Novel Alzheimer's Target Discovered Using BioFocus DPI’s Flexselect Platform
Saffron Walden, UK and Leiden, NL; 9 October 2009 - BioFocus, a leading provider of gene-to-drug candidate discovery services, announces that its FLeXSelect® target discovery platform was used to discover the novel Alzheimer’s drug target recently described in the journal Science[1].
The paper describes how BioFocus’ FLeXSelect platform was used to identify drug targets that effect the production of beta-amyloid, a protein in the brains of Alzheimer’s patients that is believed to cause the disease. In the high-throughput functional genomics screen, over 1,900 unique genes encoding potential drug targets from the FLeXSelect collection were systematically screened in a cellular assay relevant to Alzheimer’s disease.
From this target discovery campaign, the orphan G-protein coupled receptor, GPR3, was identified as a particularly interesting drug target since it enhances beta-amyloid production and has been mapped to the part of the genome associated with an increased risk of Alzheimer’s disease and is expressed in the brains of Alzheimer’s patients. The validation studies described in Science further confirm this protein’s potential as a promising drug target. GPR3 is now the focus of a drug discovery program aimed at delivering a small molecule to treat Alzheimer’s disease.
“The Science publication highlights several strengths of BioFocus’ target discovery capabilities,” said Dr. David Fischer, Director of Biology, BioFocus. “First, we focus on screening drugable and secreted proteins, those proteins which are most likely to form the basis of successful small molecule or antibody therapeutics. Secondly, we perform our screens in human primary and other disease relevant cells, which gives an increased chance of translating an observed therapeutic effect into man. Furthermore, we follow these initial screens with a series of high-content, information-rich studies to build a comprehensive package of information around the targets, so that they can enter directly into a drug discovery campaign."
More about FLeXSelect
FLeXSelect is a collection containing more than 1900 unique full-length cDNAs corresponding to the human drugable and secreted genome (see table below). This target discovery platform is based on adenoviruses that can efficiently introduce human cDNA into a wide variety of human primary cells to over-express specific human genes. High-throughput assays are then used to select for those proteins that have an effect on the disease phenotype. After undergoing further validation studies, these targets form the basis for the development of small molecule drugs or biological therapeutics. The table below shows the contents of FLeXSelect human full-length cDNA library represented by gene class. Each gene is covered by up to four cDNAs.
About BioFocus
BioFocus aims to expand its partners’ drug pipelines by accelerating the gene-to-drug candidate discovery process. This is achieved through a comprehensive discovery platform, which includes target discovery in human primary cells, focused as well as diverse compound libraries, in vitro and cell-based screening, structural biology, medicinal chemistry, ADME/PK services, supported by unique chemogenomic and informatics tools, and compound library acquisition, storage and distribution services. As the service division of Galapagos, BioFocus has over 250 employees in four countries worldwide.
The paper describes how BioFocus’ FLeXSelect platform was used to identify drug targets that effect the production of beta-amyloid, a protein in the brains of Alzheimer’s patients that is believed to cause the disease. In the high-throughput functional genomics screen, over 1,900 unique genes encoding potential drug targets from the FLeXSelect collection were systematically screened in a cellular assay relevant to Alzheimer’s disease.
From this target discovery campaign, the orphan G-protein coupled receptor, GPR3, was identified as a particularly interesting drug target since it enhances beta-amyloid production and has been mapped to the part of the genome associated with an increased risk of Alzheimer’s disease and is expressed in the brains of Alzheimer’s patients. The validation studies described in Science further confirm this protein’s potential as a promising drug target. GPR3 is now the focus of a drug discovery program aimed at delivering a small molecule to treat Alzheimer’s disease.
“The Science publication highlights several strengths of BioFocus’ target discovery capabilities,” said Dr. David Fischer, Director of Biology, BioFocus. “First, we focus on screening drugable and secreted proteins, those proteins which are most likely to form the basis of successful small molecule or antibody therapeutics. Secondly, we perform our screens in human primary and other disease relevant cells, which gives an increased chance of translating an observed therapeutic effect into man. Furthermore, we follow these initial screens with a series of high-content, information-rich studies to build a comprehensive package of information around the targets, so that they can enter directly into a drug discovery campaign."
More about FLeXSelect
FLeXSelect is a collection containing more than 1900 unique full-length cDNAs corresponding to the human drugable and secreted genome (see table below). This target discovery platform is based on adenoviruses that can efficiently introduce human cDNA into a wide variety of human primary cells to over-express specific human genes. High-throughput assays are then used to select for those proteins that have an effect on the disease phenotype. After undergoing further validation studies, these targets form the basis for the development of small molecule drugs or biological therapeutics. The table below shows the contents of FLeXSelect human full-length cDNA library represented by gene class. Each gene is covered by up to four cDNAs.
About BioFocus
BioFocus aims to expand its partners’ drug pipelines by accelerating the gene-to-drug candidate discovery process. This is achieved through a comprehensive discovery platform, which includes target discovery in human primary cells, focused as well as diverse compound libraries, in vitro and cell-based screening, structural biology, medicinal chemistry, ADME/PK services, supported by unique chemogenomic and informatics tools, and compound library acquisition, storage and distribution services. As the service division of Galapagos, BioFocus has over 250 employees in four countries worldwide.