GPCRs in Drug Discovery - Efforts to De-Orphanize Novel GPCR Targets are Increasing

Published: November 2011
No. of Pages: 143
Price: $ 3500

A superfamily of diverse transmembrane receptors, GPCRs help in the activation of cellular responses by interacting with molecules outside the cell. These molecules are known as ligands. The cellular responses are activated through a system of signaling pathways, called as signal transduction pathways. Human genome sequencing has helped us to understand the importance of these diverse classes of receptors, with about 1,000 sequences identified to be GPCRs. About 400 GPCRs bind with endogenous ligands; however such ligands have not been discovered for about 33% of all GPCR targets, thus emphasizing on the potential these receptors have as targets for future drug discovery.

Novel Research Methods are Being Employed to Identify and Develop Products that Target GPCRs More Effectively

The understanding of GPCR biology was limited for a very long time, although researchers were successful in identifying many GPCR targets using genomic approaches. However, there was no real understanding of the receptor structure-function relationship, and how different signaling molecules activated these receptors. Hence, the goal was to find the endogenous and/or exogenous ligands that paired with each GPCR, which could help the discovery of new avenues in therapy and de-orphanization of GPCRs. However, there are still more than 100 orphan GPCRs for which ligands have not yet been identified. This coupled with the fact that only about 30% of the 800 odd GPCRs have been targeted so far by currently marketed medicines leads to the conclusion that GPCR research has immense potential to bring out new therapies. Basic research advances concerning receptor X-ray structures, allosteric interactions and functional selectivity have opened the way for further exploitation of this large and diverse class of targets.

Research and Development Efforts in the Area of GPCRs will be Concentrated, Especially on De-Orphanization of Orphan GPCRs

Some of the new GPCRs discovered, especially those discovered through sequence homology, had one basic problem in that the endogenous ligands that bind to these receptors could not be identified. Hence, such receptors without any endogenous ligands were termed orphan GPCRs. One would think that functional activity of orphan GPCRs would be questioned as there are no known ligands that bind to these receptors, however expression of these orphan receptors in many different species accounts for their functional activity. Discovery of ligands that target orphan GPCRs is proving to be an extremely challenging task for researchers and for pharmaceutical and biotechnology companies all over the world. With the number of new molecules that get approval from the regulatory authorities falling drastically, coupled with the arrival of a patent cliff for the next four to five years, researchers are looking at the super-family of GPCRs with more interest than ever before. One of the most important segments of GPCR research concentrates on de-orphanizing GPCRs, identifying unknown ligands and establishing functional activity for orphan receptors.

Pipeline Analysis of Molecules Reveals the Central Nervous System, Oncology and Cardiovascular System to be the Most Targeted Therapeutic Classes

There are many programs looking at the role of GPCRs in obesity, the role of GPCRs in pain states, and in controlling tumorigenesis. A large number of CNS diseases involve GPCRs, ranging from depression to neurodegenerative diseases such as Alzheimer's disease, and they are therefore looked at in both the peripheral and the central nervous system. Many research papers defining receptor pharmacology use the brain for ligand-binding experiments. Modern research labs continue to study receptor pharmacology in brain tissue. There may be a preponderance of work on GPCRs in CNS because of this history, but there are lots of opportunities to progress GPCR therapeutics in many other areas.

Report overview

This report GPCRs in Drug Discovery - Efforts to De-Orphanize Novel GPCR Targets are Increasing provides insights in to the technical and commercial importance of G protein coupled receptors, which are the most important category of receptors in the human body. The report provides a scientific understanding of GPCRs and details the novel research methods being employed in the research of new targets and molecules that can be more effective in treating many indications. A special note on Orphan GPCRs and ways to de-orphanize them is followed by a detailed pipeline analysis to understand the therapeutic classes and indications that are being targeted through GPCRs. The report provides an in-depth analysis of the competitive landscape, including the profiling of top companies and licensing agreements involving GPCR molecules and platform technologies.

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Scope

The scope of this report includes -

• Detailed technical understanding of G protein coupled receptors

• Dedicated sections on Novel research methods being used to improve the GPCR targeted drug discovery and development process

• Understanding of Orphan GPCRs, its importance and novel methods to locate ligands and de-orphanize these receptors

• Pipeline analysis of products at various stages of development targeting receptors classified as GPCRs, including identification of major therapeutic areas and indications

• Analysis and review of important strategic partnerships and licensing agreements in the area of GPCR drug discovery and development

• The report also covers information on the leading market players and the competitive landscape, including specialist companies which have proprietary GPCR platform technology as well as major companies with molecules in not only the NDA Filed stage but also in Phase III

Reasons to buy

The report GPCRs in Drug Discovery will enhance your decision making capability. It will allow you to -

• Develop business strategies by understanding the trends shaping and driving research in the field of GPCRs

• Understand the potential areas of application for GPCR therapies.

• Identify key molecules targeting GPCRs in development based on the therapy.

• Identify the key players investing in GPCR platform technologies

• Optimize your R&D pipeline through identification of novel technologies being used in GPCR research to improve the drug discovery process

• Identify emerging players with a potentially strong product portfolio of molecules targeting GPCRs and create effective counter-strategies to gain a competitive advantage.

• What's the next big thing in GPCR research? – Identify, understand and capitalize.