2. Academic Validation
  3. A promiscuous kinase inhibitor delineates the conspicuous structural features of protein kinase CK2a1

A promiscuous kinase inhibitor delineates the conspicuous structural features of protein kinase CK2a1

  • Acta Crystallogr F Struct Biol Commun. 2019 Jul 1;75(Pt 7):515-519. doi: 10.1107/S2053230X19008951.
Masato Tsuyuguchi 1,  Tetsuko Nakaniwa 2,  Masaaki Sawa 3,  Isao Nakanishi 4,  Takayoshi Kinoshita 1
Affiliations

Affiliations

  • 1 Graduate School of Science, Osaka Prefecture University, 1-1 Gakuen-cho, Naka-ku, Sakai, Osaka 599-8531, Japan.
  • 2 Institute for Protein Research, Osaka University, Suita, Osaka 565-0871, Japan.
  • 3 Carna BioSciences, Kobe, Hyogo 650-0047, Japan.
  • 4 Department of Pharmaceutical Sciences, Kindai University, 3-4-1 Kowakae, Higashi-osaka, Osaka 577-8502, Japan.
PMID: 31282872 DOI: 10.1107/S2053230X19008951
Abstract

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.

Keywords

ATP-analogue inhibitor; off-target kinases; protein kinase CK2; selectivity; structural comparison.

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