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TitleSynthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors
Journal, issue, pagesBioorg. Med. Chem. Lett., Vol. 19, Page 1753-1757, Year 2009
Publish dateFeb 22, 2008 (structure data deposition date)
AuthorsAsoh, K. / Kohchi, M. / Hyoudoh, I. / Ohtsuka, T. / Masubuchi, M. / Kawasaki, K. / Ebiike, H. / Shiratori, Y. / Fukami, T.A. / Kondoh, O. ...Asoh, K. / Kohchi, M. / Hyoudoh, I. / Ohtsuka, T. / Masubuchi, M. / Kawasaki, K. / Ebiike, H. / Shiratori, Y. / Fukami, T.A. / Kondoh, O. / Tsukaguchi, T. / Ishii, N. / Aoki, Y. / Shimma, N. / Sakaitani, M.
External linksBioorg. Med. Chem. Lett. / PubMed:19217288
MethodsX-ray diffraction
Resolution2.4 - 2.6 Å
Structure data

PDB-2zir:
Crystal Structure of rat protein farnesyltransferase complexed with a benzofuran inhibitor and FPP
Method: X-RAY DIFFRACTION / Resolution: 2.4 Å

PDB-2zis:
Crystal Structure of rat protein farnesyltransferase complexed with a bezoruran inhibitor and FPP
Method: X-RAY DIFFRACTION / Resolution: 2.6 Å

Chemicals

ChemComp-GOL:
GLYCEROL

ChemComp-ZN:
Unknown entry

ChemComp-FPP:
FARNESYL DIPHOSPHATE

ChemComp-NH7:
2-[(S)-(4-chlorophenyl)(hydroxy)(1-methyl-1H-imidazol-5-yl)methyl]-N-morpholin-4-yl-7-phenyl-1-benzofuran-5-carboxamide

ChemComp-HOH:
WATER

ChemComp-ACY:
ACETIC ACID

ChemComp-NH8:
3-{2-[(S)-(4-cyanophenyl)(hydroxy)(1-methyl-1H-imidazol-5-yl)methyl]-5-nitro-1-benzofuran-7-yl}benzonitrile

Source
  • rattus norvegicus (Norway rat)
KeywordsTRANSFERASE / Prenyltransferase / Metal-binding / Phosphoprotein

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