학술논문
A promiscuous kinase inhibitor delineates the conspicuous structural features of protein kinase CK2a1.
Document Type
Article
Source
Subject
*PROTEIN kinases
*CYTOSKELETAL proteins
*SERINE/THREONINE kinases
*PROTEIN kinase CK2
*KINASE inhibitors
*CRYSTAL structure
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Language
ISSN
2053-230X
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. [ABSTRACT FROM AUTHOR]