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

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.

SUBMITTER: Tsuyuguchi M

PROVIDER: S-EPMC6613443 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature

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

Tsuyuguchi Masato M Nakaniwa Tetsuko T Sawa Masaaki M Nakanishi Isao I Kinoshita Takayoshi T

Acta crystallographica. Section F, Structural biology communications 20190704 Pt 7

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 ...[more]

PMID: 31282872

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