1mzc | pdb_00001mzc
Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a
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Overview
A series of novel diaryl ether lactams have been identified as very potent, dual inhibitors of protein farnesyltransferase (FTase) and protein, geranylgeranyltransferase I (GGTase-I), enzymes involved in the, prenylation of Ras. The structure of the complex formed between one of, these compounds and FTase has been determined by X-ray crystallography., These compounds are the first reported to inhibit the prenylation of the, important oncogene Ki-Ras4B in vivo. Unfortunately, doses sufficient to, achieve this endpoint were rapidly lethal.
About this Structure
1MZC is a Protein complex structure of sequences from Homo sapiens with SUC, ZN, FPP and BNE as ligands. Full crystallographic information is available from OCA.
Reference
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents., deSolms SJ, Ciccarone TM, MacTough SC, Shaw AW, Buser CA, Ellis-Hutchings M, Fernandes C, Hamilton KA, Huber HE, Kohl NE, Lobell RB, Robinson RG, Tsou NN, Walsh ES, Graham SL, Beese LS, Taylor JS, J Med Chem. 2003 Jul 3;46(14):2973-84. PMID:12825937
Page seeded by OCA on Mon Nov 12 18:16:09 2007
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- Homo sapiens
- Protein complex
- Beese, L.S.
- Buser, C.A.
- Ciccarone, T.M.
- Ellis-Hutchings, M.
- Fernandes, C.
- Graham, S.L.
- Hamilton, K.A.
- Huber, H.E.
- Kohl, N.E.
- Lobell, R.B.
- MacTough, S.C.
- Robinson, R.G.
- Shaw, A.W.
- Taylor, J.S.
- Tsou, N.N.
- Walsh, E.S.
- DeSolms, S.J.
- BNE
- FPP
- SUC
- ZN
- Alpha-alpha barrel
- Caax
- Fpp
- Ftase
- Inhibitor
- Pftase
- Ras
