G-Protein coupled receptors are a hot property for drug developers — according to some estimates, 70 percent of all drugs marketed worldwide are targeted against the protein superfamily — and several firms are finding some success marketing commercial GPCR databases. So why is drug discovery startup Primal giving away its newly compiled GPCR data via its website? “From a business standpoint, we felt that the best way to advertise is through our discoveries,” said George Gaitanaris, president and CEO.
The two-year-old Seattle-based company published a paper in last week’s Proceedings of the National Academy of Sciences describing its methodology for identifying 367 GPCRs for endogenous ligands in humans — the full repertoire of these receptors in the human genome, according to the company. These include 26 GPCRs that Primal claims were not previously identified.
The publication of the paper, and the subsequent release of the GPCR data, serves as Primal’s official debut, Gaitanaris said. “We didn’t want to make a fuss until we had the information in our hands. This paper initiates a new phase for the company,” he said.
According to John Bergmann, senior scientific director, Primal followed a standard bioinformatics approach to uncover the subset of GPCRs that it refers to as “endoGPCRS,” which are involved in neuronal regulation, metabolism, reproduction, development, and behavior. They first performed a similarity search against the human genome for all known GPCRs to find tens of thousands of similar sequences. A second approach relied on hidden Markov models to identify an additional 1,100 potential receptors. The company narrowed this set down to 367 endoGPCRs in human and 392 in mouse, and then used RT-PCR to analyze the expression patterns of 100 of the mouse GPCRs to assess function. Gaitanaris said that since the PNAS paper went to press, Primal has performed expression profiling on the remainder of the genes.
Primal has posted much of its data on its website (www.primalinc.com), but not all of it. The company, which specializes in behavioral disorders, has filed for patent protection on the entire family of GPCRs, Gaitanaris said. Surprisingly, he noted, after extensive research, the company determined that only about 30 percent of known GPCRs have “solid” patents. Armed with this knowledge, the company filed its own applications and submitted the paper for publication. “We feel confident that we have a solid IP position…there was no reason not to share [the information],” he said.
The company welcomes researchers to poke around in the GPCR database to get a glimpse of its data, and Gaitanaris said the approach is already bearing fruit. Several organizations have already contacted the company about potential collaborations, he said.
Primal’s open approach doesn’t have GPCR database providers running scared. After reviewing the company’s data, Joe Brown, CEO of LifeSpan BioSciences, reported that “we and others have discovered and not reported a lot of the information” in the database. He estimated that only one or two of the GPCRs in the set are novel.
LifeSpan’s own GPCR database contains around 400 “non-olfactory” GPCRs, Brown said, roughly the equivalent category to Primal’s endoGPCRs. He added that LifeSpan filed for patent protection several years ago on 64 GPCRs.
Brown noted that LifeSpan has added extensive literature and patent curation to its GPCR database, and that pharmaceutical companies are more than willing to pay for the added value. The company has 15 subscribers to the database currently, he said, and signed a new subscription agreement two weeks ago with an undisclosed pharmaceutical firm.
“The database field has really been beaten up recently,” he said, “but we are seeing continued demand and need.”