4EPV

Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-mediated Activation

Summary for 4EPV

Related4EPR 4EPT 4EPW 4EPX 4EPY
DescriptorGTPase KRas, GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ... (5 entities in total)
Functional Keywordssmall gtpase, signaling transduction, sos, raf, ral, pi3k, cytosol, binder, hydrolase, inhibitor of sos-mediated activation
Biological sourceHomo sapiens (human)
Cellular locationCell membrane; Lipid-anchor; Cytoplasmic side P01116
Total number of polymer chains1
Total molecular weight20028.54
Authors
Sun, Q.,Burke, J.P.,Phan, J.,Burns, M.C.,Olejniczak, E.T.,Waterson, A.G.,Lee, T.,Rossanese, O.W.,Fesik, S.W. (deposition date: 2012-04-17, release date: 2012-05-23, Last modification date: 2012-07-25)
Primary citation
Sun, Q.,Burke, J.P.,Phan, J.,Burns, M.C.,Olejniczak, E.T.,Waterson, A.G.,Lee, T.,Rossanese, O.W.,Fesik, S.W.
Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation.
Angew.Chem.Int.Ed.Engl., 51:6140-6143, 2012
PubMed: 22566140 (PDB entries with the same primary citation)
DOI: 10.1002/anie.201201358
MImport into Mendeley
Experimental method
X-RAY DIFFRACTION (1.35 Å)
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Structure validation

RfreeClashscoreRamachandran outliersSidechain outliersRSRZ outliers0.193100.7%2.4%MetricValuePercentile RanksWorseBetterPercentile relative to all X-ray structuresPercentile relative to X-ray structures of similar resolution