Diese Präsentation wurde erfolgreich gemeldet.
Wir verwenden Ihre LinkedIn Profilangaben und Informationen zu Ihren Aktivitäten, um Anzeigen zu personalisieren und Ihnen relevantere Inhalte anzuzeigen. Sie können Ihre Anzeigeneinstellungen jederzeit ändern.
Find Industry reports, Company profilesReportLinker                                                                       ...
Find Industry reports, Company profilesReportLinker                                                                   and ...
Find Industry reports, Company profilesReportLinker                                                                       ...
Find Industry reports, Company profilesReportLinker                                                                       ...
Nächste SlideShare
Wird geladen in …5
×

GPCRs: Dawn of a New Era'

305 Aufrufe

Veröffentlicht am

Current advances in functional screening methodologies, medicinal chemistry, and structure-based drug design have generated large increases in the number and diversity of GPCR drug targets. Furthermore, basic research advances have opened the way for still further exploitation of this target class. This report:Explores current and likely consequences of recent advances concerning GPCR x-ray structures, allosteric interactions, multimerization, and functional selectivity; Extensively tabulates marketed drugs and compounds in development arranged by receptor type and subtype; Presents in-depth interviews with recognized experts in the field. G protein-coupled receptors (GPCRs) are popular drug targets, accounting for about one-third of approved drugs and many hundreds of drugs currently in development. Yet one can easily argue that the pharmacologic potential of GPCRs is far from exhausted. Currently approved drugs address only a few GPCRs. Technologic and scientific advances have resulted in R&D pipelines that target a great many more GPCRs than are represented among currently marketed products. In this report, we examine newer technologies used in GPCR pharmacology.  

  • Hi! Get Your Professional Job-Winning Resume Here! 👉 http://bit.ly/rexumtop
       Antworten 
    Sind Sie sicher, dass Sie …  Ja  Nein
    Ihre Nachricht erscheint hier
  • Gehören Sie zu den Ersten, denen das gefällt!

GPCRs: Dawn of a New Era'

