Dual-specificity tyrosine phosphorylation-regulated kinases (DYRK1A, 1B, 2-4) and cdc2-like kinases (CLK1-4) belong to the CMGC group of serine/threonine kinases. These protein kinases are involved in multiple cellular functions, including intracellular signalling, mRNA splicing, chromatin transcription, DNA damage repair, cell survival, cell cycle control, differentiation, homocysteine/methionine/folate regulation, body temperature regulation, endocytosis, neuronal development, synaptic plasticity, etc.
Phosphorylation by protein kinases is the most universally used mechanism by cells to control their structural proteins and enzymes. All major physiological phenomena are regulated by phosphorylation and many diseases are associated with abnormal phosphorylation.
One example of DYRK inhibitors is Leucettinibs, a class of DYRK/CLK kinase inhibitors inspired by the marine sponge natural product known as leucettamine B. Leucettinibs inhibit the phosphorylation of DYRK1A substrates in cells. Leucettinibs provide research tools and potential leads for further optimisation towards therapeutic drug candidates.
AdipoGen’s DYRK inhibitor product range is distributed in Australia and New Zealand by Sapphire Bioscience.
Phone: 02 9698 2022
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