2red | pdb_00002red
Crystal structures of C2ALPHA-PI3 kinase PX-domain domain indicate conformational change associated with ligand binding.
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| 2red, resolution 2.10Å | |||||||||||||
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| Sites: | AC1, AC2, AC3, AC4, AC5 and AC6 | ||||||||||||
| Ligands: | GOL | ||||||||||||
| Gene: | PIK3C2A (Homo sapiens) | ||||||||||||
| Activity: | Phosphatidylinositol-4-phosphate 3-kinase, with EC number 2.7.1.154 | ||||||||||||
| Related: | 2ar5, 2rea
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
Overview
ABSTRACT: BACKGROUND: PX domains have specialized protein structures involved in binding of phosphoinositides (PIs). Through binding to the various PIs PX domains provide site-specific membrane signals to modulate the intracellular localisation and biological activity of effector proteins. Several crystal structures of these domains are now available from a variety of proteins. All PX domains contain a canonical core structure with main differences exhibited within the loop regions forming the phosphoinositide binding pockets. It is within these areas that the molecular basis for ligand specificity originates. RESULTS: We now report two new structures of PI3K-C2 PX domain that crystallised in a P3121 space group. The two structures, refined to 2.1 A and 2.5 A, exhibit significantly different conformations of the phosphoinositide-binding loops. Unexpectedly, in one of the structures, we have detected a putative-ligand trapped in the binding site during the process of protein purification and crystallisation. CONCLUSIONS: The two structures reported here provide a more complete description of the phosphoinositide binding region compared to the previously reported 2.6 A crystal structure of human PI3K-C2 PX where this region was highly disordered. The structures enabled us to further analyse PI specificity and to postulate that the observed conformational change could be related to ligand-binding.
About this Structure
2RED is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Crystal structures of PI3K-C2alpha PX domain indicate conformational change associated with ligand binding., Parkinson GN, Vines D, Driscoll PC, Djordjevic S, BMC Struct Biol. 2008 Feb 29;8(1):13. PMID:18312637
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