R-115777: Oncolytic, farnesyl protein transferase inhibitor

Drugs of the Future

Volumn 26, Issue 5, 2001, Pages 453-461

  Sorbera, L A ^a   Fernandez R ^a   Castaner J ^a  

^a PROUS SCIENCE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

3 BENZYL 7 CYANO 2,3,4,5 TETRAHYDRO 1 (1H IMIDAZOL 4 YLMETHYL) 4 (2 THIENYLSULFONYL) 1H 1,4 BENZODIAZEPINE; ANTINEOPLASTIC AGENT; ARGLABIN; AZD 3409; CAPECITABINE; CISPLATIN; CP 609754; CYTOTOXIC AGENT; GEMCITABINE; L 778123; LONAFARNIB; PACLITAXEL; PROTEIN FARNESYLTRANSFERASE INHIBITOR; TIPIFARNIB; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTHRALGIA; ARTICLE; BLOOD TOXICITY; CELL STRAIN; CLINICAL TRIAL; DIGESTIVE SYSTEM CANCER; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENTIATION; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; FATIGUE; GASTROINTESTINAL SYMPTOM; HUMAN; HUMAN CELL; HYPOKALEMIA; ONCOGENE K RAS; SOLID TUMOR; STRUCTURE ANALYSIS;

EID: 0034921499     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.2001.026.05.621725     Document Type: Article

References (38)

1. Human lamin B contains a farnesylated cysteine residue
2. The processing pathway of prelamin A
3. Isoprenylation of a protein kinase. Requirement of farnesylation/α-carboxyl methylation for full enzymatic activity of rhodopsin kinase
4. The γ subunit of transducin is farnesylated
5. Protein farnesyl transferase as a target for the development of anticancer drugs
6. Ras oncogenes in human cancer: A review
7. Function and regulation of Ras
8. Ras signalling and apoptosis
9. Isoprenoid addition to Ras proteins is the critical modification for its membrane association and transforming activity
10. Benzodiazepine peptidomimetics: Potent inhibitors of Ras farnesylation in animal cells
11. Selective inhibition of ras-dependent transformation by a farnesyltransferase inhibitor
12. Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes
13. Protein farnesyl-transferase inhibitors block the growth of ras-dependent tumors in nude mice
14. Benzodiazepine peptidomimetic BZA-5B interrupts the MAP kinase activation pathway in H-Ras-transformed Rat-1 cells, but not in untransformed cells
15. Peptidomimetic inhibitors of Ras farnesylation and function in whole cells
16. Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion
17. Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro
18. Unusual tight binding of R115777 to farnesyl protein transferase (FPT) allows for ex vivo measurement of FPT inhibition
19. Effects of farnesyl transferase inhibitor R115777 on hematopoiesis, leukemic cell proliferation, and signalling through the mitogen-activated protein kinase (MAPK) pathway
20. Interaction of the farnesyl protein transferase inhibitor (FTI) R115777 with cytotoxic chemotherapeutics in vitro and in vivo
21. Combined cell cycle and cytotoxic effects of paclitaxel and R115777, a specific inhibitor of p21 ras function and protein farnesylation in human prostate and breast carcinoma cell lines
22. Farnesyl transferase inhibitor R115777 radiosensitizes human glioma cell lines
23. Farnesylated RhoB increases cell survival after irradiation of NIH3T3 cells
24. Drug resistance to the farnesyl transferase inhibitor R115777
25. Preclinical antitumor and pharmacodynamic studies with the farnesyl transferase inhibitor (FTI) R115777
26. Unexpected pharmacodynamics of the farnesyl protein transferase inhibitor (FTI) R115777
27. Effects of R115777, a farnesyl transferase inhibitor (FTI), on methylnitrosourea (MNU)-induced mammary cancers: Role of HaRas mutation
28. Phase I clinical and pharmacokinetic trial of the farnesyltransferase inhibitor R115777 on a 21-day dosing schedule
29. Phase I and pharmacologic study with the novel farnesyltransferase inhibitor (FTI) R115777
30. Phase I and pharmacokinetic study of the orally administered farnesyl transferase inhibitor R115777 in patients with advanced solid tumors
31. Phase I and pharmacokinetic study of farnesyl protein transferase inhibitor R115777 in advanced cancer
32. Inhibition of HDJ2 protein farnesylation in peripheral blood mononuclear cells as a pharmacodynamic endpoint in a phase I study of R115777 and gemcitabine
33. Phase-I combination trial of the farnesyltransferase inhibitor (FTI) R115777 with a 5FU/LV regimen in advanced colorectal (CRC) or pancreatic (PC) cancer
34. A phase I, pharmacological and biological study of the farnesyl transferase inhibitor (FTI) R115777 and capecitabine in patients (pts) with advanced solid malignancies
35. Clinical activity with the farnesyl transferase inhibitor R115777 in patients with advanced breast cancer - Relationship with tumour phenotype
36. Phase I and pharmacologic study with the novel farnesyl-transferase inhibitor (FTI) R115777