Farnesyl transferase inhibitors cause enhanced mitotic sensitivity to taxol and epothilones
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چکیده
منابع مشابه
Farnesyl transferase inhibitors cause enhanced mitotic sensitivity to taxol and epothilones.
An important class of cellular proteins, which includes members of the p21ras family, undergoes posttranslational farnesylation, a modification required for their partition to membranes. Specific farnesyl transferase inhibitors (FTIs) have been developed that selectively inhibit the processing of these proteins. FTIs have been shown to be potent inhibitors of tumor cell growth in cell culture a...
متن کاملLipid posttranslational modifications. Farnesyl transferase inhibitors.
Some proteins undergo posttranslational modification by the addition of an isoprenyl lipid (farnesyl- or geranylgeranyl-isoprenoid) to a cysteine residue proximal to the C terminus. Protein isoprenylation promotes membrane association and contributes to protein-protein interactions. Farnesylated proteins include small GTPases, tyrosine phosphatases, nuclear lamina, cochaperones, and centromere-...
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Three mammalian nuclear lamin proteins, lamin B(1), lamin B(2) and the lamin A precursor, prelamin A, undergo canonical farnesylation and processing at CAAX motifs. In the case of prelamin A, there is an additional farnesylation-dependent endoproteolysis, which is defective in two congenital diseases: Hutchinson-Gilford progeria (HGPS) and restrictive dermopathy (RD). These two diseases arise r...
متن کاملWorking together: Farnesyl transferase inhibitors and statins block protein prenylation.
Farnesyl transferase inhibitors (FTIs) have so far proved to have limited value as single agents in clinical trials. This PharmSight will focus on the use of a novel group of FTIs that are most effective in vitro when used in combination with the "statin" class of anti-hypercholesterolemic agents, which also block protein prenylation. We recently showed that these novel FTIs in combination with...
متن کاملFarnesyl transferase inhibitors--a novel therapy for breast cancer.
Inhibitors of the enzyme farnesyl protein transferase prevent a key step in the post-translational processing of the Ras protein, and were developed initially as a therapeutic strategy to inhibit cell signalling in ras-transformed cells. As more has been learnt about the biological effects of farnesyl transferase inhibitors (FTIs) on cancer cells, it is clear that tumours without oncogenic ras ...
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ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 1998
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.95.4.1369