Proteinases as Drug Targets
This unique book describes newly discovered proteolytic enzymes and their biological function. In many cases, these enzymes are targets for new drug discovery in order to provide new therapeutic approaches to control human diseases and/or metabolic conditions. The chapters in this book will help other investigators to pursue drug discovery by detailing methods of production and assay of the enzymes. In addition, the latest structural studies that are described in the book will permit rapid advances in drug design. The most important elements of this book are the state-of-the-art, detailed descriptions of the properties of the proteolytic enzymes. The chapters in the book, written by leading experts in the field, collect the best work on the topics with complete bibliographies for each target enzyme. The illustrations are highly informative to aid and facilitate a new design of inhibitors that can be developed as drug candidates. Key chapters include those by Mark Gorrell and Catherine Abbott, both describing dipeptidyl peptidases, which have been implicated in a number of metabolic conditions including diabetes. The chapters are written from two very different perspectives, thus enriching the literature in this area. In addition, the chapter by Sheena McGowan focuses on aminopeptidases from the malaria parasite, Plasmodium falciparum, and the chapter by Ben Dunn deals with the aspartic peptidases from the same organism.
Proteinases as Drug Targets, The Royal Society of Chemistry, 2011.
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Table of contents
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Dipeptidyl Peptidases: Substrates and Therapeutic Targeting in Human Health and Diseasep1-43ByClaire H. Wilson;Claire H. WilsonSchool of Biological SciencesFlinders University, GPO BOX 2100Adelaide 5001South Australia,AustraliaSearch for other works by this author on:Catherine A. AbbottCatherine A. AbbottSchool of Biological SciencesFlinders University, GPO BOX 2100Adelaide 5001South Australia,AustraliaSearch for other works by this author on:
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Chapter 2: The Metalloproteases Meprin α and β: Pathophysiological Roles in Inflammation, Cardiovascular Disease, Cancer, and Fibrosisp44-61ByChristoph Becker-PaulyChristoph Becker-PaulyCell and Matrix BiologyJohannes Gutenberg-University, Johannes-von-Müller-Weg 6, D-55128 MainzGermanySearch for other works by this author on:
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Chapter 3: Glutamate Carboxypeptidase II as a Therapeutic Targetp62-95ByKlára Hlouchová;Klára HlouchováInstitute of Organic Chemistry and BiochemistryAcademy of Sciences of the Czech Republic, Flemingovo n. 2, 166 10 Praha 6Czech RepublicSearch for other works by this author on:Cyril BaŘinka;Cyril BaŘinkaInstitute of BiotechnologyAcademy of Sciences of the Czech Republic, Videnska 1093, 140 00 Praha 4Czech RepublicSearch for other works by this author on:Jan KonvalinkaJan KonvalinkaInstitute of Organic Chemistry and BiochemistryAcademy of Sciences of the Czech Republic, Flemingovo n. 2, 166 10 Praha 6Czech RepublicSearch for other works by this author on:
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Chapter 4: The Role of Proteolytically Inactive Serine Proteases from Sarcoptes scabiei in Complement Evasionp96-117BySimone Reynolds;Simone ReynoldsQueensland Institute of Medical Research and Australian Centre for International and Tropical Health and NutritionUniversity of QueenslandBrisbaneQueenslandAustraliaSchool of Veterinary SciencesUniversity of QueenslandSt. LuciaAustraliaSearch for other works by this author on:Katja FischerKatja FischerQueensland Institute of Medical Research and Australian Centre for International and Tropical Health and NutritionUniversity of QueenslandBrisbaneQueenslandAustraliaSearch for other works by this author on:
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Chapter 5: Targeting Dipeptidyl Peptidase-4 (DPP-4) and Fibroblast Activation Protein (FAP) for Diabetes and Cancer Therapyp118-144ByF. M. Keane;F. M. KeaneLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaSearch for other works by this author on:S. Chowdhury;S. ChowdhuryLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaSearch for other works by this author on:T.-W. Yao;T.-W. YaoLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaSearch for other works by this author on:N. A. Nadvi;N. A. NadviLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaPharmaceutical Chemistry, Faculty of PharmacyUniversity of SydneyNew South WalesAustraliaSearch for other works by this author on:M. G. Gall;M. G. GallLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaSearch for other works by this author on:Y. Chen;Y. ChenLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaSearch for other works by this author on:B. Osborne;B. OsborneLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaSearch for other works by this author on:A. J. V. Ribeiro;A. J. V. RibeiroLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaSearch for other works by this author on:W. B. Church;W. B. ChurchPharmaceutical Chemistry, Faculty of PharmacyUniversity of SydneyNew South WalesAustraliaSearch for other works by this author on:G. W. McCaughan;G. W. McCaughanLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaSearch for other works by this author on:M. D. Gorrell;M. D. GorrellLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaSearch for other works by this author on:D. M. T. YuD. M. T. YuLiver ImmunobiologyCentenary Institute and Sydney Medical School, University of SydneyNew South WalesAustraliaSchool of Engineering and Science—SES Life SciencesJacobs University Bremen, Campus Ring 6D-28759 BremenGermanySearch for other works by this author on:
