Crystal structures of human CK2?2 in new crystal forms arising from a subtle difference in salt concentration.

ABSTRACT: The catalytic subunits of protein kinase CK2 are classified into two subtypes: CK2?1 and CK2?2. CK2?1 is an attractive drug-discovery target for various diseases such as cancers and nephritis. CK2?2 is defined as an off-target of CK2?1 and is a potential target in the development of male contraceptive drugs. High-resolution crystal structures of both isozymes are likely to provide crucial clues for the design of selective inhibitors of CK2?1 and/or CK2?2. To date, several crystal structures of CK2?1 have been solved at high resolutions of beyond 1.5?Å. However, crystal structures of CK2?2 have barely achieved a low resolution of around 3?Å because of the formation of needle-shaped crystals. In this study, new crystal forms were exploited and one provided a crystal structure of CK2?2 at 1.89?Å resolution. This result, together with the structure of CK2?1, will assist in the development of highly selective inhibitors for both isozymes.

SUBMITTER: Tsuyuguchi M 

PROVIDER: S-EPMC5931141 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature