3dbs Summary


Structure of PI3K gamma in complex with GDC0941

The structure was published by Folkes, A.J., Ahmadi, K., Alderton, W.K., et al., Zhyvoloup, A., Zvelebil, M.J., and Shuttleworth, S.J., in 2008 in a paper entitled "The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer" (abstract).

This crystal structure was determined using X-ray diffraction at a resolution of 2.8 Å and deposited in 2008.

The experimental data on which the structure is based was also deposited.

The PDB entry contains the structure of Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform. This molecule has the UniProt identifier P48736 (PK3CG_HUMAN)search. The sample contained 960 residues which is < 90% of the natural sequence. Out of 960 residues 840 were observed and are deposited in the PDB.

It also contains one or more heterogenic compounds (e.g., ligands, co-factors, ions, modified amino acids, etc.); see here for a complete list.

The molecule is most likely monomeric.

The following tables show cross-reference information to other databases (to obtain a list of all PDB entries sharing the same property or classification, click on the magnifying glass icon):

Chain Name UniProt Name of source organism % of UniProt sequence present in the sample Residues in the sample molecules % of residues observed
A Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform P48736 (144-1102) (PK3CG_HUMAN)search Homo sapienssearch < 90% 960 87%

This entry contains 1 unique UniProt protein:

UniProt accession Name Organism PDB
P48736 (144 - 1102) Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens

Chain Structural classification (CATH) Sequence family (Pfam)
A Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, domain 1search, C2- domain Calcium/lipid binding domainsearch, Serine Threonine Protein Phosphatase 5, Tetratricopeptide repeatsearch, Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, domain 4search, Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, domain 5search Phosphatidylinositol 3- and 4-kinasesearch, Phosphoinositide 3-kinase family, accessory domain (PIK domain)search, Phosphoinositide 3-kinase C2search, PI3-kinase family, ras-binding domainsearch

Chain ID Biological process (GO) Molecular function (GO)
A (P48736) phosphatidylinositol phosphorylationsearch phosphatidylinositol-mediated signalingsearch phosphotransferase activity, alcohol group as acceptorsearch transferase activity, transferring phosphorus-containing groupssearch

Chain InterPro annotation
A C2 domainsearch Phosphatidylinositol 3-kinase Ras-binding (PI3K RBD) domainsearch Phosphatidylinositol 3-/4-kinase, catalytic domainsearch Phosphoinositide 3-kinase, accessory (PIK) domainsearch Phosphatidylinositol 3-kinase, C2 domainsearch Protein kinase-like domainsearch Phosphatidylinositol Kinasesearch Armadillo-type foldsearch Phosphatidylinositol 3/4-kinase, conserved sitesearch Ubiquitin-related domainsearch