4FUL: Pi3 Kinase Gamma Bound To A Pyrmidine Inhibitor

Citation:
Abstract
hSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment. From our screening efforts, we have identified pyrimidine derivatives as hSMG-1 kinase inhibitors. We report structure-based optimization of this pan-kinase scaffold to improve its biochemical profile and overall kinome selectivity, including mTOR and CDK, to generate the first reported selective hSMG-1 tool compound.
PDB ID: 4FULDownload
MMDB ID: 104086
PDB Deposition Date: 2012/6/28
Updated in MMDB: 2012/11
Experimental Method:
x-ray diffraction
Resolution: 2.47  Å
Source Organism:
Similar Structures:
Biological Unit for 4FUL: monomeric; determined by author and by software (PISA)
Molecular Components in 4FUL
Label Count Molecule
Protein (1 molecule)
1
Phosphatidylinositol 4,5-bisphosphate 3-kinase Catalytic Subunit Gamma Isoform(Gene symbol: PIK3CG)
Molecule annotation
Chemical (1 molecule)
1
1
* Click molecule labels to explore molecular sequence information.

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