casein-kinase-ii and 5-iodotubercidin

Protein kinase CK2a1 is a serine/threonine kinase that plays a crucial role in the growth, proliferation and survival of cells and is a well known target for tumour and glomerulonephritis therapies. Here, the crystal structure of the kinase domain of CK2a1 complexed with 5-iodotubercidin (5IOD), an ATP-mimetic inhibitor, was determined at 1.78 Å resolution. The structure shows distinct structural features and, in combination with a comparison of the crystal structures of five off-target kinases complexed with 5IOD, provides valuable information for the development of highly selective inhibitors.

Topics: Amino Acid Sequence; Casein Kinase II; Crystallography, X-Ray; Humans; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein Structure, Secondary; Static Electricity; Tubercidin