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Discovery of ASTX029, a clinical candidate which modulates the phosphorylation and catalytic activity of ERK1/2

X-ray diffraction
1.943Å resolution
PDB entry 7nqq coloured by chain, front view.
PDB entry 7nqq coloured by chain, side view.
PDB entry 7nqq coloured by chain, top view.
Source organism: Homo sapiens
Assembly composition:
monomeric (preferred)
Entry contents: 1 distinct polypeptide molecule

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Assemblies

Assembly 1 (preferred)
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Assembly Name: Mitogen-activated protein kinase 1
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Multimeric state: monomeric
PDBe Complex ID: PDB-CPX-151230

Macromolecules

Mitogen-activated protein kinase 1
Chain: A
Length: 368 amino acids
Theoretical weight: 42.55 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P28482 (Residues: 1-360; Coverage: 100%)
Gene names: ERK2, MAPK1, PRKM1, PRKM2
Pfam: Protein kinase domain
InterPro:
Mitogen-activated protein kinase 1 in PDB entry 7nqq, assembly 1, front view.
Mitogen-activated protein kinase 1 in PDB entry 7nqq, assembly 1, side view.
Mitogen-activated protein kinase 1 in PDB entry 7nqq, assembly 1, top view.
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