1mzc
From Proteopedia
(New page: 200px<br /> <applet load="1mzc" size="450" color="white" frame="true" align="right" spinBox="true" caption="1mzc, resolution 2.00Å" /> '''Co-Crystal Structur...) |
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| - | [[Image:1mzc. | + | [[Image:1mzc.jpg|left|200px]]<br /><applet load="1mzc" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1mzc, resolution 2.00Å" /> | caption="1mzc, resolution 2.00Å" /> | ||
'''Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a'''<br /> | '''Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1MZC is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SUC, ZN, FPP and BNE as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1MZC is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SUC:'>SUC</scene>, <scene name='pdbligand=ZN:'>ZN</scene>, <scene name='pdbligand=FPP:'>FPP</scene> and <scene name='pdbligand=BNE:'>BNE</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1MZC OCA]. |
==Reference== | ==Reference== | ||
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[[Category: ras]] | [[Category: ras]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:26:13 2008'' |
Revision as of 14:26, 15 February 2008
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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 with , , and 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 Fri Feb 15 16:26:13 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. | BNE | FPP | SUC | ZN | Alpha-alpha barrel | Caax | Fpp | Ftase | Inhibitor | Pftase | Ras