  1. 1. Find Industry reports, Company profilesReportLinker and Market Statistics >> Get this Report Now by email!GPCRs: Dawn of a New EraPublished on October 2008 Report SummaryCurrent advances in functional screening methodologies, medicinal chemistry, and structure-based drug design have generated largeincreases in the number and diversity of GPCR drug targets. Furthermore, basic research advances have opened the way for stillfurther exploitation of this target class.This report:Explores current and likely consequences of recent advances concerning GPCR x-ray structures, allosteric interactions,multimerization, and functional selectivity; Extensively tabulates marketed drugs and compounds in development arranged byreceptor type and subtype; Presents in-depth interviews with recognized experts in the field. G protein-coupled receptors (GPCRs)are popular drug targets, accounting for about one-third of approved drugs and many hundreds of drugs currently in development. Yetone can easily argue that the pharmacologic potential of GPCRs is far from exhausted. Currently approved drugs address only a fewGPCRs. Technologic and scientific advances have resulted in R&D pipelines that target a great many more GPCRs than arerepresented among currently marketed products. In this report, we examine newer technologies used in GPCR pharmacology. Table of ContentChapter 1INTRODUCTION: THE UNTAPPED PHARMACOLOGIC POTENTIAL OF GPCRS1.1. Research Advances StimulatingGPCR-Based Drug Discovery1.2. Goals and Organization of ReportChapter 2SCIENTIFIC BACKGROUND ANDTECHNOLOGIES2.1. Nature of GPCRsGPCRs as Drug TargetsGPCR Classification2.2. Compound SelectionFunctional Assays forGPCR Signaling Calcium Assays Cellular Dielectric Spectroscopy Beta-Arrestin AssaysStructure-Based Drug DiscoveryChapter 3GPCR PHARMACOLOGY: KEY ADVANCES IN BASIC RESEARCH3.1. Significance of GPCR StructuresX-RayCrystallographic Structure of the Beta2-Adrenergic Receptor…SolvedImplications for Structure-Based Drug Design forGPCRs3.2. Deorphanization3.3. Allosteric Modulators3.4. Dimers and Oligomers3.5. Functional SelectivityChapter 4APPLIEDRESEARCH4.1. Small Companies Push the Limits of GPCR Pharmacology7TM PharmaAcadiaPharmaceuticalsActelionAcurePharmaAddex PharmaceuticalsAdenosine Therapeutics (Acquired by Clinical Data)ArenaPharmaceuticalsCara TherapeuticsDimerix BioscienceEPIX PharmaceuticalsTrevena4.2. The GPCR PipelineSerotonin Receptors5-HT1 Receptor 5-HT2 Receptor 5-HT4 to 5-HT7 ReceptorsAdenosine Receptors A1 Receptor A2 and A3ReceptorsAdrenergic Receptors Alpha Adrenergic Receptor Beta Adrenergic ReceptorAngiotensin II ReceptorArginineVasopressin ReceptorBradykinin ReceptorsCalcitonin ReceptorsCannabinoid ReceptorChemokine ReceptorsCholecystokininReceptorMuscarinic Acetylcholine ReceptorCoagulation Factor II ReceptorCorticotropin-Releasing Hormone Receptor 1DopamineReceptorsEndothelin Receptor Type AGABAB ReceptorGlucagon Receptor FamilyMetabotropic GlutamateReceptorsGonadotropin-Releasing Hormone ReceptorGhrelin ReceptorHistamine ReceptorInterleukin 8ReceptorMelanin-Concentrating Hormone Receptor 1Melanocortin ReceptorMotilin ReceptorOpiate Receptor-Like 1 and OpioidReceptorsOxytocin ReceptorProstaglandin ReceptorsGPCR44Purinergic P2Y ReceptorsSphingosine-1-Phosphate Receptor1Tachykinin ReceptorsAdditional GPCR ModulatorsChapter 5DEALS, OBSERVATIONS, AND CONCLUSIONS5.1. SelectedGPCR-Related Deals5.2. Strengths and Weaknesses of GPCRs as a Target ClassStrengthsWeaknesses5.3. General Observationsand FindingsDiversity of GPCRs for Drug Discovery and DevelopmentTranslation of Basic Research and NewGPCRs: Dawn of a New Era (From Slideshare) Page 1/4
  2. 2. Find Industry reports, Company profilesReportLinker and Market Statistics >> Get this Report Now by email!TechnologiesFunctional Versus Ligand-Binding Screening Assays Cell Impedance Screening TechnologyRole of Allostery in DrugDiscovery and DevelopmentRole of Dimers and Oligomers in Drug Discovery and DevelopmentRelationship of Signaling Pathway toDiseaseDeorphanization and Unfamiliar GPCRsStructure-Based Drug Design5.4. ConclusionsChapter 6EXPERT INTERVIEWS6.1.Annette Gilchrist, PhDAdjunct Professor; Northwestern University6.2. Graeme Milligan, PhDProfessor of Molecular Pharmacology;Joint Research Director, Faculty of Biomedical and Life Sciences; University of Glasgow6.3. AnonymousScreening and ProfilingDirector; Major Pharmaceutical Company X6.4. P. Jeffrey Conn, PhDLee E. Limbird Professor of Pharmacology; Director, VanderbiltProgram in Drug Discovery; Vanderbilt University Medical Center6.5. Sidney Topiol, PhDAssociate Director, ComputationalChemistry; Lundbeck Research6.6. Vincent Mutel, PhDCEO, Vice Chairman, and Co-Founder; Addex PharmaceuticalsFIGURESFigure 2.1. Diagram of a FLIPR Instrument and Typical Kinetic TracingsFigure 2.2. Crystal Structure of the Beta2-AdrenergicReceptor ProteinTABLESTable 2.1. Major GPCR SubclassesTable 4.1. Launched Drugs Targeting Serotonin 1 ReceptorsTable 4.2.Drug Candidates for Serotonin 1 ReceptorsTable 4.3. Launched Drugs Targeting Serotonin 2 ReceptorsTable 4.4. Drug Candidatesfor Serotonin 2 ReceptorsTable 4.5. Launched Drugs Targeting Serotonin 4 ReceptorsTable 4.6. Drug Candidates for Serotonin 4ReceptorsTable 4.7. Drug Candidates for Serotonin 5, 6, and 7 ReceptorsTable 4.8. Drug Candidates for Adenosine A1ReceptorsTable 4.9. Drug Candidates for Adenosine A2 and A3 ReceptorsTable 4.10. Launched Drugs Targeting Alpha AdrenergicReceptorsTable 4.11. Drug Candidates for Alpha Adrenergic ReceptorsTable 4.12. Launched Drugs Targeting Beta-1 