WEE1, a nuclear kinase, belongs to WEE kinase family that negatively regulates the cell cycle via phosphorylation of CDK1. WEE1 serves as a dual-specificity kinase which selectively phosphorylates both Thr14 and Tyr15 residues of both CDK1 and CDK2 to restrain their activation and halt cell cycle progression in the response to DNA damage. Overexpression of WEE1 is commonly observed in malignant cells and its high expression has been associated with poor rates of survival in various cancer types. Inhibition of WEE1 facilitates or even expedites mitotic progression, leading to an increase in genomic instability. Therefore, WEE1 is considered a potential therapeutic target for cancer treatment.
Function
High throughput screening of compounds that inhibit WEE1 for drug discovery.
Reactivity
Human
Target
WEE1
Shipping
Dry Ice
Format
TR-FRET, time-resolved fluorescence resonance energy transfer