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Crystal Structures of the Catalytic Domain of Human Protein Kinase Associated with Apoptosis and Tumor Suppression

Journal Article · · Nat. Struct. Mol. Biol.
OSTI ID:1006370

We have determined X-ray crystal structures with up to 1.5 {angstrom} resolution of the catalytic domain of death-associated protein kinase (DAPK), the first described member of a novel family of pro-apoptotic and tumor-suppressive serine/threonine kinases. The geometry of the active site was studied in the apo form, in a complex with nonhydrolyzable AMPPnP and in a ternary complex consisting of kinase, AMPPnP and either Mg{sup 2+} or Mn{sup 2+}. The structures revealed a previously undescribed water-mediated stabilization of the interaction between the lysine that is conserved in protein kinases and the {beta}- and {gamma}-phosphates of ATP, as well as conformational changes at the active site upon ion binding. Comparison between these structures and nucleotide triphosphate complexes of several other kinases disclosed a number of unique features of the DAPK catalytic domain, among which is a highly ordered basic loop in the N-terminal domain that may participate in enzyme regulation.

Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
USDOE
OSTI ID:
1006370
Journal Information:
Nat. Struct. Mol. Biol., Journal Name: Nat. Struct. Mol. Biol. Journal Issue: 2001 Vol. 8
Country of Publication:
United States
Language:
ENGLISH

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