Ernest Giralt & Mark Peczuh 
Protein Surface Recognition [PDF ebook] 
Approaches for Drug Discovery

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.

สารบัญ

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

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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