1mzc: Difference between revisions
No edit summary |
No edit summary |
||
| Line 4: | Line 4: | ||
==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== | ||
| Line 13: | Line 13: | ||
[[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]] | ||
| Line 42: | Line 42: | ||
[[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
|
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 SUC, ZN, FPP and BNE 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
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.
- BNE
- FPP
- SUC
- ZN
- Alpha-alpha barrel
- Caax
- Fpp
- Ftase
- Inhibitor
- Pftase
- Ras