AdrenergicReceptorsTable 4.13. Drug Candidates for Beta-1 Adrenergic ReceptorsTable 4.14. Launched Drugs Targeting Beta-2 AdrenergicReceptorsTable 4.15. Drug Candidates for Beta-2 Adrenergic ReceptorsTable 4.16. Drug Candidates for Beta-3 AdrenergicReceptorsTable 4.17. Launched Drugs Targeting Angiotensin II Receptor, Type 1Table 4.18. Drug Candidates for ArginineVasopressin ReceptorsTable 4.19. Drug Candidates for Bradykinin ReceptorsTable 4.20. Drug Candidates for Calcitonin andCalcitonin-Like ReceptorsTable 4.21. Preclinical Drug Candidates for Cannabinoid 1 ReceptorsTable 4.22. Clinical Drug Candidatesfor Cannabinoid 1 ReceptorsTable 4.23. Drug Candidates for Cannabinoid 2 ReceptorsTable 4.24. Drug Candidates for ChemokineReceptorsTable 4.25. Drug Candidates for Cholecystokinin ReceptorsTable 4.26. Launched Drugs Targeting Muscarinic Receptor1Table 4.27. Drug Candidates for Muscarinic 1 and 2 Cholinergic ReceptorsTable 4.28. Launched Drugs Targeting MuscarinicReceptor 3Table 4.29. Drug Candidates for Muscarinic 3 Cholinergic ReceptorsTable 4.30. Drug Candidates for Coagulation Factor IIReceptorTable 4.31. Drug Candidates for Corticotropin-Releasing Hormone ReceptorsTable 4.32. Launched Drugs Targeting theDopamine D2 ReceptorTable 4.33. Drug Candidates for Dopamine ReceptorsTable 4.34. Drug Candidates for Endothelin ReceptorType ATable 4.35. Drug Candidates for GABAB ReceptorsTable 4.36. Drug Candidates for Glucagon and Glucagon-Like Peptide-1ReceptorsTable 4.37. Drug Candidates for Metabotropic Glutamate ReceptorsTable 4.38. Launched Drugs Targeting theGonadotropin-Releasing Hormone ReceptorTable 4.39. Drug Candidates for the Gonadotropin-Releasing Hormone ReceptorTable4.40. Drug Candidates for Ghrelin (aka Growth Hormone Secretagogue) ReceptorsTable 4.41. Launched Drugs Targeting theHistamine H1 and H2 ReceptorsTable 4.42. Drug Candidates for Histamine ReceptorsTable 4.43. Drug Candidates for Interleukin 8ReceptorsTable 4.44. Drug Candidates for Melanin-Concentrating Hormone Receptor 1Table 4.45. Drug Candidates for MelanocortinReceptorsTable 4.46. Drug Candidates for the Motilin ReceptorTable 4.47. Drug Candidates for Opiate Receptor-Like 1; Also forDelta 1 and Kappa 1 Opioid ReceptorsTable 4.48. Drug Candidates for Opioid Receptors Mu and SigmaTable 4.49. Drug Candidatesfor the Oxytocin ReceptorTable 4.50. Launched Drugs Targeting Prostaglandin ReceptorsTable 4.51. Drug Candidates forProstaglandin ReceptorsTable 4.52. Drug Candidates for GPCR 44Table 4.53. Drug Candidates for Purinergic ReceptorsTable 4.54.Drug Candidates for Sphingosine-1-Phosphate Receptor 1Table 4.55. Drug Candidates for Tachykinin ReceptorsTable 4.56.Launched Drugs Targeting Miscellaneous GPCRsTable 4.57. Miscellaneous GPCR-Targeted Drugs in DevelopmentTable 5.1.Selected Recent GPCR Candidate-Compound-Related DealsGPCRs: Dawn of a New Era (From Slideshare) Page 2/4
  3. 3. Find Industry reports, Company profilesReportLinker and Market Statistics >> Get this Report Now by email! Fax Order Form To place an order via fax simply print this form, fill in the information below and fax the completed form to: Europe, Middle East and Africa : + 33 4 37 37 15 56 Asia, Oceania and America : + 1 (805) 617 17 93 If you have any questions please visit http://www.reportlinker.com/notify/contact Order Information Please verify that the product information is correct and select the format(s) you require. GPCRs: Dawn of a New Era Product Formats Please select the product formats and the quantity you require. Hard Copy--USD 2 995.00 Quantity: _____ Digital Copy--USD 3 750.00 Quantity: _____ Contact Information Please enter all the information below in BLOCK CAPITALS Title: Mr Mrs Dr Miss Ms Prof First Name: _____________________________ Last Name: __________________________________ Email Address: __________________________________________________________________________ Job Title: __________________________________________________________________________ Organization: __________________________________________________________________________ Address: __________________________________________________________________________ City: __________________________________________________________________________ Postal / Zip Code: __________________________________________________________________________ Country: __________________________________________________________________________ Phone Number: __________________________________________________________________________ Fax Number: __________________________________________________________________________GPCRs: Dawn of a New Era (From Slideshare) Page 3/4
  4. 4. Find Industry reports, Company profilesReportLinker and Market Statistics >> Get this Report Now by email! Payment Information Please indicate the payment method, you would like to use by selecting the appropriate box. Payment by credit card Card Number: ______________________________________________ Expiry Date __________ / _________ CVV Number _____________________ Card Type (ex: Visa, Amex…) _________________________________ Payment by wire transfer Crédit Mutuel RIB : 10278 07314 00020257701 89 BIC : CMCIFR2A IBAN : FR76 1027 8073 1400 0202 5770 189 Payment by check UBIQUICK SAS 16 rue Grenette – 69002 LYON, FRANCE Customer signature:   Please note that by ordering from Reportlinker you are agreeing to our Terms and Conditions at http://www.reportlinker.com/index/terms Please fax this form to: Europe, Middle East and Africa : + 33 4 37 37 15 56 Asia, Oceania and America : + 1 (805) 617 17 93GPCRs: Dawn of a New Era (From Slideshare) Page 4/4

×