San Diego, May, 21st, 2012: CalAsia Pharmaceuticals today launched a new drug target implicated in Parkinson’s disease and other neurological disorders, FK506 binding protein-12 (FKBP12), ready to be used for structure based and conventional drug discovery.
FKBP12 produced by CalAsia is biologically active, greater than 95% pure and can be produced in tens of milligram quantity. In addition, this pure FKBP12 protein yields high resolution diffracting quality crystals suitable for crystallography based fragment screening and structure based drug discovery. FKBP12 belongs to the family of immunophilins enzymes, collectively known as the peptidylprolyl cis-trans isomerases (PPIases). As the name suggests, FKPB12 is a receptor for a class of immunosuppressive drugs such as FK506, rapamycin and cyclosporin A. FKBP12 levels are ten times higher in the brain compared to immune system. Studies have shown Lewy bodies, which are the pathological hallmark of Parkinson’s disease predominantly consists of fibrillar of the protein alpha-synuclein (alpha-SYN). FKBP12 is shown to cause the acceleration of the recombinant alpha-SYN in vitro, an effect that can be reversed by inhibiting its PPIase activity using brain penetrant small molecule inhibitors.
“We are excited to have produced biologically active, pure and crystallography grade FKBP12 and make it available to the research and drug discovery community in helping them find drugs to cure Parkinson’s disease and related neurological disorders”, said Dr. Jeffrey Stebbins, Head of Biology.
About CalAsia's Drug-discovery:
CalAsia Pharmaceuticals, Inc. is an employee owned early stage pharmaceutical company focused on the rapid discovery of drug-like small molecules by utilizing its core technologies. In detail, CalAsia core technologies combine functional fragment screening with X-ray crystallography co-crystallization to rationally design and synthesize New Chemical Entities (NCEs) with drug-like properties. By differential fragment screening of closely related isotypes, CalAsia also develops selective NCEs early in the drug discovery process thereby increasing the quality of potential drug candidates. Currently, CalAsia has 6 internal drug-discovery programs for the treatment unmet medical needs for Parkinson Disease, Type II Diabetes, Inflammation, Prostate Cancer and Malaria. Of note, CalAsia team has decades of drug-discovery experience and has been involved in numerous drug-discovery programs that have resulted in multiple clinical candidates as well as one marketed drug.
About CalAsia's Services:
The CalAsia team provides its expertise; which includes cloning, recombinant protein expression (E. coli, Baculovirus & Yeast), recombinant protein purification, biochemical assays, cellular assays, fragment screening, and X-ray crystallography co-crystallization; to the drug discovery community through contract research.