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2.7.1.153: phosphatidylinositol-4,5-bisphosphate 3-kinase

This is an abbreviated version!
For detailed information about phosphatidylinositol-4,5-bisphosphate 3-kinase, go to the full flat file.

Word Map on EC 2.7.1.153

Reaction

ATP
+
1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
=
ADP
 +
1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate

Synonyms

class I phosphoinositide 3-kinase, class I PI3K, class IA phosphatidylinositol 3-kinase, class IA phosphatidylinositol-4,5-bisphosphate 3-kinase, CXCR2/phosphatidylinositol 3-kinase gamma, kinase (phosphorylating), phosphatidylinositol 4,5-diphosphate 3-, More, p101-PI3K, p110alpha, p110beta, p110delta, p110delta PI 3-kinase, p110gamma/p101, P120-PI3K, phosphatidyl-inositol-3-kinase, phosphatidylinositol (4,5)-bisphosphate 3-hydroxykinase, phosphatidylinositol 3'-kinase, phosphatidylinositol 3-hydroxyl kinase, phosphatidylinositol 3-kinase alpha, phosphatidylinositol 3-kinase gamma, phosphatidylinositol-4,5-bisphosphate 3-kinase, phosphoinositide 3-kinase, phosphoinositide 3-kinase p110delta, phosphoinositol 3-kinase, PI 3-K, PI 3-kinase, PI-3K, PI3-K, PI3-kinase, PI3K, PI3K p110delta, PI3Kalpha, PI3Kbeta, PI3Kdelta, PI3Kgamma, PI3Kp110delta, PIK3, PIK3CA, Pik3r1, PtdIns(4,5)P2 3-OH kinase, PtdIns-3-kinase p101, PtdIns-3-kinase p110, PtdInsP 3-OH-kinase, type I phosphoinositide 3-kinase

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.153 phosphatidylinositol-4,5-bisphosphate 3-kinase

Crystallization

Crystallization on EC 2.7.1.153 - phosphatidylinositol-4,5-bisphosphate 3-kinase

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CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
cocrystal strucutre of inhibitor 4-(2-((6-methoxypyridin-3-yl)amino)-5-((4-(methylsulfonyl)piperazin-1-yl)methyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine bound to catalytic subunit gamma isoform. Compound binds with two hydrogen bonds from the aminotriazine ring to the hinge, with the triazine methyl substituent oriented toward the Tyr867 side chain, and with the 4-methoxypyridine substituent projected into the affinity pocket. The methoxypyridine nitrogen atom makes a hydrogen bond to an ordered water molecule sitting between Tyr867 and Asp841, and the piperazine sulfonamide extended into the ribose pocket
docking of inhibitor TGX-221-R into a homology model of the PI3K-beta enzyme. The morpholine-oxygen accepts an H-bond from the hinge region Val854 while the pyrido-pyrimidinone template core interacts in the central pocket lined by Met926 and Ile residues 803, 851 and 936 from the N and C-terminal of the kinase domain
purified enzyme mutant, mixing of 25 nl 11 mg/ml protein with 0.9 mM inhibitor delalisib in 20 mM Tris, pH 7.2, 50 mM (NH4)2SO4, 1% v/v ethylene glycol, 1% w/v betaine, 300 mM CHAPS, and 5 mM TCEP, with 25 nl of reservoir solution containing 25% w/v PEG 3350, 0.1 M Bis-Tris, pH 6.5, microseeding in 480 nl of 2.5% w/v n-dodecyl-beta-D-maltoside, 300 nl of 20 mM ligand, and 0.12 ml of 12 mg/ml DELTAABD-p110delta in storage buffer 20 mM Tris, pH 7.2, 50 mM (NH4)2SO4, 1% v/v ethylene glycol, 1% w/v betaine, 300 nM CHAPS, and 5mM TCEP, X-ray diffraction structure determination and analysis at 2.4-2.5 A resolution
structure activity relationship study of inhibitor 2-(difluoromethyl)-1-[4,6-di-(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole, i.e. ZSTK474, with catalytic subunit gamma isoform, PDB entry 2CHX