Protein Surface Recognition (eBook)

Approaches for Drug Discovery

Ernest Giralt, Mark Peczuh, Xavier Salvatella (Herausgeber)

eBook Download: PDF

2010
John Wiley & Sons (Verlag)
978-0-470-97212-0 (ISBN)

Infos

A new perspective on the design of molecular therapeutics is emerging. This new strategy emphasizes the rational complementation of functionality along extended patches of a protein surface with the aim of inhibiting protein/protein interactions. The successful development of compounds able to inhibit these interactions offers a unique chance to selectively intervene in a large number of key cellular processes related to human disease.

Protein Surface Recognition presents a detailed treatment of this strategy, with topics including:

• an extended survey of protein-protein interactions that are key players in human disease and biology and the potential for therapeutics derived from this new perspective
• the fundamental physical issues that surround protein-protein interactions that must be considered when designing ligands for protein surfaces
• examples of protein surface-small molecule interactions, including treatments of protein-natural product interactions, protein-interface peptides, and rational approaches to protein surface recognition from model to biological systems
• a survey of techniques that will be integral to the discovery of new small molecule protein surface binders, from high throughput synthesis and screening techniques to in silico and in vitro methods for the discovery of novel protein ligands.

Protein Surface Recognition provides an intellectual 'tool-kit' for investigators in medicinal and bioorganic chemistry looking to exploit this emerging paradigm in drug discovery.

ERNEST GIRALT, Department of Organic Chemistry, University of Barcelona and Institute for Research in Biomedicine, Barcelona, Spain

MARK PECZUH, Department of Chemistry, University of Connecticut, USA

XAVIER SALVATELLA, ICREA and Institute for Research in Biomedicine, Barcelona, Spain

Inhalt

Preface

List of Contributors

SECTION A. PRINCIPLES

1 The discovery and characterization of protein-protein interactions

C. Bertoncini, A. Higueruelo, and Xavi Salvatella

2 Biophysics of protein-protein interactions

Irene Luque

SECTION B. APPROACHES

3 On the logic of natural product binding in protein-protein interactivity

James J. La Clair

4 Interface peptide inhibitors of PPIs

Mark W. Peczuh, and Richard T. Desmond

5 Inhibition of protein-protein interactions by peptide mimics

Jorge Becerril, Johanna M. Rodriguez, Pauline N. Wyrembak, and Andrew D. Hamilton

6 Discovery of inhibitors of protein-protein interactions by screening chemical libraries

Carlos García-Echeverría

SECTION C. TECHNIQUES

7 High-throughput methods of chemical synthesis applied to the Preparation of inhibitors of protein-protein interactions

Annaliese K. Franz, Jared T. Shaw, and Yuchen Tang

8 In silico screening

F.J. Luque, and Xavier Barril

9.1 In vitro and in vivo screening: Screening by Nuclear Magnetic Resonance

Ernest Giralt

9.2 In vitro and in vivo screening: Methods of High Throughput Screening

Wenjiao Song and Qing Lin

SECTION D. CASE STUDIES

10 Case Study: Inhibitors of the MDM2-p53 protein-protein interaction

Sanjeev Shangary, Denzil Bernard, and Shaomeng Wang

11 Case Study: The Discovery of Potent LFA-1 Antagonists

Tom Gadek

Index

Rezensionen

"This book picks up this trend and provides an excellent overview
of the current topics in the field of PPI modulation by small
molecules and peptides. . . Taken together, this excellent book is
very suitable both as an introduction to the field, as well as a
compendium for readers already familiar with the chemical approach
of modulating PPIs." (ChemMedChem, 2011)

Produkt-Details

• Erscheint lt. Verlag: 23.9.2010
• Sprache: englisch
• Themenwelt: Naturwissenschaften ► Biologie ► Biochemie
• Themenwelt: Naturwissenschaften ► Chemie
• Schlagworte: Able • AIM • along • APPROACHES • Biochemie u. Chemische Biologie • Biochemistry (Chemical Biology) • Biowissenschaften • Cell & Molecular Biology • Chance • Chemie • Chemistry • Complementation • Design • Development • Drug • Extended • Functionality • Large • Life Sciences • molecular • Molekularbiologie • New • patches • Perspective • Pharmaceutical & Medicinal Chemistry • Pharmazeutische u. Medizinische Chemie • Protein • Proteine • Rational • Recognition • strategy emphasizes • Successful • Surface • therapeutics • Wirkstoffforschung • Zell- u. Molekularbiologie
• ISBN-10: 0-470-97212-2 / 0470972122
• ISBN-13: 978-0-470-97212-0 / 9780470972120