This book focuses on peptides as drugs, a growing area of pharmaceutical research and development. It helps readers solve problems of discovering, developing, producing, and delivering peptide–based drugs.• Identifies promising new areas in peptide drug discovery• Includes chapters on discovery from natural sources, metabolic modification, and drug delivery• Overviews separation methods and techniques for analysis, bond formation, and purification• Offers readers both a professional reference and a text or resource for graduate–level students INDICE: 1 Peptide TherapeuticsNader Fatouhi1.1 History of peptides as drugs1.2 Factors limiting use of peptides in the clinic1.3 Advances that have stimulated the use of peptides as drugs1.4 The development of peptide libraries1.5 Modification of peptides to promote stability and cell entry1.6 Targeting peptides to specific cells1.7 Formulations to improve propertiesReferences2 Methods for the Peptide Synthesis and AnalysisJudit Tulla–Puche, Ayman El–Faham, Athanassios S. Galanis, Eliandre de Oliveira, Aikaterini A. Zompra, and Fernando Albericio2.1 Introduction2.2 Solid Supports2.3 Linkers2.4 Protecting Groups2.5 Methods for Peptide Bond Formation2.6 Solid–Phase Stepwise Synthesis2.7 Synthesis in Solution2.8 Hybrid Synthesis – Combination of Solid And Solution Synthesis2.9 Cyclic Peptides2.10 Depsipeptides2.11 Separation and Purification of Peptides2.12 Characterization of Peptides via Mass Spectrometry2.13 ConclusionsAcknowledgmentsAbbreviationsReferences3 Peptide Design Strategies for G–Protein Coupled Receptors (GPCRs)Anamika Singh and Carrie Haskell–Luevano3.1 Introduction3.2 Classification of GPCRs3.3 Catalogue of Peptide–Activated G–Protein Coupled Receptors3.4 Structure of GPCRs: Common features3.5 GPCR Activation3.6 Structure and Function of Peptide Hormones3.7 Design Approaches for GPCR selective peptide ligands3.8 ConclusionsAcknowledgementsReferences4 Peptide–Based Inhibitors of EnzymesAnna Knapinska, Sabrina Amar, Trista K. Robichaud, and Gregg B. Fields4.1 Introduction4.2 Angiotensin–Converting Enzyme and Neprilysin/Neutral Endopeptidase4.3 Peptide Inhibitors of the HIV–1 Viral Life Cycle4.4 Matrix Metalloproteinases4.5 Antrax Lethal Factor Inhibition by Defensins4.6 Kinases4.7 Glycosyltransferases (Oligosaccharyltransferases)4.8 Telomerase Inhibitors4.9 Tyrosinase4.10 Peptidyl–Prolyl Isomerase4.11 Histone Modifying Enzymes4.12 Putting It All Together: Peptide Inhibitor Applications in Skin Care4.13 Strategies for the Discovery of Novel Peptide InhibitorsAcknowledgmentsReferences5 Discovery of Peptide Drugs as Enzyme Inhibitors and ActivatorsJeffrey–Tri Nguyen and Yoshiaki Kiso5.1 Introduction5.2 Enzyme types that process peptides5.3 Amino acid drugs5.4 Serine proteases and blood clotting5.5 Diabetes mellitus5.6 Renin–angiotensin–aldosterone system5.7 Penicillin and Cephalosporin Antibiotics5.8 HIV Protease5.9 Peptide drugs under development5.10 DiscussionAcknowledgmentsReferences6 The Biochemistry and Pharmacology of Chemokines and Chemokine Receptors in Diseases and Development of Novel TherapeuticsRunquan Zhang, Won–Tak Choi, Maocai Yan, Srinivas Duggineni, Jing An, and Ziwei Huang6.1 Introduction6.2 Chemokine receptors in HIV–1 entry6.3 Chemokine receptors and HIV–associated dementia6.4 Chemokines and chemokine receptors6.5 Chemokine receptor inhibitorsAcknowledgmentsReferences7 Discovery of peptide drugs from natural sourcesSonia Troeira Henriques and David J. Craik7.1 Introduction7.2 Peptides are involved in the host defense mechanism of living organisms7.3 Animal venoms, a rich source of peptides with therapeutic potential7.4 Optimization of peptides for drug development7.5 ConclusionsAcknowledgmentsReferences8 Modification of Peptides to Limit MetabolismIsuru R. Kumarasinghe and Victor J. Hruby8.1 Introduction8.2 Introduction of unnatural amino acids8.3 Cyclization of linear peptides to improve stability towards blood and brain protease degradation8.4 Introduction of D–amino acids into peptides improves stability towards blood and brain protease degradation8.5 Introduction of beta amino acids increases the stability towards blood and brain protease degradation8.6 Introduction of peptide bond isosteres8.7 Introduction of a N–methylation of the amide bond of peptides can improve the stability towards blood and brain protease degradation8.8 Use of unnatural amino acids – Use of topographically constrained amino acid8.9 Using glycosylated amino acids to increase the resistance of the proteolytic degradation8.10 Creation of peptides as multiple antigen peptide (MAP) dendrimeric forms increases the stability towards blood and brain protease degradation8.11 Halogenations of aromatic residues in peptides can reduce the enzymatic recognition required for peptide hydrolysis8.12 Concluding DiscussionReferences9 Delivery of Peptide DrugsJeffrey–Tri Nguyen and Yoshiaki KisoIntroduction9.1 Lipinski s Rule of Five9.2 Approaches to delivering peptide drugs9.3 Parenteral peptide drugs9.4 Topical peptide drugs for local effects9.5 Intranasal peptide drug delivery9.6 Enteral peptide drugs9.7 Different routes of administration for insulin9.8 DiscussionAcknowledgmentsReferences
- ISBN: 978-0-470-31761-7
- Editorial: Wiley–Blackwell
- Encuadernacion: Cartoné
- Páginas: 352
- Fecha Publicación: 08/04/2015
- Nº Volúmenes: 1
- Idioma: Inglés