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TitleA twist in the tale: shifting from covalent targeting of a tyrosine in JAK3 to a lysine in MK2.
Journal, issue, pagesRsc Med Chem, Vol. 16, Page 4906-4919, Year 2025
Publish dateMay 8, 2025 (structure data deposition date)
AuthorsHillebrand, L. / Wang, G. / Rasch, A. / Masberg, B. / Chaikuad, A. / Kronenberger, T. / Gunther, E. / Forster, M. / Poso, A. / Lammerhofer, M. ...Hillebrand, L. / Wang, G. / Rasch, A. / Masberg, B. / Chaikuad, A. / Kronenberger, T. / Gunther, E. / Forster, M. / Poso, A. / Lammerhofer, M. / Laufer, S.A. / Knapp, S. / Gehringer, M.
External linksRsc Med Chem / PubMed:40756524
MethodsX-ray diffraction
Resolution1.8 - 3 Å
Structure data

PDB-9r59:
Crystal structure of MAPKAPK2 with a covalent compound GCL334 targeting lysine
Method: X-RAY DIFFRACTION / Resolution: 3 Å

PDB-9r5z:
Crystal structure of JAK3 with GCL258
Method: X-RAY DIFFRACTION / Resolution: 1.8 Å

Chemicals

PDB-1jh4:
Solution structure of the C-terminal PABC domain of human poly(A)-binding protein in complex with the peptide from Paip1

ChemComp-HOH:
WATER

PDB-1jju:
Structure of a Quinohemoprotein Amine Dehydrogenase with a Unique Redox Cofactor and Highly Unusual Crosslinking

ChemComp-PHU:
1-phenylurea

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / kinase / covalent inhibitor / lysine / MAPKAPK2

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