US 9,176,064 B2 · Bisubstrate fluorescent probes for protein kinase CK2

Abstract

This invention relates to fluorescent probes for screening and characterization of compounds binding to protein kinase CK2, measurement of concentration of the catalytically active form of CK2 and imaging of CK2 activity in cells and tissues. The CK2-selective probe of the present invention interacts with binding sites of both substrates of the catalytic subunit of CK2 and therefore can be used for characterization of all inhibitors binding to the active site of CK2 in the binding/displacement assay. The high affinity of the probe affords the detection of the enzyme at low concentration and characterization of inhibitors in a wide affinity range. The invention also relates to the application of the probes for mapping and monitoring of CK2 activity in cells, tissues and live organisms.

Claims16

Dependent claims

A bisubstrate fluorescent probe

which binds to protein kinase CK2 (casein kinase 2) with affinity KD=0.02-10 nm and wherein fragment X is 1H-benzimidazol or substituted 1H-benzimidazol, j is from 1 to 10, i is from 1 to 10, R1 and R2 are independently H or —(CH2)nCOOH, n is independently 0 to 3, at least one of R1 and R2 is —(CH2)nCOOH, and the α-carbon connected to R2 is independently in either R or S configuration, FL is a fluorescent label, and L is a linker formed of a hydrocarbon chain.

Dependencies are inferred from the claim text.

Bisubstrate fluorescent probes for protein kinase CK2

Life of this patent

Bisubstrate fluorescent probes for protein kinase CK2

Life of this patent

Abstract

Claims16