Medicinal Chemistry Reviews

Volume 50, Chapter 12
Fifty Five Years of Structural Biology:  A Perspective on How Biophysics has Influenced Medicinal Chemistry
Mark C. Noe and Ravi G. Kurumbail

1.    Introduction                                                                                                                299

      1.1        Protein X-ray Crystallography                                                                       300

      1.2        Protein NMR and Biophysical Methods                                                       301

2.   Case Studies of Structure-Based Drug Design                                                           304

      2.1        Proteases                                                                                                         304

      2.2       Hydrolases                                                                                                       316

      2.3       Protein Kinases                                                                                               319

      2.4       Other Enzymes                                                                                                331

3.   New Frontiers in Structural Biology and Drug Discovery                                        334

      3.1        Fragment-Based Drug Discovery                                                          334         

      3.2       Structural Biology of Macromolecular Assemblies: Prokaryotic               
                 and Eukaryotic Ribosomes                                                                 336                            3.3       Structural Biology of Integral Membrane Proteins: G-Protein Coupled                                                  Receptors                                                                                         337

      3.4       Structural Biology of Integral Membrane Proteins: Ion Channels      339         

4.         Conclusion                 341

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