What is it about?
We tested more than a thousand chemical compounds in order to select one which controls a master switch, an enzyme in the human cell. Here we report the chemical structure of the enzyme and the way, it can be controlled.
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Why is it important?
The new chemical compound controls CLK2, a human cell's master switch, that is linked to various neuronal diseases, growth regulation and virus infection. It is a potential drug target for Alzheimer’s disease, Gaucher’s disease and a form of mental retardation, ataxia and atrophy of the brain. It regulates HIV virus production and influenza virus infection. A number of clinical trials in this area in diverse diseases such as diabetes, acute myeloid leukemia, HIV infection, and cystic fibrosis are ongoing.
Perspectives
The high-throughput data analysis was classical in this project. Biochemical screen with one luminescence value per well analyzed by the cellHTS2 package from R (Bioconductor). Calculating dose-response curves with R was an interesting additional component of the data analysis pipeline.
Dr Janos KristonVizi
University College London
Read the Original
This page is a summary of: Benzobisthiazoles Represent a Novel Scaffold for Kinase Inhibitors of CLK Family Members, Biochemistry, January 2016, American Chemical Society (ACS),
DOI: 10.1021/acs.biochem.5b01128.
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Contributors
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