Dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) are a family of serine/threonine kinases, consisting of DYRK1A, DYRK1B, DYRK2, DYRK3 and DYRK4. The DYRK family is closely related to the CMGC group of kinases (which contains CDKs, MAPKs, GSK and CLKs).
DYRKs are self-activated through auto phosphorylation of tyr-321 within the activation loop of their catalytic domain. Once activated, DYRKs phosphorylate serine and threonine residues on target proteins, which have been reported to include STAT3, Gli1, dynamin, glycogen synthase, CREB, tau and Hip-1. DYRKs can also act as priming kinases, whereby DYRK phosphorylation of a target protein enhances the efficiency of further phosphorylation by another kinase. For example DYRK1A can prime tau for further phosphorylation by GSK-1.
Physiologically DYRK1A, -1B and -3 have been implicated in cell survival, proliferation and differentiation, whereas DYRK2 is proapoptotic. The DYRK1A gene is localized to the Down Syndrome critical region of chromosome 21 and thus has been implicated in Down Syndrome pathology. Overexpression of DRYK1A in Down Syndrome neurons has been associated with the developmental defects and early onset of neurodegeneration and dementia seen in Down Syndrome. DYRK1A has also been implicated in the pathology of Alzheimer's, Parkinson's and Huntington's disease, whilst DYRK1B is over-expressed in solid tumors.View all products for DYRK »
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Literature for DYRK
A collection of over 400 products for kinase research, the listing includes inhibitors of:
- Receptor Tyrosine Kinases
- Protein Kinases A, C, D and G
- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
- Receptor Serine/Threonine Kinases
A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:
- Alzheimer's disease
- Parkinson's disease
- Huntington's disease
Written by Alan Palmer and updated in 2015, this poster summarizes structural and functional changes observed in the progression of Alzheimer's disease (AD), as well as classic AD drug targets. The hypotheses behind the neurobiology of AD are discussed alongside the different stages in disease progression. Compounds available from Tocris are listed.Request copy | Download PDF | View all posters
Written by Anthony H.V. Schapira, this poster summarizes the neurobiology of Parkinson's disease (PD), including new genetic insight, neurotransmitter pathways, and the role of aberrant α-synuclein metabolism in PD pathogenesis. This poster also presents new and emerging therapeutic strategies to delay the onset and progress of PD. Compounds available from Tocris are listed.Request copy | Download PDF | View all posters
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