DYRK1A Human

Dual-Specificity Tyrosine-(Y)-Phosphorylation Regulated Kinase 1A (DYRK1A) is an evolutionarily conserved protein kinase that plays a crucial role in various cellular processes. It is known for its dual specificity, meaning it can phosphorylate both serine/threonine and tyrosine residues. This kinase is encoded by the DYRK1A gene located on chromosome 21 in humans.

DYRK1A is a member of the DYRK family of protein kinases, which are characterized by their ability to autophosphorylate on tyrosine residues and phosphorylate exogenous substrates on serine/threonine residues. The protein consists of several domains, including a kinase domain, a PEST domain, and a nuclear localization signal. The kinase domain is responsible for its catalytic activity, while the PEST domain is involved in protein-protein interactions and regulation of protein stability.

DYRK1A is involved in a wide range of cellular processes, including:

• Cell Cycle Regulation: DYRK1A phosphorylates several key regulators of the cell cycle, thereby controlling cell proliferation and differentiation.
• Neuronal Development: It plays a significant role in brain development and function, influencing processes such as neurogenesis, synaptic plasticity, and cognitive functions.
• DNA Damage Response: DYRK1A is involved in the cellular response to DNA damage, helping to maintain genomic stability.
• Cancer: Abnormal expression or activity of DYRK1A has been linked to various cancers, making it a potential target for cancer therapy .

Recombinant DYRK1A refers to the protein that is produced through recombinant DNA technology. This involves inserting the DYRK1A gene into an expression vector, which is then introduced into a host cell (such as bacteria, yeast, or mammalian cells) to produce the protein. Recombinant DYRK1A is used in various research applications, including:

• Drug Discovery: It is used to screen for potential inhibitors that can modulate its activity, which is valuable in developing therapies for diseases such as cancer and neurodegenerative disorders.
• Structural Studies: Recombinant DYRK1A is used in crystallography and other structural biology techniques to understand its three-dimensional structure and the mechanisms underlying its function.
• Functional Assays: It is employed in biochemical assays to study its enzymatic activity, substrate specificity, and regulatory mechanisms.

Given its involvement in critical cellular processes and disease states, DYRK1A is considered a promising therapeutic target. Inhibitors of DYRK1A have shown potential in preclinical studies for the treatment of various cancers, particularly hematological malignancies and small cell lung cancer . Additionally, modulating DYRK1A activity may have therapeutic benefits in neurodegenerative diseases such as Alzheimer’s disease and Down syndrome, where DYRK1A is implicated in the pathophysiology.