1mzc | pdb_00001mzc
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| 1mzc, resolution 2.00Å | |||||||||||||
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| Ligands: | BNE, FPP, SUC, ZN | ||||||||||||
| Related: | 1LD7, 1LD8, 1JCQ
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a
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. 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 Sun Mar 30 22:23:11 2008
Proteopedia Page Contributors and Editors (what is this?)
- Pages with broken file links
- 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.
- Alpha-alpha barrel
- Caax
- Fpp
- Ftase
- Inhibitor
- Pftase
- Ra
