Biological effects and mechanism of action of farnesyl transferase inhibitors

Chemical Research in Toxicology

Volumn 13, Issue 10, 2000, Pages 949-952

  Ashar, H R ^a   Armstrong, L ^a   James, L J ^a   Carr, D M ^a   Gray, K ^a   Taveras, A ^a   Doll, R J ^a   Bishop, W R ^a   Kirschmeier, P T ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [[2 [[2 [(2 AMINO 3 MERCAPTOPROPYL)AMINO] 3 METHYLPENTYL]OXY] 1 OXO 3 PHENYLPROPYL]AMINO] 4 (METHYLSULFONYL)BUTANOIC ACID ISOPROPYL ESTER; FARNESYL TRANS TRANSFERASE; LONAFARNIB; PROTEIN FARNESYLTRANSFERASE INHIBITOR;

ANTINEOPLASTIC ACTIVITY; APOPTOSIS; CELL CYCLE; CELL TRANSFORMATION; CONFERENCE PAPER; DRUG EFFECT; ENZYME INHIBITION; GENE MUTATION; PRENYLATION; PROTEIN PROCESSING; SIGNAL TRANSDUCTION;

ALKYL AND ARYL TRANSFERASES; ANIMALS; ANTINEOPLASTIC AGENTS; CELL CYCLE; ENZYME INHIBITORS; HUMANS; TUMOR SUPPRESSOR PROTEIN P53;

EID: 0033791628     PISSN: 0893228X     EISSN: None     Source Type: Journal    
DOI: 10.1021/tx000138v     Document Type: Conference Paper

References (18)

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3. A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis
4. Ras oncogenes in human cancer: A review
5. Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956
6. A peptidomimetic inhibitor of farnesyl: Protein transferase blocks the anchorage-dependent and -independent growth of human tumor cell lines
7. Polylysine and CVIM sequences of K-RasB dictate specificity of prenylation and confer resistance to benzodiazepine peptidomimetic in vitro
8. K-and N-Ras are geranylgeranylated in cells treated with farnesyl protein transferase inhibitors
9. A farnesyl-protein transferase inhibitor induces p21 expression and G1 block in p53 wild type tumor cells
10. FTIs block the farnesylation of CENP-E and CENP-F, and alter the association of CENP-E with the microtubules
11. CENP-E is a plus end-directed kinetochore motor required for metaphase chormosome alignment
12. CENP-F is a protein of the nuclear matrix that assembles onto kinetochores at late G2 and is rapidly degraded after mitosis
13. The microtubule-dependent motor centromere-associated protein E (CENP-E) is an integral component of kinetochore corona fibers that link centromeres to spindle microtubules
14. Cell division gatekeepers identified
15. The checkpoint delaying anaphase in response to chromosome monoorientation is mediated by an inhibitory signal produced by unattached kinetochores
16. Farnesyltransferase inhibitors: Antineoplastic mechanism and clinical prospects