eNovel Approaches for Prevention and Treatment 210 1$aNewark :$cJohn Wiley & Sons, Incorporated,$d2022. 210 4$d©2023. 215 $a1 online resource (395 pages) 311 08$aPrint version: Kendrekar, Pravin Drug Development for Malaria Newark : John Wiley & Sons, Incorporated,c2022 9783527348602 327 $aCover -- Title Page -- Copyright -- Contents -- Part I Introduction -- Chapter 1 Chronology of Drug Development for Malaria -- 1.1 Introduction -- 1.1.1 Life Cycle of Malaria (Adapted from CDC) -- 1.2 Malaria - Erstwhile Memories -- 1.2.1 Progress Fighting Malaria -- 1.3 Current Chemotherapy Used to Treat Malaria -- 1.3.1 Current Combination Therapy -- 1.4 Drug Resistance of Antimalarial Drugs -- 1.4.1 Detection of Drug Resistance -- 1.5 Newer Drugs Approved for Malaria Treatment -- 1.6 Current Approaches to Developing a Malaria Vaccine -- 1.6.1 Hope for Vaccine Lies in the Parasite Itself -- 1.7 Conclusion: The Path Forward -- 1.7.1 RTS, ?S Vaccine: A New Tool with Potential for Africa -- References -- Part II Challenges and Opportunities in Malaria Therapy -- Chapter 2 Scientific Challenges and Treatment Opportunities in the Face of Shifting Malaria Epidemiology -- 2.1 Introduction -- 2.2 The Scientific Challenges Against Malarial Drug -- 2.3 Advances in Understanding and Managing Drug Resistance -- 2.3.1 Vector and Its Control -- 2.3.2 Parasite and Its Control -- 2.3.2.1 Malaria Vaccine -- 2.3.2.2 Antimalarial Drugs -- 2.4 Methods to Assess the Presence and Level of Drug Resistance -- 2.4.1 Therapeutic Efficacy of Antimalarial Drugs -- 2.4.2 Molecular Markers Associated with P. falciparum -- 2.5 Antimalarial Drugs Currently in Use and in the Pipeline -- 2.6 Future -- References -- Chapter 3 Emerging Formulation Technologies Against Malaria Resurgence -- List of Abbreviations -- 3.1 Introduction -- 3.1.1 Major Pathological Hallmarks of Malaria -- 3.1.2 Current Treatment Strategies -- 3.2 Pitfalls of the Current Treatment Regimen -- 3.2.1 Drug Resistance -- 3.2.2 High Drug Dose -- 3.2.3 Long?Term Treatment -- 3.2.4 Recurrence and Reversion of Diseases -- 3.3 Nanotechnology?Based Strategies for Targeting in Antimalarial Therapy. 327 $a3.3.1 Passive Targeting -- 3.3.2 Active Targeting -- 3.3.2.1 Hepatocyte Targeting -- 3.3.2.2 Erythrocyte Targeting -- 3.3.2.3 Brain Targeting -- 3.3.3 Rapid Diagnosis and Vector Control -- 3.4 Nano Formulations for Malarial Treatment -- 3.4.1 Lipid?Based Nanoplatforms -- 3.4.1.1 Nanoemulsion -- 3.4.1.2 Self?Emulsifying Drug Delivery System (SEDDS) -- 3.4.1.3 Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs) -- 3.4.1.4 Liposome -- 3.4.2 Polymer?Based Nanoplatforms for Malaria -- 3.4.2.1 Nanoparticles -- 3.4.2.2 Nanocapsules -- 3.4.2.3 Dendrimers -- 3.4.2.4 Micelles -- 3.4.2.5 Polymeric Hydrogel Nanoparticles -- 3.4.2.6 Nanosuspension -- 3.4.3 Organized Layer?by?Layer Assembly -- 3.4.4 Inorganic Nano?architectonics -- 3.4.4.1 Metallic Platforms -- 3.4.4.2 Quantum Dots -- 3.4.4.3 Carbon Nanostructures -- 3.4.4.4 Bio?ceramics -- 3.4.5 Bio?inspired Nanocarriers -- 3.4.5.1 Vaccines Based on Bio?inspired Nanocarriers -- 3.4.5.2 Bio?engineered Strategy Based on Erythrocytes -- 3.4.6 Protein-Peptide?Based Drug Delivery System -- 3.4.7 Stimuli?Responsive Platforms for Malaria -- 3.4.7.1 pH?Responsive Formulations -- 3.4.7.2 