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Dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) are conserved serine/threonine kinases. DYRKs have been implicated in cell survival, proliferation and differentiation, and in the pathology of Down Syndrome and Alzheimer's disease.
|Cat No||Product Name / Activity|
|Potent DYRK1B inhibitor|
|5632||AZ Dyrk1B 33|
|Potent and selective Dyrk1B kinase inhibitor|
|Potent and selective DYRK1A inhibitor|
|5700||ML 315 hydrochloride|
|Inhibitor of Clk and DYRK kinases|
|DYRK1A/B inhibitor; prodrug of INDY (Cat. No. 4997)|
|Potent and selective DYRK1A/B inhibitor|
|Potent DYRK1A/B inhibitor; also inhibitor of Clk-family kinases|
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.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
|Gene||Species||Gene Symbol||Gene Accession No.||Protein Accession No.|