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Chapter 6: Discovery of the Cysteine Protease Cathepsin B as a Drug Target for Alzheimer's Diseasep145-168ByVivian Hook;Vivian HookSkaggs School of Pharmacy and Pharmaceutical SciencesDepartments of Neurosciences, Pharmacology, and Medicine, University of California, La Jolla, CA 92093USASearch for other works by this author on:Mark Kindy;Mark KindyDepartment of NeurosciencesMedical University of South Carolina and the Ralph H. Johnson VA Medical Center, Charleston, SC 29425USASearch for other works by this author on:Gregory HookGregory HookAmerican Life Science Pharmaceuticals, Inc.San Diego, CA 92109USASearch for other works by this author on:
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Chapter 7: Plasmodium falciparum Neutral Aminopeptidases: Development of Novel Anti-Malarials by Understanding Enzyme Structurep169-185ByDonald Gardiner;Donald GardinerMalaria Biology LaboratoryThe Queensland Institute of Medical Research, 300 Herston Rd, HerstonBrisbaneQueensland 4006,AustraliaSearch for other works by this author on:John Dalton;John DaltonInstitute for the Biotechnology of Infectious Diseases (IBID)University of Technology Sydney, Level 6, Building 4, Corner of Thomas and Harris Street, UltimoSydneyNSW 2007,AustraliaInstitute of ParasitologyMcGill University, 21111 Lakeshore RoadSainte-Anne De BellevueQC H9X 3V9,CanadaSearch for other works by this author on:Sheena McGowanSheena McGowanDepartment of Biochemistry and Molecular BiologyMonash University, Clayton Campus, MelbourneVIC, 3800AustraliaSearch for other works by this author on:
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Chapter 8: Blood-Feeding Human Hookworm Proteasesp186-198ByA. Loukas;A. LoukasQueensland Tropical Health AllianceJames Cook UniversityCairnsQLD 4878AustraliaSearch for other works by this author on:N. Ranjit;N. RanjitQueensland Tropical Health AllianceJames Cook UniversityCairnsQLD 4878AustraliaSchool of Veterinary MedicineUniversity of PennsylvaniaPhiladelphiaPA 19104USASearch for other works by this author on:D. A. Pickering;D. A. PickeringQueensland Tropical Health AllianceJames Cook UniversityCairnsQLD 4878AustraliaSearch for other works by this author on:M. S. PearsonM. S. PearsonQueensland Tropical Health AllianceJames Cook UniversityCairnsQLD 4878AustraliaSearch for other works by this author on:
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Chapter 9: Pharmacological Targeting of Human Tissue Kallikrein-Related Peptidasesp199-228ByGeorgios Pampalakis;Georgios PampalakisUniversity of PatrasDepartment of Pharmacy, Rion-Patras, 26500GreeceSearch for other works by this author on:Georgia SotiropoulouGeorgia SotiropoulouUniversity of PatrasDepartment of Pharmacy, Rion-Patras, 26500GreeceSearch for other works by this author on:
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Chapter 10: Structural Mechanisms of Inactivation in Proteolytically Inactive Serine Proteases from Sarcoptes scabieip229-241ByKatja Fischer;Katja FischerScabies LaboratoryQueensland Institute of Medical Research Brisbane, 4029AustraliaSearch for other works by this author on:James A. Irving;James A. IrvingThe Department of Biochemistry and Molecular BiologySchool of Biomedical Sciences, Faculty of Medicine, Nursing and Health Sciences, Monash UniversityClaytonVictoria3800AustraliaSearch for other works by this author on:Robert Pike;Robert PikeThe Department of Biochemistry and Molecular BiologySchool of Biomedical Sciences, Faculty of Medicine, Nursing and Health Sciences, Monash UniversityClaytonVictoria3800AustraliaSearch for other works by this author on:Ashley M. BuckleAshley M. BuckleThe Department of Biochemistry and Molecular BiologySchool of Biomedical Sciences, Faculty of Medicine, Nursing and Health Sciences, Monash UniversityClaytonVictoria3800AustraliaSearch for other works by this author on:
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Chapter 11: The Aspartic Proteinases from the Malaria Parasite: Structure and Function of the Plasmepsinsp242-269ByBen M. DunnBen M. DunnDepartment of Biochemistry & Molecular BiologyUniversity of Florida College of Medicine, PO 100245GainesvilleFL32610-0245USASearch for other works by this author on:
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