1MZC: Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate And Inhibitor Compound 33a

Citation:
Abstract
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.
PDB ID: 1MZCDownload
MMDB ID: 23419
PDB Deposition Date: 2002/10/7
Updated in MMDB: 2007/10
Experimental Method:
x-ray diffraction
Resolution: 2  Å
Source Organism:
Similar Structures:
Biological Unit for 1MZC: dimeric; determined by author and by software (PISA)
Molecular Components in 1MZC
Label Count Molecule
Proteins (2 molecules)
1
Protein Farnesyltransferase Alpha Subunit(Gene symbol: FNTA)
Molecule annotation
1
Protein Farnesyltransferase Beta Subunit(Gene symbol: FNTB)
Molecule annotation
Chemicals (4 molecules)
1
1
2
1
3
1
4
1
* Click molecule labels to explore molecular sequence information.

Citing MMDB
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