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Peptide and Peptidomimetic Therapeutics: From Bench to Beside offers applied, evidence-based instruction on developing and applying peptide therapeutics in disease treatment, driving drug discovery, and improving patient care. Here, researchers, clinicians and students will find tools to harness the full power of peptides and peptidomimetics and improve bioavailability, stability, efficiency and selectivity of new therapeutics and their application in treatment plans. More than 20 leaders in the field share their approaches for identifying and advancing peptide and peptidomimetic therapeutics. Topics examined run from "bench to bedside," beginning with fundamental peptide science, protein-protein interactions and peptide synthesis. Later chapters examine modes for peptide drug delivery, including cell penetration peptide and peptidomimetic delivery, as well as the targeting of specific disease types, peptide therapeutics as applied to infectious disease, cancer, metabolic disorders, neurodegenerative disorders, and skin disorders, and antiparasitic and immunosuppressive peptidomimetics.

Peptide drugs. --- Peptide drugs --- Design. --- Peptide pharmaceuticals --- Drugs --- Peptides --- Peptidomimetics --- Drug Design --- pharmacology --- therapeutic use --- Drug Design. --- pharmacology. --- therapeutic use.

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Leading scientists offer detailed profiles of ten protein drugs currently in development. The case histories of these important new compounds are described from the perspective of their formulation, characterization, and stability. This ready reference also features recent data and an abundance of previously unpublished information. The in-depth coverage includes a highly useful compendium of degradation sites occurring in over 70 proteins. An invaluable aid in the rapid identification of potential `hot spots' in proteins, this accessible compilation allows for inspection of the protein's primary structure and preparation of a hydroflex plot.

Protein drugs. --- Peptide drugs. --- Toxicology. --- Pharmacy. --- Pharmacology/Toxicology. --- Pharmacology. --- Chemistry --- Medicine --- Drugs --- Materia medica --- Pharmacology --- Drug effects --- Medical pharmacology --- Medical sciences --- Chemicals --- Chemotherapy --- Pharmacy --- Physiological effect --- Peptide pharmaceuticals --- Protein pharmaceuticals

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Macromolecular (specifically peptide-based) drugs could potentially be highly effective medicines. However they have a relatively short duration of action and variable therapeutic index. An example of such a peptide is Glucagon-like Peptide I which could potentially be used as a revolutionary drug for diabetes. This is because it stimulates insulin only when the blood glucose level is high thereby reducing the risk of hypoglycemia (a significant disadvantage of using insulin is that an insulin overdose is the single most potent cause of life-threatening hypoglycemia). However it’s short duration of action (half-life of 2 minutes in plasma) precludes its therapeutic use. In this volume, the use of novel therapeutics like GLP1 as an alternative to tradition insulin-based drugs in diabetes is described. Application of Peptide-Based Prodrug Chemistry in Drug Development elucidates the traditional concept of prodrugs as “specialized non-toxic protective groups used in a transient manner to alter or to eliminate certain limiting properties in the parent small molecule” (IUPAC definition). It goes on to provide insight into how prodrugs of peptides (with GLP1 as an example) could be appropriately used to extend the biological half life, broaden the therapeutic index of macromolecules and improve the pharmacodynamics of such drugs.  Author explains the logic behind designing peptide prodrugs, synthetic procedures and bioassays to examine the conversion of the prodrug to the drug under therapeutic conditions. The prodrugs described slowly convert to the parent drug at physiological conditions of 37C and pH 7.2 driven by their inherent chemical instability without the need of any enzymatic cleavage. The diketopiperazine and diketomorpholine (DKP and DMP) strategies for prodrug conversion are demonstrated in detail with special emphasis on the chemical flexibility that it offers to develop prodrugs with variable time actions. This book will be of useful to chemists, biochemists, medicinal chemists, biologists and people in the medical profession (doctors). It may be used in undergraduate classes but will certainly help post-graduate students and advanced professionals. The author is grateful to Prof. Richard DiMarchi (Standiford H. Cox Professor of Chemistry and the Linda & Jack Gill Chair in Biomolecular Sciences at Indiana University) for valuable suggestions. The foreword for the book has been written by Prof. Jean Martinez, (Legion d'Honneur awarded by the French Republic; Professor of Chemistry and Medicinal Chemistry of the University of Montpellier, France; and Chairman of European Peptide Society, 2002-2010).

Peptide drugs --- Drugs --- Drug design --- Pharmaceutical design --- Peptide pharmaceuticals --- Physiological transport. --- Design. --- Medicine. --- Pharmacology. --- Pharmaceutical technology. --- Diabetes. --- Biomedicine. --- Pharmaceutical Sciences/Technology. --- Pharmacology/Toxicology. --- Drug development --- Toxicology. --- Brittle diabetes --- Diabetes mellitus --- IDDM (Disease) --- Insulin-dependent diabetes --- Ketosis prone diabetes --- Type 1 diabetes --- Carbohydrate intolerance --- Endocrine glands --- Diabetic acidosis --- Glycosylated hemoglobin --- Chemicals --- Medicine --- Pharmacology --- Poisoning --- Poisons --- Pharmaceutical laboratory techniques --- Pharmaceutical laboratory technology --- Technology, Pharmaceutical --- Technology --- Diseases --- Toxicology --- Drug effects --- Medical pharmacology --- Medical sciences --- Chemotherapy --- Pharmacy --- Physiological effect

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Peptides --- Proteins --- Protéines --- Therapeutic use --- Emploi en thérapeutique --- Peptide drugs --- Drugs --- Protein drugs --- Metabolism --- Congresses --- Dosage forms --- Administration --- -Peptide drugs --- -Peptides --- -Protein drugs --- -Proteins --- -Proteids --- Biomolecules --- Polypeptides --- Proteomics --- Protein pharmaceuticals --- Organic compounds --- Amino acids --- Peptide pharmaceuticals --- Medicaments --- Medications --- Medicine (Drugs) --- Medicines (Drugs) --- Pharmaceuticals --- Prescription drugs --- Bioactive compounds --- Medical supplies --- Pharmacopoeias --- Chemotherapy --- Materia medica --- Pharmacology --- Pharmacy --- -Congresses --- Biopharmaceutics --- Chemistry, Pharmaceutical --- Dosage Forms --- Congresses. --- congresses. --- -Administration --- Protéines --- Emploi en thérapeutique --- Proteins - Metabolism - Congresses --- Peptide drugs - Dosage forms - Congresses --- Drugs - Administration - Congresses --- Peptides - Metabolism - Congresses --- Protein drugs - Dosage forms - Congresses --- Bile --- Calcitonin --- Insulin --- Interferons --- Microbial degradation --- Toxicity