subject: Aarkstore Enterprise -The Future of GPCRs in Drug Discovery: Novel technologies, leading companies, [print this page] The Future of GPCRs in Drug Discovery: Novel technologies, leading companies, and opportunities for target expansion
G-protein coupled receptors (GPCRs) constitute the largest, most ubiquitous, and most versatile family of membrane receptors. They also constitute the class of targets that has been most effectively exploited by the pharmaceutical industry, with approximately 30% of all currently marketed drugs acting on one or more GPCRs. Despite this, there are many GPCRs that have yet to be effectively exploited, for a variety of reasons. A number of new approaches to GPCRs are being explored that should lead to a much wider, and more effective, exploitation of this class of targets and thus provide sustained commercial success from these new developments.
Major opportunities are not solely offered by successfully targeting unexploited targets. Improved knowledge of GPCR structure and function has opened up many more opportunities for more effectively targeting exploited receptors. Better knowledge of the 3-dimensional structure of receptors, of receptor signalling pathways, and of alternative binding sites on receptors all offer new opportunities for the development of improved drugs. Such drugs may have better absolute selectivity or they may selectively modulate some aspects of receptor function.
The benefits of each strategic approach are explored, and the role of specialist companies in their exploitation is highlighted. These specialist companies provide major companies with opportunities to develop new strategic partnerships and licensing opportunities to reinforce their pipelines.
Key features of this report
Analysis of which classes of GPCR and which specific GPCRs have been exploited or explored.
Examination of novel approaches to targeting GPCRs and discussion of their benefits, such as exploiting X-ray structural data, targeting allosteric sites, and selectively modulating distinct GPCR signaling pathways.
Case histories highlighting how enhanced selectivity can be achieved by exploiting improved knowledge of GPCR targets.
Discussion of developments in targeting selected, recently deorphaned GPCRs.
Scope of this report
Understand how new opportunities in the GPCR field are not confined to underexploited or orphan GPCRs.
Gain awareness of the multiplicity of opportunities that are, or will become, available as knowledge of specific GPCRs improves.
Understand which specialist companies offer technologies that would make them most relevant as potential partners.
Identify which new approaches might be most relevant to specific project goals.
Key Market Issues
Commercial success in exploiting GPCRs has been almost exclusively confined to a minor fraction (approximately 30%) of the 184 non-orphan class A GPCRs, primarily to the receptors activated by monoamines.
The pharmaceutical industry still views the GPCR class of targets as offering considerable opportunities for commercial exploitation.
There is a considerable need for new and improved treatments for metabolic diseases, especially diabetes, many CNS disorders, and some inflammatory and autoimmune diseases such as COPD and multiple sclerosis. Targeting specific GPCRs for the treatment of these conditions remains an attractive option because of the druggability of this class of targets.
Key findings from this report
The pharmaceutical industry has more effectively exploited GPCRs than it has any other target class, with GPCRs accounting for about 30% of exploited targets and revenues of over $60 billion in 2009.
The vast majority (about 80%) of GPCRs have yet to be effectively or commercially exploited, for a variety of reasons, thus offering many opportunities.
Alternative methods of modulating GPCR function considerably amplify the number of potential opportunities with respect to both target and strategy, and they also enhance the prospects of obtaining secure intellectual property.
Specialist companies are leading the field in the exploitation of new approaches to the modulation of GPCR activity.
Key questions answered
1. Which GPCRs have been successfully exploited?
2. Which other GPCRs are currently viewed as desirable targets for exploitation?
3. Which recently deorphaned GPCRs have stimulated significant R&D activity?
4. Which targets are currently attracting the most attention?
5. Do opportunities remain for pursuing GPCRs which have already been commercially exploited?
6. Which targets are being pursued using new approaches to the selective modulation of GPCR function?
