A gem of a partnership

Emerald BioStructures, FORMA Therapeutics partner to develop treatments for lymphoma and other cancers

Jeffrey Bouley
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BAINBRIDGE ISLAND, Wash.—Aimed at developing potential drug targets for its pipeline and discovering effective treatment for lymphoma and other cancers, small-molecule therapeutics developer FORMA Therapeutics Inc., headquartered in Cambridge, Mass., recently partnered with Emerald BioStructures.

This high-tech, multi-target, multiyear, gene-to-structure research partnership leverages Bainbridge Island, Wash.-based Emerald's X-ray crystallography expertise with FORMA's proprietary computational platform and Diversity Oriented Synthesis (DOS) chemistry capabilities, in order to elucidate key cancer targets and optimize the binding of FORMA's drug candidates.

The financial terms of the deal, announced June 29, were not disclosed, but the collaboration will provide funding to cover several full-time employees at Emerald BioStructures, a contract research organization that assists biotechnology firms, pharmaceutical companies, government organizations and academic institutions.

This collaboration with Emerald "highlights the breadth and depth of Emerald BioStructures' capabilities to fully integrate co-crystallization into the latest advances in drug discovery and highlights our interest in partnering with our customers," says Lance Stewart, CEO of Emerald BioStructures.

"Emerald has contributed to the structure-based design of multiple promising drug candidates for our customers, and we look forward to continuing to apply our leading-edge capabilities …  in support of FORMA's drug discovery activities," Stewart says. "Emerald will be expressing and purifying hundreds of protein targets selected by FORMA's cancer genomics platform, and in parallel, generating hundreds of co-crystal structures of inhibitors identified through FORMA's screening platform."

The partnership takes advantage of Emerald's proven ability to generate traditionally intractable X-ray crystal structures including protein-protein complexes, Stewart says.

"By combining this technology with FORMA's platforms, we believe the partnership creates an entirely new way to identify small-molecule lead series that modulate protein-protein interactions," he adds. "We believe this partnership will demonstrate that Emerald is redefining the paradigm for how structural biology adds value to drug discovery."

Emerald has industrialized the entire gene-to-structure process, allowing the company to significantly decrease the cost of obtaining protein-ligand co-crystal structures, Stewart adds. Emerald offers automated gene design and cloning together with high-throughput protein expression capabilities in E. coli, baculovirus infected insect cells and mammalian cells.

In addition, Emerald's protein purification methods and microfluidic crystallization "allows us to obtain traditionally difficult structures including membrane proteins, protein-protein complexes and protein-nucleic acid complexes," says Stewart.

Emerald also brings to the table a diverse set of biophysical screening technologies, including NMR, SPR and microcalorimetry, Stewart says. These screening technologies—together with Emerald's Fragments of Life library—can be used to identify new binding sites and novel ligands.

Emerald believes the sky is the limit.

"The number of X-ray co-crystal structures that will be generated in this collaboration is unprecedented, and will create a new paradigm for how high-throughput structural biology can accelerate hit discovery and lead development," Stewart said.

In January 2009, FORMA CEO Steve Tregay hinted at what was to come when he said publicly that FORMA would capitalize on the Cancer Genome Project to go after new targets and cancer types. FORMA then went public with the news that it raised $25 million. Part of that money came from the Novartis Option Fund and Singapore's Bio*One Capital, followed by "in-kind collaborations with developers at a time most fledgling developers only dream of future pacts." FORMA's ability to secure financial backers has reportedly had a lot to do with its founders—genomics experts at the Broad Institute of MIT and Harvard, Todd Golub, Stuart Schreiber and Michael Foley.

Using the new tools and technology being generated in chemistry biology research, FORMA reportedly placed itself in a position to develop new compounds to target the specific genomes that play a role in disease.

Mizra Cifric, FORMA's director of corporate development, tells ddn, "Emerald is one of—if not the world's—leading structural biology CRO. Most importantly, by utilizing the information gained from high throughput structural biology, we hope to rapidly inform and drive our discovery efforts against high-value targets."

Jeffrey Bouley

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