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1mzc

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[[Image:1mzc.jpg|left|200px]]
[[Image:1mzc.jpg|left|200px]]
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{{Structure
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|PDB= 1mzc |SIZE=350|CAPTION= <scene name='initialview01'>1mzc</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_1mzc", creates the "Structure Box" on the page.
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|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>
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{{STRUCTURE_1mzc| PDB=1mzc | SCENE= }}
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|RELATEDENTRY=[[1ld7|1LD7]], [[1ld8|1LD8]], [[1jcq|1JCQ]]
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|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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'''Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a'''
'''Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a'''
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[[Category: Tsou, N N.]]
[[Category: Tsou, N N.]]
[[Category: Walsh, E S.]]
[[Category: Walsh, E S.]]
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[[Category: deSolms, S J.]]
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[[Category: DeSolms, S J.]]
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[[Category: alpha-alpha barrel]]
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[[Category: Alpha-alpha barrel]]
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[[Category: caax]]
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[[Category: Caax]]
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[[Category: fpp]]
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[[Category: Fpp]]
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[[Category: ftase]]
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[[Category: Ftase]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: pftase]]
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[[Category: Pftase]]
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[[Category: ra]]
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[[Category: Ra]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 01:53:39 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:23:11 2008''
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Revision as of 22:53, 2 May 2008

Image:1mzc.jpg

Template:STRUCTURE 1mzc

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 Sat May 3 01:53:39 2008

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