DiscoveRx Introduces a High-Throughput Biochemical Screening Platform for Bromodomain Epigenetic "Reader" Proteins

Release date: 5/16/2012

California, USA - May 16, 2012 - DiscoveRx Corporation today announced the launch of BROMOscanSM, a new service platform for identification and optimization of inhibitors targeting bromodomain epigenetic “reader” proteins.  Developed in a scientific collaboration with the laboratory of James Bradner, MD, at Dana-Farber Cancer Institute in Boston, the new platform is based on the proven KINOMEscan® technology and will drive lead discovery and optimization programs by enabling researchers to rapidly and quantitatively characterize potential inhibitors across a diversity of bromodomains. BROMOscan can be applied to high throughput screening, selectivity profiling and quantitative affinity (Kd) determinations across several bromodomain families, including the BET family.

Bromodomains are epigenetic reader proteins that recognize acetylated lysine residues on histone tails, which are important epigenetic marks associated with the regulation of gene expression.  With many drug discovery programs aimed at identifying small molecule bromodomain inhibitors, the availability of a quantitative and high-throughput platform represents a substantial leap forward and a powerful solution to initiate new discovery programs while supporting and expediting existing projects.

“Our research previously developed a first, direct-acting bromodomain inhibitor, targeting the BET family bromodomains,” says Bradner.  “Extending this research to new, compelling bromodomain targets has been limited by the availability of a quantitative, comparative biochemical screening platform.  We therefore collaborated with DiscoveRx to apply their leading KINOMEscan technology to epigenetic reader proteins.”

The initial panel launched today includes assays for 12 of the ~56 known human bromodomains, contains all 8 BET family domains and is expected to double in size by the end of 2012. This milestone achievement reaffirms DiscoveRx’s commitment to the drug discovery community by providing innovative screening and profiling solutions for key drug targets, including GPCRs, Kinases, NHRs and now epigenetic regulators.

About DiscoveRx Corporation
Founded in 2000, DiscoveRx is a privately held, venture-backed company headquartered in Fremont, California, with additional offices in San Diego, California and Birmingham, England. The Company pioneered the use of β-galactosidase enzyme fragment complementation (EFC) in HitHunter® biochemical and PathHunter® cell based assays for discovery research. In addition to the EFC platform, DiscoveRx also holds extensive intellectual property for its second core technology, an in vitro binding assay platform called KINOMEscan®. Utilizing these two proprietary platforms, DiscoveRx has developed and commercialized industry leading panels of GPCR, Kinase, and NHR assay solutions for drug discovery research.  Many of DiscoveRx’s innovative solutions have been widely adopted in pharmaceutical, academic and biotechnology laboratories worldwide. For more information, visit www.discoverx.com.

Media Contact
DiscoveRx Corporation
Sailaja Kuchibhatla
Sr. VP Business Development
42501 Albrae Street, Fremont, CA 94538
tel | 510.979.1415 x104
skuchibhatla@discoverx.com
www.discoverx.com