Gene Family Targeted Molecular Design

Preface.Contributors.Chapter 1: Drug Discovery by Gene Family (Karen Lackey).1.1 General drug discovery components.1.2 Further reading for expert knowledge.1.3 References.Chapter 2: G-Protein Coupled Receptors (Stephen Garland and Tom Heightman).2.1 Introduction.2.2 GPCR Structure and Function.2.3 Challenges Facing the Area of GPCR Drug Discovery.2.4 Conclusions and Outlook.2.5 References.Chapter 3: Ion Channels Gene Family: Strategies for Discovering Ion Channel Drugs (Maria L Garcia and Gregory J. Kaczorowski).3.1 Introduction.3.2 Ion Channel Sub-Family Descriptions.3.3 Structure of Potassium Channels.3.4 Criteria for Selection of Targets and Establishing Screens.3.5 A Case Study in Ion Channel Drug Discovery.3.6 Perspective on Ion Channels as Drug Targets.3.7 Ion Channel References.Chapter 4: Integrins (David D. Miller).4.1 Introduction.4.2 Integrin Inhibitor Discovery.4.3 Structure Based Design.4.4 Challenges - Past and Future.4.5 References.Chapter 5: Strategies for Discovering Kinase Drugs (Jerry Adams, Paul Bamborough, David Drewry and Lisa Shewchuk).5.1 Introduction.5.2 Protein Kinase Structural Features.5.3 Generating and Optimizing Kinase Inhibition.5.4 Establishing Screens for Understanding Kinase Activity and Selectivity.5.5 Case Studies of Successful Kinase Drug Discovery.5.6 Kinase References.Chapter 6: Protease-Directed Drug Discovery (Richard Sedrani, Ulrich Hommel and J"rg Eder).6.1 Introduction.6.2 Aspartic Proteases.6.3 Metalloproteases.6.4 Serine Proteases.6.5 Cysteine Proteases.6.6 Perspective on Proteases as Drug Targets.6.7 Protease References.Chapter 7: Small Molecule Inhibitors of Protein-Protein Interactions: Challenges and Prospects (Adrian Whitty).7.1 Introduction.7.2 Structure and Properties of PPI.7.3 Structural and Physicochemical Challenges to Inhibiting PPI with Small Molecules.7.4 Identifying Hits and Leads Against PPI Targets.7.5 Assessing the Druggability of New PPI Targets.7.6 References.Chapter 8: Transporters (Anne Hersey,

Karen E. Lackey is the Vice President of Chemistry in Molecular Discovery Research at GlaxoSmithKline. She is responsible for exploratory chemistry and new technology early stage research. Prior to her current assignment, Lackey served as International Director of Systems Chemistry in Discovery Research for GlaxoSmithKline, responsible for generating multiple chemical series for over ten therapeutic areas of drug discovery.

"The authors offer useful information regarding medicinal chemistry and drug discovery for early career as well as established academic and industrial scientists." (Doody's Reviews, May 2009) "This book is well written by knowledgeable scientists primarily from the pharmaceutical industry. Their collective years of experience are apparent in the descriptions of small molecule development for various drug targets." (Doody's, April 2009)