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.
Mục lục
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
Giới thiệu về tác giả
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
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