PDBsum entry 3uyt

Transferase/transferase inhibitor

PDB id: 3uyt

Contents

Protein chains

287 a.a.

268 a.a.

Ligands

0CK ×4

SO4 ×7

Waters ×940

References listed in PDB file

Key reference

• Title: Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor.
• Authors: A.Long, H.Zhao, X.Huang.
• Ref.: J Med Chem, 2012, 55, 956-960.
• PubMed id: 22168824

Abstract

Casein kinase 1 delta (CK1δ) and its closest homologue CK1ε are key regulators of diverse cellular growth and survival processes such as Wnt signaling, DNA repair, and circadian rhythms. We report three crystal structures of the kinase domain of human CK1δ, one apo and two complexed with a potent and selective CK1δ/ε inhibitor PF670462 in two different crystal forms. These structures provide a molecular basis for the strong and specific inhibitor interactions and suggest clues for further development of CK1δ/ε inhibitors.