CHAPTER 1: EXECUTIVE SUMMARY
Introduction to GPCRs and Focus of This Report
GPCR Categories, Signaling and Drug Discovery
Market Opportunity in the GPCRs Space
CHAPTER 2: MOLECULAR DETAILS OF GPCR CLASSIFICATION, BIOLOGY, AND
TECHNOLOGIES FOR THEIR INTERROGATION AND SCREENING
Scope of This Chapter
Overview of the GPCR Space
GPCR Signaling Cascades In Vivo—The Molecular Events Triggered Upon GPCR Activation
New Paradigms of GPCR Signaling
GPCR Cross Talk and Dimerization
RGS Proteins
GPCR Kinases (GRKs) and Desensitization of GPCRs
Orphan GPCRs (oGPCRs)
Structural Approaches: A Major Hurdle in GPCR Drug Discovery
GPCR Assay Technologies—How to Study GPCRs for Screening and Analysis Especially in Drug Discovery
Environments
Receptor Ligand Binding and GTP Binding Assays
Second Messenger Assays
Protein Interaction Assays
GPCR Trafficking Assays
Gene Reporter Assays
Bioimpedance Assays
Selected Technical References on GPCRs
CHAPTER 3: BUSINESS ANALYSIS OF THE G PROTEIN-COUPLED RECEPTORS (GPCRS)
SPACE
Scope of this Chapter
Analysis of the Pharmaceutical Targets Space and Overview of Druggability of Targets—Qualitative and
Quantitative Trends
GPCRs as Drug Targets
Market Trends in the GPCR Interrogation/Analysis Space—Qualitative and Quantitative Market Trends
Size of GPCR Interrogation/Analysis Screening Campaigns and the Overall Market Size
Qualitative Impressions of the GPCR Marketplace, Trends Therein, and Open Questions
The Intellectual Property Landscape for GPCRs and Other Biologics
References
CHAPTER 4: THERAPEUTICS PIPELINE: GPCR-ADDRESSING POTENTIAL DRUGS AND
TARGETS ADDRESSED
Scope of This Chapter
CHAPTER 5: COMPANY PROFILES
3M Pharmaceuticals
7TM Pharma
Arena
atugen
Euroscreen
APPENDIX 1: INTELLECTUAL PROPERTY OVERVIEW
Trademarks and Service Marks: Logos and Brand Names
Copyright: Written and Audiovisual Works
Trade Secrets: A Grab-Bag of Perpetual Secrets
A Short Patent Primer
Patents: Procedures and Players
After the Grant: Patent Litigation and Licensing
Patenting GPCRs and Other Proteins
The Four Key Elements of Patents: Patentable Subject Matter, Usefulness, Novelty, and
Non-obviousness
Subject Matter: What Can Be Claimed?
Usefulness: Proving the Receptor’s Function
Changes in the Utility Examination Guidelines
Meeting the New Utility Test: Characterizing Receptor Function
Novelty and Non-obviousness: Searching for Prior Art
Two More Elements: Adequate Written Descriptions and Enablement
Forging an IP-Savvy Business Model
Managing the Tradeoffs
Tradeoff #1: Patenting Early vs. Patenting Strong
Tradeoff #2: Patent Strength vs. Patent Cost
Tradeoff #3: Litigation and Licensing vs. The Core Business
When You Find Prior Art: Patenting a GPCR in the Face of Prior Discovery
Equivalent Inventions—The Impact of the Festo Case
Notes and References.
APPENDIX 2: IMPORTANT AND EMERGING THEMES IN THE GPCRS SPACE
