Peptide drug discovery and development : translational research in academia and industry / edited by Miguel Castanho and Nuno C. Santos.

Format:

Book

Contributor:

Castanho, Miguel.

Santos, Nuno C.

Language:

English

Subjects (All):

Peptide drugs.

Drugs--Design.

Drugs.

Pharmacology.

Physical Description:

1 online resource (xix, 370 pages) : illustrations

Edition:

1st ed.

Place of Publication:

Weinheim, Germany : Wiley-VCH, 2011.

Language Note:

English

Summary:

Filling a real knowledge gap, this handbook and ready reference is both modern and forward-looking in its emphasis on the ""bench to bedside"" translational approach to drug development.Clearly structured into three major parts, the book stakes out the boundaries of peptide drug development in the preclinical as well as clinical stages. The first part provides a general background and focuses on the characteristic strengths and weaknesses of peptide drugs. The second section contains five cases studies of peptides from diverse therapeutic fields, and the lessons to be learned from them, wh

Contents:

Peptide Drug Discovery and Development: Translational Research in Academia and Industry; Contents; Preface; List of Contributors; Part I: The Academia - Market Bouncing of Peptide Drugs - Challenges and Strategies in Translational Research with Peptide Drugs; 1: Peptides as Leads for Drug Discovery; 1.1: Introduction; 1.2: Overview of Process for Transforming Peptides to Peptidomimetics; 1.3: HCMV Protease; 1.3.1: HCMV Protease: Identification and Characterization of Antiviral Inhibitors Targeting the Serine Protease Domain of the Human Cytomegalovirus (HCMV Protease)

1.3.2: Mapping Essential Elements of the Substrate Peptides and Determining Structures of Ligands Bound to HCMV1.3.3: Improving Peptide Activity to Allow SAR Studies; 1.3.4: Elucidation of the Binding Mode of the Optimized Peptidyl Segment; 1.3.5: Ligand Adaptations upon Binding; 1.3.6: Strategic Summary for HCMV Peptide Mimic Design Process; 1.4: HCV Protease; 1.4.1: HCV Protease as an Antiviral Target; 1.4.2: NS3 Serine Protease Possesses a Chymotrypsin-Like Fold; 1.4.3: Discovery of the Peptide DDIVPC as an Inhibitor of NS3 Protease

1.4.4: ''Sensemaking'' and Knowledge Building: Mapping of the Critical Binding Residues of the Peptide and Creation of an Inhibitor-Protease Model1.4.5: Knowledge Building: Monitoring Ligand Flexibility in the Free-State and Changes Upon Binding - P3 Rigidification; 1.4.6: N-Terminal Truncation and Improved P1, P2 and P5 Substituents; 1.4.7: Macrocyclization: Linking the Flexible P1 Side-Chain to P3; 1.4.8: HCV Protease Inhibitor BI00201335; 1.5: Herpes Simplex Virus; 1.5.1: Herpes Simplex Virus-Encoded Ribonucleotide Reductase Inhibitors; 1.6: Renin

1.6.1: Aspartyl Protease Renin as a Target1.7: HIV; 1.7.1: HIV Protease Inhibitors; 1.8: Conclusions; 2: Marketing Antimicrobial Peptides: A Critical Academic Point of View; 2.1: Introduction; 2.2: Basic Research: Antimicrobial Peptides; 2.3: Patents; 2.4: Potential Applications of AMPs; 2.5: Technology Transfer: Valorization, Licensing, or Spin-Off Creation; 2.6: Spin-Off Creation: An Academic Point of View; 3: Oral Peptide Drug Delivery: Strategies to Overcome Challenges; 3.1: Introduction; 3.2: Challenges Associated with Oral Peptide Delivery

3.2.1: Transport Pathways Across the Intestinal Epithelium3.2.2: Unfavorable Physicochemical Properties of Peptide Drugs; 3.2.2.1: Molecular Size, Hydrophilicity, and Physical Stability; 3.2.3: Physical Barriers of the Gastrointestinal Tract; 3.2.3.1: Transcellular Pathway; 3.2.3.2: Paracellular Pathway; 3.2.4: Biochemical Barriers of the Gastrointestinal Tract; 3.2.4.1: Luminal Enzymes; 3.2.4.2: Brush Border Membrane Bound Enzymes and Intracellular Enzymes; 3.2.5: Efflux Transport Systems; 3.2.6: Gastrointestinal Transit Time and Site-Specific Absorption; 3.3: Strategies to Overcome the Barriers of the Gastrointestinal Tract

Notes:

Description based upon print version of record.

ISBN:

9786613302519

9783527636747

3527636749

9781283302517

1283302519

9783527636730

3527636730

9783527636754

3527636757

OCLC:

761319845