GPCRs Mining the Richest Vein in Drug Discovery

This Report Evaluates Key Issues in Exploiting the Full Therapeutic Potential of GPCRs:

Efforts to identify ligands, or to develop ligand-independent means of targeting receptors.

New technologies and approaches to GPCR screening and targeting.

Potential solutions to the lack of structural information about GPCRs.

Pharmaceutical and biotechnology companies have long recognized the therapeutic potential of targeting G protein-coupled receptors (GPCRs). The success of GPCR-targeted drugs is well documented; blockbusters Zyprexa (Eli Lilly) and Clarinex (Schering-Plough) each generated more than $2 billion in sales in 2000. GPCRs: Mining the Richest Vein in Drug Discovery, examines the leading technologies that competitors in this market are using to further exploit GPCRs and their ligands, as well as downstream molecules, in the development of branded pharmaceuticals. 

The flood of gene sequence and gene expression data has made identifying novel GPCRs considerably easier than it was a decade ago. Yet, significant challenges still must be overcome before the full potential of GPCRs can be realized. Most GPCRs (including sensory receptors) remain orphans, i.e., their ligands are unknown. Ligand identification thus continues to be a major focus, although some players have opted to circumvent ligand identification and are instead concentrating their efforts on ligand-independent means of targeting receptors. 

The report addresses the following challenges to the development of GPCR-targeting drugs:

What is the most efficient way to identify ligands?

Which sites are necessary for ligand binding?

What does oligomerization mean for drug design and therapeutic efficacy?

How does one create a compound specific enough to distinguish between closely related receptors that can trigger very distinct pathways?

The hurdles are daunting, but given the pharmaceutical industry’s prior successes with this target class, and the huge amount of genomic and proteomic information now available, the commercial prospects for GPCR-targeted discovery and development services are robust. This report is crucial reading for companies seeking to profit from this steadily growing marketplace. 

Thought Leaders Interviewed for This Report:

Haim Aviv, Oren M. Becker, Dale S. Dhanoa, Michael Kauffman, Silvia Noiman, & Sharon Shacham, Predix Pharmaceuticals, Inc.; Theresa Branchek, Synaptic Pharmaceutical Corporation; Joseph P. Brown, LifeSpan BioSciences Inc.; Neil Cook, PerkinElmer Life Sciences; Richard Eglen, Pyare Khanna, Tony Lima, & Enal Razvi, DiscoveRx Corporation; John Harrington & Robert W. Mays, Athersys Inc.; Peter Moldt, 7TM Pharma; Stephen Oldfield, Molecular Devices Corporation; Terry E. Willard, Norak Biosciences Inc.

Publication date/length: June 2003, 116 pages.

Publisher: Cambridge Healthtech Institute

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