Title page -- Preface -- List of Contributors -- Contents -- Conference Preface and Keynote Lecture -- Conference Preface -- Keynote Lecture - Targets for Therapy. Are We Doing Anything Well? -- A Thermodynamic Platform for Drug Discovery and Optimization -- Structure-Based Design: Past, Present, and Future -- Sense and Nonsense in Drug Discovery: A Chemical Perspective -- Synthesis at the Interface of Chemistry and Biology: How and Why? -- Drug Design with ADME in Mind: Recent Paradigm Shifts in Drug Discovery -- Hypothesis Generation for Scientific Discovery. Examples from the Use of KEM®, a Rule-Based Method for Multi-Objective Analysis and Optimization -- Does Size Matter? Facts and Thoughts on Recombinant Drugs -- Can Nanotechnology Improve the Oral Delivery of Therapeutic Proteins? -- The Omeprazole Story: How Endurance in Research May Pay Off -- Conceptual Design of Cannabinoid CB1 Receptor Antagonists -- Author Index.