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TitleDual-Mechanism ERK1/2 Inhibitors Exploit a Distinct Binding Mode to Block Phosphorylation and Nuclear Accumulation of ERK1/2.
Journal, issue, pagesMol. Cancer Ther., Vol. 19, Page 525-539, Year 2020
Publish dateMay 15, 2019 (structure data deposition date)
AuthorsKidger, A.M. / Munck, J.M. / Saini, H.K. / Balmanno, K. / Minihane, E. / Courtin, A. / Graham, B. / O'Reilly, M. / Odle, R. / Cook, S.J.
External linksMol. Cancer Ther. / PubMed:31748345
MethodsX-ray diffraction
Resolution1.96 Å
Structure data

PDB-6rq4:
Inhibitor of ERK2
Method: X-RAY DIFFRACTION / Resolution: 1.96 Å

Chemicals

ChemComp-SO4:
SULFATE ION

ChemComp-KE8:
6,6-dimethyl-2-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-5-(2-morpholin-4-ylethyl)thieno[2,3-c]pyrrol-4-one

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsSIGNALING PROTEIN / protein kinase ATP-binding site serine/threonine kinase

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