1mzc
From Proteopedia
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|PDB= 1mzc |SIZE=350|CAPTION= <scene name='initialview01'>1mzc</scene>, resolution 2.00Å | |PDB= 1mzc |SIZE=350|CAPTION= <scene name='initialview01'>1mzc</scene>, resolution 2.00Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= | + | |LIGAND= <scene name='pdbligand=BNE:2-[3-(3-ETHYL-1-METHYL-2-OXO-AZEPAN-3-YL)-PHENOXY]-4-[1-AMINO-1-(1-METHYL-1H-IMIDIZOL-5-YL)-ETHYL]-BENZONITRILE'>BNE</scene>, <scene name='pdbligand=FPP:FARNESYL+DIPHOSPHATE'>FPP</scene>, <scene name='pdbligand=SUC:SUCROSE'>SUC</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene> |
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1ld7|1LD7]], [[1ld8|1LD8]], [[1jcq|1JCQ]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1mzc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mzc OCA], [http://www.ebi.ac.uk/pdbsum/1mzc PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1mzc RCSB]</span> | ||
}} | }} | ||
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[[Category: Walsh, E S.]] | [[Category: Walsh, E S.]] | ||
[[Category: deSolms, S J.]] | [[Category: deSolms, S J.]] | ||
| - | [[Category: BNE]] | ||
| - | [[Category: FPP]] | ||
| - | [[Category: SUC]] | ||
| - | [[Category: ZN]] | ||
[[Category: alpha-alpha barrel]] | [[Category: alpha-alpha barrel]] | ||
[[Category: caax]] | [[Category: caax]] | ||
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[[Category: ra]] | [[Category: ra]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:23:11 2008'' |
Revision as of 19:23, 30 March 2008
| |||||||
| , resolution 2.00Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , , , | ||||||
| Related: | 1LD7, 1LD8, 1JCQ
| ||||||
| 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
Categories: 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
