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TitleDestabilizers of the thymidylate synthase homodimer accelerate its proteasomal degradation and inhibit cancer growth.
Journal, issue, pagesElife, Vol. 11, Year 2022
Publish dateDec 16, 2013 (structure data deposition date)
AuthorsCostantino, L. / Ferrari, S. / Santucci, M. / Salo-Ahen, O.M.H. / Carosati, E. / Franchini, S. / Lauriola, A. / Pozzi, C. / Trande, M. / Gozzi, G. ...Costantino, L. / Ferrari, S. / Santucci, M. / Salo-Ahen, O.M.H. / Carosati, E. / Franchini, S. / Lauriola, A. / Pozzi, C. / Trande, M. / Gozzi, G. / Saxena, P. / Cannazza, G. / Losi, L. / Cardinale, D. / Venturelli, A. / Quotadamo, A. / Linciano, P. / Tagliazucchi, L. / Moschella, M.G. / Guerrini, R. / Pacifico, S. / Luciani, R. / Genovese, F. / Henrich, S. / Alboni, S. / Santarem, N. / da Silva Cordeiro, A. / Giovannetti, E. / Peters, G.J. / Pinton, P. / Rimessi, A. / Cruciani, G. / Stroud, R.M. / Wade, R.C. / Mangani, S. / Marverti, G. / D'Arca, D. / Ponterini, G. / Costi, M.P.
External linksElife / PubMed:36475542
MethodsX-ray diffraction
Resolution2.26 - 2.32 Å
Structure data

PDB-4o1u:
Crystal structure of human thymidylate synthase mutant Y202C
Method: X-RAY DIFFRACTION / Resolution: 2.26 Å

PDB-4o1x:
Crystal structure of human thymidylate synthase double mutant C195S-Y202C
Method: X-RAY DIFFRACTION / Resolution: 2.32 Å

Chemicals

ChemComp-SO4:
SULFATE ION

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-CL:
Unknown entry

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / Dimer-dimer interface modification / inactive conformation / Methyltransferase / Nucleotide biosynthesis / active conformation

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