GPCR Molecular Pharmacology and Drug Targeting : Shifting Paradigms and New Directions

G Protein-coupled Receptors (gpcrs) Are A Large Protein Family Of Transmembrane Receptors Vital In Dictating Cellular Responses. Gpcrs Are Involved In Many Diseases, But Are Also The Target Of Around Half Of All Modern Medicinal Drugs. Shifting Paradigms In G Protein Coupled Receptors Takes A Look At The Way Gpcrs Are Examined Today, How They React, How Their Mutations Lead To Disease, And The Many Ways In Which They Can Be Screened For Compounds That Modulate Them. Chemists, Pharmacologists, And Biologists Will Find Essential Information In This Comprehensive Reference. Frontmatter -- The Evolution Of Receptors: From On-off Switches To Microprocessors / Terry Kenakin -- The Evolving Pharmacology Of Gpcrs / Lauren T May, Nicholas D Holliday, Stephen J Hill -- The Emergence Of Allosteric Modulators For G Protein-coupled Receptors / Karen J Gregory, Celine Valant, John Simms, Patrick M Sexton, Arthur Christopoulos -- Receptor-mediated G Protein Activation: How, How Many, And Where? / Ingrid Gsandtner, Christian W Gruber, Michael Freissmuth -- Molecular Pharmacology Of Frizzleds With Implications For Possible Therapy / Gunnar Schulte -- Secretin Receptor Dimerization: A Possible Functionally Important Paradigm For Family B G Protein-coupled Receptors / Kaleeckal G Harikumar, Maoqing Dong, Laurence J Miller -- Past And Future Strategies For Gpcr Deorphanization / Anǧlique Levoye, Nathalie Clement, Elodie Tenconi, Ralf Jockers --^ High-throughput Gpcr Screening Technologies And The Emerging Importance Of The Cell Phenotype / Terry Reisine, Richard M Eglen -- Are ₃traditional₄ Biochemical Techniques Out Of Fashion In The New Era Of Gpcr Pharmacology? / Maria Teresa Dell'anno, Maria Rosa Mazzoni -- Fluorescence And Resonance Energy Transfer Shine New Light On Gpcr Function / Carsten Hoffmann, Moritz Bünemann -- Integration Of Label-free Detection Methods In Gpcr Drug Discovery / Oliver Nayler, Magdalena Birker-robaczewska, John Gatfield -- Screening For Allosteric Modulators Of G Protein-coupled Receptors / Christopher Langmead -- Ultra-high-throughput Screening Assays For Gpcrs / Priya Kunapuli -- New Techniques To Express And Crystallize G Protein-coupled Receptors / James C Errey, Fiona H Marshall -- Structure And Modeling Of Gpcrs: Implications For Drug Discovery / Kimberly A Reynolds, Vsevolod Katritch, Ruben Abagyan --^ X-ray Structure Developments For Gpcr Drug Targets / Michael Sabio, Sidney W Topiol -- Pharmacological Chaperones: Potential For The Treatment Of Hereditary Diseases Caused By Mutations In G Protein-coupled Receptors / Kenneth J Valenzano, Elfrida R Benjamin, Patricia René, Michel Bouvier -- Index. Edited By Annette Gilchrist. Includes Index. Includes Bibliographical References And Index. G Protein-coupled Receptors (gpcrs) Are A Large Protein Family Of Transmembrane Receptors Vital In Dictating Cellular Responses. Gpcrs Are Involved In Many Diseases, But Are Also The Target Of Around Half Of All Modern Medicinal Drugs. Shifting Paradigms In G Protein Coupled Receptors Takes A Look At The Way Gpcrs Are Examined Today, How They React, How Their Mutations Lead To Disease, And The Many Ways In Which They Can Be Screened For Compounds That Modulate Them. Chemists, Pharmacologists, And Biologists Will Find Essential Information In This Comprehensive Reference. Frontmatter -- The Evolution Of Receptors: From On-off Switches To Microprocessors / Terry Kenakin -- The Evolving Pharmacology Of Gpcrs / Lauren T May, Nicholas D Holliday, Stephen J Hill -- The Emergence Of Allosteric Modulators For G Protein-coupled Receptors / Karen J Gregory, Celine Valant, John Simms, Patrick M Sexton, Arthur Christopoulos -- Receptor-mediated G Protein Activation: How, How Many, And Where? / Ingrid Gsandtner, Christian W Gruber, Michael Freissmuth -- Molecular Pharmacology Of Frizzleds With Implications For Possible Therapy / Gunnar Schulte -- Secretin Receptor Dimerization: A Possible Functionally Important Paradigm For Family B G Protein-coupled Receptors / Kaleeckal G Harikumar, Maoqing Dong, Laurence J Miller -- Past And Future Strategies For Gpcr Deorphanization / Anǧlique Levoye, Nathalie Clement, Elodie Tenconi, Ralf Jockers --^ High-throughput Gpcr Screening Technologies And The Emerging Importance Of The Cell Phenotype / Terry Reisine, Richard M Eglen -- Are 3traditional4 Biochemical Techniques Out Of Fashion In The New Era Of Gpcr Pharmacology? / Maria Teresa Dell'anno, Maria Rosa Mazzoni -- Fluorescence And Resonance Energy Transfer Shine New Light On Gpcr Function / Carsten Hoffmann, Moritz Bünemann -- Integration Of Label-free Detection Methods In Gpcr Drug Discovery / Oliver Nayler, Magdalena Birker-robaczewska, John Gatfield -- Screening For Allosteric Modulators Of G Protein-coupled Receptors / Christopher Langmead -- Ultra-high-throughput Screening Assays For Gpcrs / Priya Kunapuli -- New Techniques To Express And Crystallize G Protein-coupled Receptors / James C Errey, Fiona H Marshall -- Structure And Modeling Of Gpcrs: Implications For Drug Discovery / Kimberly A Reynolds, Vsevolod Katritch, Ruben Abagyan --^ X-ray Structure Developments For Gpcr Drug Targets / Michael Sabio, Sidney W Topiol -- Pharmacological Chaperones: Potential For The Treatment Of Hereditary Diseases Caused By Mutations In G Protein-coupled Receptors / Kenneth J Valenzano, Elfrida R Benjamin, Patricia René, Michel Bouvier -- Index. Edited By Annette Gilchrist. Includes Index. Includes Bibliographical References And Index. "The focus of this book, G protein-coupled receptors (GPCRs) are a large protein family of transmembrane proteins that sense molecules outside the cell and relay the information, thus initiating cellular responses. When this molecular process breaks down, GPCRs become the culprit of many diseases, making them the target of nearly half of all modern medicinal drugs * G protein-coupled receptors (GPCRs), are a large protein family of transmembrane receptors that sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses. GPCRs are involved in many diseases, but are also the target of around half of all modern medicinal drugs. 01......Page 1 02......Page 19 03......Page 45 04......Page 79 05......Page 106 06......Page 131 07......Page 156 08......Page 183 09......Page 209 10......Page 227 11......Page 244 12......Page 270 13......Page 294 14......Page 318 15......Page 342 16......Page 403 17......Page 452 18......Page 478 index......Page 529