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0WR 2-[1-({2-[2-(dimethylamino)-1h-benzimidazol-1-yl]-9-methyl-6-(morpholin-4-yl)-9h-purin-8-yl}methyl)piperidin-4-yl]propan-2-ol
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Code : 4GB9   PDBj   RCSB PDB   PDBe
Header : transferase/transferase inhibitor
Title : Potent and Highly Selective Benzimidazole Inhibitors of PI3K-delta
Release Data : 2012-08-22
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: unp residues 144-1102
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Spodoptera frugiperda  (taxid:7108)
gene: PIK3CG
expression_system_common: Fall armyworm
expression_system_cell_line: Sf9
expression_system_vector_type: plasmid
Authors : Murray, J.M.
Keywords : kinase p110 gamma-isoform, kinase, lipid kinase, transferase-transferase inhibitor complex
Exp. method : X-RAY DIFFRACTION ( 2.4380 Å )
Citation :

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.

Murray, J.M.,Sweeney, Z.K.,Chan, B.K.  et al.
(2012)  J.Med.Chem.  55 : 7686 - 7695

PubMed: 22877085
DOI: 10.1021/jm300717c

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