Mechanism of CK2 Inhibition by a Ruthenium-Based Polyoxometalate.

Fabbian S, Giachin G, Bellanda M, Borgo C, Ruzzene M, Spuri G, Campofelice A, Veneziano L, Bonchio M, Carraro M, Battistutta R, Front Mol Biosci 9:906390 (2022) Europe PMC

SASDNG7 – CK2α (Casein kinase II subunit alpha) dimer bound to ruthenium-based polyoxometalate (Ru4POM)

Casein kinase II subunit alpha
MWexperimental 88 kDa
MWexpected 78 kDa
VPorod 122 nm3
log I(s) 1.15×102 1.15×101 1.15×100 1.15×10-1
Casein kinase II subunit alpha small angle scattering data  s, nm-1
ln I(s)
Casein kinase II subunit alpha Guinier plot ln 1.15×102 Rg: 3.0 nm 0 (3.0 nm)-2 s2
(sRg)2I(s)/I(0)
Casein kinase II subunit alpha Kratky plot 1.104 0 3 sRg
p(r)
Casein kinase II subunit alpha pair distance distribution function Rg: 3.1 nm 0 Dmax: 11.8 nm

Data validation


Fits and models


log I(s)
 s, nm-1
Casein kinase II subunit alpha CUSTOM IN-HOUSE model

Synchrotron SAXS data from solutions of CK2α (Casein kinase II subunit alpha) dimer bound to ruthenium-based polyoxometalate (Ru4POM) in 25 mM Tris, 500 mM NaCl, pH 8.5 were collected on the BM29 beam line at the ESRF storage ring (Grenoble, France) using a Pilatus3 2M detector at a sample-detector distance of 2.9 m and at a wavelength of λ = 0.099 nm (I(s) vs s, where s = 4πsinθ/λ, and 2θ is the scattering angle). In-line size-exclusion chromatography (SEC) SAS was employed. The SEC parameters were as follows: A 50.00 μl sample at 7.6 mg/ml was injected at a 0.30 ml/min flow rate onto a GE Superdex 200 Increase 5/150 column at 20°C. One 2 second frame was collected. The data were normalized to the intensity of the transmitted beam and radially averaged; the scattering of the solvent-blank was subtracted.

Probable catalytic subunit of a constitutively active serine/threonine-protein kinase complex that phosphorylates a large number of substrates containing acidic residues C-terminal to the phosphorylated serine or threonine. Amplification-dependent oncogene; promotes cell proliferation and tumorigenesis by down-regulating expression of the tumor suppressor protein, PML. May play a role in the pathogenesis of the lung cancer development and progression.

Casein kinase II subunit alpha (CK2α)
Mol. type   Protein
Organism   Homo sapiens
Olig. state   Dimer
Mon. MW   39.2 kDa
 
UniProt   P68400 (3-330)
Sequence   FASTA