Brand  (β version)

PDB ID: 4FHK

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Ligands
Code Name Style Show Link
0U0 3-[2-methyl-6-(pyrazin-2-ylamino)pyrimidin-4-yl]-N-(1h-pyrazol-3-yl)imidazo[1,2-B]pyridazin-2-amine PoSSuM
SO4 Sulfate ion PoSSuM
Non-standard Residues
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Structure summary

Code : 4FHK   PDBj   RCSB PDB   PDBe
Header : Transferase/Transferase Inhibitor
Title : Crystal Structure of PI3K-gamma in Complex with Imidazopyridazine 19e
Release Data : 2013-04-10
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_vector_type: Baculovirus
Authors : Shaffer, P.L., Tang, J., Yakowec, P.
Keywords : p110, kinase, ATP-binding, p84, p101, Transferase-Transferase Inhibitor complex
Exp. method : X-RAY DIFFRACTION ( 3.00 Å )
Citation :

Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.

Peterson, E.A.,Boezio, A.A.,Andrews, P.S.  et al.
(2012)  Bioorg.Med.Chem.Lett.  22 : 4967 - 4974

PubMed: 22765895
DOI: 10.1016/j.bmcl.2012.06.033

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