What question did this study set out to answer?

To resolve the three-dimensional crystal structure of the inactive human SGK1 catalytic domain and identify structural features to inform selective drug design.

October 26, 2007Protein ScienceOpen Access

Crystal structure of the kinase domain of serum and glucocorticoid‐regulated kinase 1 in complex with AMP–PNP

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Authors

BZBaoguang ZhaoWoosuk University RLRuth LehrTexas Tech University ASAngela SmallwoodSouth College

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Implication

Crystallographic analysis reveals a unique active-site conformation in human SGK1 kinase domain complexed with AMP-PNP, highlighting opportunities for selective inhibitor design.

Key Points

To resolve the three-dimensional crystal structure of the inactive human SGK1 catalytic domain and identify structural features to inform selective drug design.
Determined the X-ray crystal structure of the human SGK1 catalytic domain bound to the non-hydrolyzable ATP analogue AMP-PNP at 1.9 Å resolution.
Demonstrated that SGK1 forms a homodimer stabilized by two intermolecular disulfide bonds between Cys258 in the activation loop and Cys193.
Identified that the canonical alphaC helix is absent and instead forms a beta-strand that pairs with the activation loop into an antiparallel beta-sheet near the ATP binding site.

Cite This Study

Zhao et al. (2007) studied this question.

synapsesocial.com/papers/6a898795176d2ac34cfba4fa https://doi.org/10.1110/ps.073161707

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Implication

Crystallographic analysis reveals a unique active-site conformation in human SGK1 kinase domain complexed with AMP-PNP, highlighting opportunities for selective inhibitor design.

Crystal structure of the kinase domain of serum and glucocorticoid‐regulated kinase 1 in complex with AMP–PNP

Discussion

Member takes

Implication

Key Points

Cite This Study

Crystal structure of the kinase domain of serum and glucocorticoid‐regulated kinase 1 in complex with AMP–PNP

Discussion

Member takes

Implication

Key Points

Cite This Study

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