Work

The challenge of selecting protein kinase assays for lead discovery optimization

Year: 2008

Type: article

Abstract: BACKGROUND: Protein kinases represent one of the most promising groups of drug targets owing to their involvement in such pathological conditions as cancer, inflammatory diseases, neural disorders, and metabolism problems. In the last few years, numerous pharmaceutical and biotech companies have established kinase high-throughput screening (HTS) programs, and the reagent and service industries for kinase assay platforms, kits, and profiling services have begun to thrive. OBJECTIVE: The plethora of different assay formats available today poses a great challenge to scientists who want to select a technology that will be cost efficient, convenient to use, and have low false positive and false negative rates. METHODS: In the current review, we summarize the most commonly used kinase assay methods in the drug discovery process, present the advantages and disadvantages of each of these methods, and discuss the challenges of discovering kinase inhibitors by using these technologies. CONCLUSIONS: The decision of selecting the assay formats for HTS or service platform for profiling should take into account not only the final goals of the screens but also the limitation of resources.

Source: Expert Opinion on Drug Discovery

DOI: 10.1517/17460441.3.6.607

Authors: Haiching Ma, Sean Deacon, Kurumi Horiuchi

Institution: Reaction Biology Corporation (United States)

Language: English

Topic: Computational Drug Discovery Methods

Subfield: Drug Discovery

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

Open Access status: green

Funders: National Human Genome Research Institute, National Cancer Institute, National Institute of Dental and Craniofacial Research

Awards: Enzyme Assay Chips for Apoptosis Discovery, Microarraying and Screening Chemical Libraries, Kinome Drug Bioassay Platform, Kinome Drug Bioassay Platform