Thermo?Responsive Formulations -- 3.4.7.3 Redox State Responsive Substances -- 3.4.7.4 Stimuli?Responsive Liquid Crystalline Materials -- 3.5 Diagnostics -- 3.5.1 Stimuli?Responsive Iron Oxide and Gold Nanoparticle Reagent System -- 3.5.2 Immunological Adjuvants -- 3.5.3 Nanofibers -- 3.6 Challenges in Clinical Translation of Nanomedicine -- 3.6.1 Biological Challenges -- 3.6.2 Biocompatibility and Safety -- 3.6.3 Challenges in Manufacturing Scale?Up and Reproducibility -- 3.6.4 Analytical Characterization and Quality Control Challenges of Nano?Formulations -- 3.6.5 Regulatory Challenges -- 3.6.6 Other Challenges -- 3.7 Summary and Future Perspective -- 3.8 Conclusion -- Acknowledgments -- References. 327 $aChapter 4 Targeted Drug Delivery for Antimalarial Therapy -- 4.1 Introduction -- 4.2 Remodelling of Parasite?Infected Red Blood Cell (pRBC) -- 4.2.1 The Red Blood Cell Membrane (RBCM) -- 4.2.2 The Parasitophorous Vacuole Membrane (PVM) -- 4.2.3 The Parasite Plasma Membrane (PPM) -- 4.3 The Emergence of Resistance and Antimalarial Therapy Approach -- 4.4 Nanocarriers for Antimalarial Drug Delivery -- 4.4.1 Liposomes -- 4.4.2 Solid Lipid Nanoparticles (SLNs) -- 4.4.3 Nanostructured Lipid Carriers (NLCs) -- 4.4.4 Nano?emulsions (NEs) -- 4.4.5 Polymeric Nanoparticles -- 4.5 Targeted Antimalarial Drug Delivery Systems -- 4.5.1 Passive Drug Targeting with Conventional Nanocarriers -- 4.5.2 Active Drug Targeting with Surface?Modified Nanocarrier -- 4.6 Conclusion: Moving Towards the Future -- Acknowledgements -- References -- Chapter 5 The Imminent Threat of Antimalarial Drug Resistance -- 5.1 Introduction -- 5.2 Antimalarial Drugs: An Overview -- 5.3 The Evolution of CQ Resistance -- 5.3.1 Mechanism of Action of CQ -- 5.3.2 Basis of CQ Resistance -- 5.3.3 Prevalence of CQ Resistance -- 5.3.4 WHO Guidelines to Use CQ -- 5.4 Impact of Sulfadoxine-Pyrimethamine Resistance -- 5.4.1 Mechanism of Action of SP -- 5.4.2 SP Resistance -- 5.4.3 Distribution of DHPS and DHFR Mutation Across Globe -- 5.4.3.1 dhfr -- 5.4.3.2 dhps -- 5.4.4 WHO Guidelines to Use SP -- 5.4.4.1 IPTp Guidelines -- 5.4.4.2 IPTi Guidelines -- 5.5 ACT Resistance -- 5.5.1 Mechanism of Action of ART -- 5.5.2 ART Resistance and ACT Failure -- 5.5.3 WHO Guidelines -- 5.6 Conclusion: The Road Ahead -- References -- Chapter 6 Current Therapies and New Drug Targets for the Future Drug Development of Drug Resistant Malaria -- 6.1 Introduction -- 6.2 Life Cycle of Plasmodium falciparum -- 6.3 Current Antimalarial Therapy and Their Shortcomings -- 6.4 Drug Targets for Current Antimalarial Therapy. 327 $a6.4.1 Drug?Resistant Malaria and Identification of New Targets -- 6.4.1.1 Food Vacuole as Drug Targets -- 6.4.1.2 Shikimic Acid Pathway Targeting -- 6.4.1.3 Targeting Folate Pathway and Methionine Synthesis Pathway -- 6.4.1.4 Glycolytic Pathway Inhibition -- 6.4.2 Mitochondria as Drug Targets -- 6.4.2.1 Targeting Electron Transport Chain -- 6.4.2.2 Inhibition of Dihydroorate Dehydrogenase -- 6.5 Future Drug Development for the Treatment of Malaria -- 6.5.1 Benefits of Nanocarriers -- 6.5.2 Lipid?Based Drug Delivery -- 6.5.3 Liposomes (as Nanocarriers) -- 6.5.4 Nanostructured Lipid Carriers -- 6.5.5 Solid Lipid Nanocarriers -- 6.6 Conclusion -- References -- Part III Drug Development -- Chapter 7 Assays for Antimalarial Drug Discovery -- 7.1 Introduction -- 7.2 In Vitro Assays for Antimalarial Drug Discovery -- 7.2.1 Schizont Maturation Inhibition Assay (Microscopic Test) -- 7.2.2 In Vitro Micro Test Technique -- 7.2.3 Radioisotope Assay -- 7.2.4 Colorimetric Assay (Plasmodium Lactate Dehydrogenase Assay [pLDH]) -- 7.2.5 ELISA?Based Methods -- 7.2.5.1 DELI Assay -- 7.2.5.2 Assay Based on Histidine?Rich Protein II (HRP II) of P. falciparum -- 7.2.6 Flow Cytometry -- 7.2.7 Fluorometric Assay -- 7.2.8 ??Hematin Formation (Haemozoin Test) -- 7.2.9 Drug Interaction Assay and Isobologram Analysis -- 7.2.10 PCR?Based Methods -- 7.2.11 In Vitro Assays Targeting Exo?erythrocytic and Sexual Stages of the Parasite -- 7.2.11.1 Exo?erythrocytic Schizontocidal Assay -- 7.2.11.2 Ex?flagellation Assay -- 7.3 In Vivo Assays for Antimalarial Drug Discovery -- 7.3.1 Peters' 4?Day Test -- 7.3.2 Dose Ranging Full 4?Day Test -- 7.3.3 Onset/Recrudescence Test -- 7.3.4 Preventive Test -- 7.3.5 Curative Test -- 7.3.6 Hill's Test for Causal Prophylaxis and Residual Activity -- 7.3.7 Assays with P. berghei Green Fluorescent Protein (PbGFP). 327 $a7.3.8 Assays Employing Immunocompromised Mice -- 7.3.9 Primate Models for In Vivo Studies -- 7.3.10 Sporontocidal Assays -- 7.3.11 Anti?sporozoite Assay -- 7.4 Ex Vivo Assays for Antimalarial Drug Discovery -- 7.5 Assays for Assessment of In Vitro Toxicity -- 7.5.1 MTT Assay -- 7.5.2 XTT Assay -- 7.5.3 LDH (Lactate Dehydrogenase) Assay -- 7.5.4 Protein Content Assay -- 7.5.5 Neutral Red Uptake Assay (NRU) -- 7.6 Assays for Assessment of In Vivo Toxicity -- 7.6.1 Acute Toxicity -- 7.6.1.1 Limit Test of Lorke -- 7.6.1.2 Up and Down Procedure -- 7.6.2 Chronic Toxicity -- 7.7 Conclusion -- References -- Chapter 8 Aminoacyl?tRNA Synthetases as Malarial Drug Targets: A Structural Biology Perspective -- 8.1 Introduction -- 8.2 Pf/Pv?aaRSs -- 8.2.1 Pf/Pv Genome -- 8.2.2 Aminoacyl?tRNA Synthetases (aaRSs) -- 8.3 Aminoacyl?tRNA Synthetases as Druggable Targets -- 8.4 Biochemical Screening of Drug Libraries -- 8.4.1 Colorimetric Assays -- 8.4.2 Enzyme?Coupled Assays -- 8.4.3 Luciferase Assay -- 8.4.4 Assay to Test Synthetic as Well as Proofreading Activity -- 8.5 Structurally Validated Pf/Pv?aaRSs as Drug Targets -- 8.5.1 Lysyl?tRNA Synthetase (KRS) -- 8.5.2 Prolyl?tRNA Synthetase -- 8.6 Potential Drug Targets Pf/Pv?aaRSs -- 8.6.1 Leucyl?tRNA Synthetase (LRS) -- 8.7 Arginyl?tRNA Synthetase (RRS) -- 8.7.1 Tryptophanyl?tRNA Synthetase (WRS) -- 8.7.2 Tyrosyl?tRNA Synthetase -- 8.8 Others -- 8.9 Conclusion: The Road Ahead -- References -- Chapter 9 Natural Products as a Source for Antimalarial Drug Development Process - An Overview -- 9.1 Introduction -- 9.2 Phytochemicals as Antimalarial Agents: Recent Developments -- 9.2.1 Alkaloids -- 9.2.2 Terpenes -- 9.2.2.1 Sesquiterpene Lactones -- 9.2.2.2 Diterpenes -- 9.2.2.3 Triterpenes -- 9.2.2.4 Steroids and Others -- 9.2.3 Polyphenols -- 9.2.3.1 Biflavonoids -- 9.2.3.2 Prenylated Flavonoids -- 9.2.3.3 Other Flavonoids. 327 $a9.3 Traditional System of Medicine and Malaria. 608 $aElectronic books. 676 $a616.9362061 700 $aKendrekar$b Pravin$01254806 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910590098503321 996 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