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TitleUnraveling the Prenylation-Cancer Paradox in Multiple Myeloma with Novel Geranylgeranyl Pyrophosphate Synthase (GGPPS) Inhibitors.
Journal, issue, pagesJ. Med. Chem., Vol. 61, Page 6904-6917, Year 2018
Publish dateJan 15, 2018 (structure data deposition date)
AuthorsLacbay, C.M. / Waller, D.D. / Park, J. / Gomez Palou, M. / Vincent, F. / Huang, X.F. / Ta, V. / Berghuis, A.M. / Sebag, M. / Tsantrizos, Y.S.
External linksJ. Med. Chem. / PubMed:30016091
MethodsX-ray diffraction
Resolution2.8 - 3.5 Å
Structure data

PDB-6c56:
Crystal structure of mutant human geranylgeranyl pyrophosphate synthase (Y246D) in its Apo form
Method: X-RAY DIFFRACTION / Resolution: 2.8 Å

PDB-6c57:
Crystal structure of mutant human geranylgeranyl pyrophosphate synthase (Y246D) in complex with bisphosphonate inhibitor FV0109
Method: X-RAY DIFFRACTION / Resolution: 3.5 Å

Chemicals

ChemComp-VT0:
{[(2-phenylthieno[2,3-d]pyrimidin-4-yl)amino]methylene}bis(phosphonic acid)

ChemComp-HOH:
WATER

ChemComp-FV9:
{[(2-{3-[(4-fluorobenzene-1-carbonyl)amino]phenyl}thieno[2,3-d]pyrimidin-4-yl)amino]methylene}bis(phosphonic acid)

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / ISOPRENOID PATHWAY / ISOPENTENYL TRANSFERASE / TRANSFERASE/TRANSFERASE INHIBITOR / TRANSFERASE INHIBITOR / TRANSFERASE-TRANSFERASE INHIBITOR complex

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