Protein surface recognition: 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: ...

The discovery and characterization of protein-protein interactions / C. Bertoncini, A. Higueruelo, and Xavi Salvatella. Biophysics of protein-protein interactions / Irene Luque. On the logic of natural product binding in protein-protein interactivity / James J. La Clair. Interface peptide inhibitors of PPIs / Mark W. Peczuh, and Richard T. Desmond. Inhibition of protein-protein interactions by peptide mimics / Jorge Becerril ... [et al.]. Discovery of inhibitors of protein-protein interactions by screening chemical libraries / Carlos García-Echeverría. 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. In silico screening / F.J. Luque, and Xavier Barril. In vitro and in vivo screening : screening by nuclear magnetic resonance / Ernest Giralt. In vitro and in vivo screening : methods of high throughput screening / Wenjiao Song and Qing Lin. Case study : inhibitors of the MDM2-p53 protein-protein interaction / Sanjeev Shangary, Denzil Bernard, and Shaomeng Wang. Case study : the discovery of potent LFA-1 antagonists / Tom Gadek

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 Garcia-Echeverria; 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 Li SECTION D. CASE STUDIES; 10 Case Study: Inhibitors of the MDM2-…