1mzc
From Proteopedia
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==Overview== | ==Overview== | ||
| - | A series of novel diaryl ether lactams have been identified as very potent | + | 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== | ==About this Structure== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| - | [[Category: Beese, L | + | [[Category: Beese, L S.]] |
| - | [[Category: Buser, C | + | [[Category: Buser, C A.]] |
| - | [[Category: Ciccarone, T | + | [[Category: Ciccarone, T M.]] |
[[Category: Ellis-Hutchings, M.]] | [[Category: Ellis-Hutchings, M.]] | ||
[[Category: Fernandes, C.]] | [[Category: Fernandes, C.]] | ||
| - | [[Category: Graham, S | + | [[Category: Graham, S L.]] |
| - | [[Category: Hamilton, K | + | [[Category: Hamilton, K A.]] |
| - | [[Category: Huber, H | + | [[Category: Huber, H E.]] |
| - | [[Category: Kohl, N | + | [[Category: Kohl, N E.]] |
| - | [[Category: Lobell, R | + | [[Category: Lobell, R B.]] |
| - | [[Category: MacTough, S | + | [[Category: MacTough, S C.]] |
| - | [[Category: Robinson, R | + | [[Category: Robinson, R G.]] |
| - | [[Category: Shaw, A | + | [[Category: Shaw, A W.]] |
| - | [[Category: Taylor, J | + | [[Category: Taylor, J S.]] |
| - | [[Category: Tsou, N | + | [[Category: Tsou, N N.]] |
| - | [[Category: Walsh, E | + | [[Category: Walsh, E S.]] |
| - | [[Category: deSolms, S | + | [[Category: deSolms, S J.]] |
[[Category: BNE]] | [[Category: BNE]] | ||
[[Category: FPP]] | [[Category: FPP]] | ||
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[[Category: ras]] | [[Category: ras]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:00:38 2008'' |
Revision as of 12:00, 21 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 Thu Feb 21 14:00:38 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
