3DBS: Structure of Pi3k Gamma in Complex With Gdc0941

Phosphatidylinositol-3-kinase (PI3K) is an important target in cancer due to the deregulation of the PI3K/ Akt signaling pathway in a wide variety of tumors. A series of thieno[3,2-d]pyrimidine derivatives were prepared and evaluated as inhibitors of PI3 kinase p110alpha. The synthesis, biological activity, and further profiling of these compounds are described. This work resulted in the discovery of 17, GDC-0941, which is a potent, selective, orally bioavailable inhibitor of PI3K and is currently being evaluated in human clinical trials for the treatment of cancer.
PDB ID: 3DBSDownload
MMDB ID: 65020
PDB Deposition Date: 2008/6/2
Updated in MMDB: 2012/10
Experimental Method:
x-ray diffraction
Resolution: 2.8  Å
Source Organism:
Similar Structures:
Biological Unit for 3DBS: monomeric; determined by author and by software (PISA)
Molecular Components in 3DBS
Label Count Molecule
Protein (1 molecule)
Phosphatidylinositol-4,5-bisphosphate 3-kinase Catalytic Subunit Gamma Isoform(Gene symbol: PIK3CG)
Molecule annotation
Chemical (1 molecule)
* Click molecule labels to explore molecular sequence information.

Citing MMDB