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Ligands
Code Name Style Show Link
0KO 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
SO4 Sulfate ion
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Code : 4DK5   PDBj   RCSB PDB   PDBe
Header : Transferase/Inhibitor
Title : Crystal structure of human PI3K-gamma in complex with a pyridyl-triazine inhibitor
Release Data : 2012-05-16
Compound :
mol_id molecule chains synonym
1 Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform A PI3-kinase subunit gamma, PI3K-gamma, PI3Kgamma, PtdIns-3-kinase subunit gamma, Phosphatidylinositol-4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma, PtdIns-3-kinase subunit p110-gamma, p110gamma, Phosphoinositide-3-kinase catalytic gamma polypeptide, Serine/threonine protein kinase PIK3CG, p120-PI3K
ec: 2.7.1.153, 2.7.11.1
fragment: catalytic domain, UNP residues 114-1102
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Spodoptera frugiperda  (taxid:7108)
gene: PIK3CG
expression_system_cell_line: Sf9
expression_system_vector_type: baculovirus
Authors : Whittington, D.A., Tang, J., Yakowec, P.
Keywords : phosphotransferase, cancer, p85-alpha, p85-beta, Ras, Transferase-Inhibitor complex
Exp. method : X-RAY DIFFRACTION ( 2.950 Å )
Citation :

Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.

Smith, A.L.,D'Angelo, N.D.,Bo, Y.Y.  et al.
(2012)  J.Med.Chem.  55 : 5188 - 5219

PubMed: 22548365
DOI: 10.1021/jm300184s

Chain : A
UniProt : P48736 (PK3CG_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol) + ATP = a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol-3-phosphate) + ADP + H(+) 2.7.1.137 PubMed:11277933, PubMed:16123124
left-to-right PubMed:11277933
a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol-4,5- bisphosphate) + ATP = a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo- inositol-3,4,5-trisphosphate) + ADP + H(+) 2.7.1.153 PubMed:15135396, PubMed:16123124, PubMed:31554793
left-to-right PubMed:15135396
a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol 4- phosphate) + ATP = a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo- inositol-3,4-bisphosphate) + ADP + H(+) 2.7.1.154 PubMed:16123124
left-to-right
ATP + L-seryl-[protein] = ADP + H(+) + O-phospho-L-seryl- [protein] 2.7.11.1 PubMed:12502714, PubMed:16094730
left-to-right PubMed:12502714