GSG2 + K00508

GSG2 + K00508

GSG2 + K00508: Human haspin in complex with an Imidazo-pyridazine ligand
PDB Code: 3F2N
Description
Haspin (haploid germ cell–specific nuclear protein kinase) is a serine/threonine kinase that tightly associates with chromosomes during mitosis. Haspin-like proteins are identified in several major eukaryotic phyla including yeasts, plants, flies, fish, and mammals. Kinases of this family share only very low sequence homology with other protein kinases, contain several large insertions and lack a subset of residues that are almost invariant in known kinases. Phosphorylation of Haspin itself and its specific substrate histone H3 threonine-3 (H3T3ph) occurs during mitosis. Haspin has been shown to be vital for the maintenance of chromosome cohesion. Depletion of Haspin leads to a loss of cohesin association, premature chromatid separation, activation of the spindle assembly checkpoint, and a block in mitosis in a pro-metaphase-like state. Although no direct link to cancer has been established so far, Haspin has been suggested as a target for drug development as it has been shown to activate the well established oncology target Aurora 2.
Here we present the structure of the Haspin kinase domain refined at 1.8 Å resolution in complex with an imidazo[1.2-b]pyridazine inhibitor. We have also determined the structures of the Haspin kinase domain in complex with the ATP mimetic inhibitor 5-Iodotubercidin (4-Amino-5-iodo-7-(b-D-ribofuranosyl) pyrrolo[2,3-d]pyrimidine) (PDB ID 2VUW), with a pyrazolo[1.5a]pyrimidine inhibitor (PDB ID 3E7V) and with an isoquinoline inhibitor (PDB ID 3FMD). In order to get insight into ATP recognition we also determined the structure of Haspin in complex with ATP/Mg (PDB ID 3DLZ).

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