Abstract
G Protein-Coupled Receptors (GPCRs) account for 50% of the current drug targets, and remain about one-third of the drug discovery effort in the drug discovery-development community. As a result of the sequencing of the human genome, more than 150 orphan and non-chemosensory GPCRs have been identified for which their cognate ligands or biological functions are unknown. De-orphanization of those receptors could bring novel therapeutic targets to the industry against which novel therapeutics could be designed. In addition, current GPCR-based drugs only target ~30% of the approximately 200 known GPCRs in the genome. This is a rich target class that is highly-druggable.This Report will benefit those companies, institutions, and individuals requiring an in-depth and thorough analysis of the technical areas in GPCRs, the emerging technologies in this space, as well as qualitative and quantitative market analyses, trends, and attendant business opportunities. Further, this Report provides thorough profiles of those companies currently active within the GPCR space.
Table of Contents
Chapter 1: Overview
- Scope of this Report: Technology and Market Trends in the GPCR Target Space 1--1
- Top Technical Trends in GPCR Research and Drug Discovery 1--2
- Unmet Needs in the GPCR Interrogation/Analysis Tools and Technology Space 1--3
- Cell-based Assays for GPCR Interrogation and Analysis: Pros and Cons 1--4
- Classification of GPCR Ligands 1--6
- Correlating Structure with Function for GPCRs 1--8
- GPCR Biology 1--9
- Half of All Pharmaceuticals Address GPCRs. Why Then is Drug Discovery Addressing GPCR Targets so Fraught with Uncertainty? 1--10
- GPCR Industry Challenges 1--13
- Contents of this Report 1--13
Chapter 2: Emerging Technologies and Areas of Focus in the GPCRs Space
- Scope 2--1
- Introduction to the Chapter 2--1
- Emerging Bioinformatics Approaches in the GPCRs Space: Predicting Ligands for Orphan GPCRs . 2--2
- Pairwise Sequence Searches 2--2
- Profile Methods 2--2
- Support Vector Machines 2--3
- Agglomerative Clustering Methods 2--4
- Motif-based Classifiers 2--4
- Alignment-independent Approaches to GPCR Classification 2--5
- Computational Approaches to Interrogate Aminergic GPCRs 2--7
- The Approach 2--8
- Emerging G-Protein Coupled Receptor Assay Technologies 2--9
- What can be Measured? 2--10
- Receptor Ligand Binding and GTP Binding Assays 2--10
- Second Messenger Assays 2--12
- Protein Interaction Assays 2--14
- Trafficking Assays 2--17
- Gene Reporter Assays 2--19
- Bioimpedance Assays 2--20
- Multiplexed GPCR Assays 2--20
- Screening Strategies 2--23
- Technical References in the GPCRs Space 2--24
Chapter 3: Qualitative and Quantitative Market Analysis of the GPCRs Space
- Introduction to the GPCR Marketplace 3--1
- Market Analysis of the GPCR Space Based on an End-User Survey 3--2
- Breakout of Survey Respondents 3--3
- Survey Responses of a Predominantly Quantitative Nature 3--3
- Survey Responses of a Predominantly Qualitative Nature 3--9
- Key issues and challenges affecting the whole GPCR marketplace as a whole 3--9
- Key technologies deployed for GPCR screening 3--13
- Quantitative Metrics of the GPCR Landscape 3--16
- The Intellectual Property Landscape in the GPCRs Space 3--18
