Brand  (β version)

PDB ID: 4FJY

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Ligands
Code Name Style Show Link
FJY 4-[3,3-dimethyl-6-(morpholin-4-yl)-2,3-dihydro-1h-indol-1-yl]-7-fluoro-3-methyl-2-(pyridin-3-yl)quinoline PoSSuM
SO4 Sulfate ion PoSSuM
Non-standard Residues
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Glycosylation
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Structure summary

Code : 4FJY   PDBj   RCSB PDB   PDBe
Header : Transferase/Inhibitor
Title : Crystal structure of PI3K-gamma in complex with quinoline-indoline inhibitor 24f
Release Data : 2012-10-24
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 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_cell_line: Sf9
expression_system_vector_type: baculovirus
Authors : Whittington, D.A., Tang, J., Yakowec, P.
Keywords : inflammation, cancer, p110, C2 domain, leukocytes, kinase, p85, phosphotransferase, Transferase-Inhibitor complex
Exp. method : X-RAY DIFFRACTION ( 2.900 Å )
Citation :

Discovery and in Vivo Evaluation of Dual PI3K-beta/delta inhibitors

Gonzalez-Lopez de Turiso, F.,Shin, Y.,Brown, M.  et al.
(2012)  J.Med.Chem.  55 : 7667 - 7685

PubMed: 22876881
DOI: 10.1021/jm300679u

Reaction

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