Farnesyl transferase inhibitors - A novel therapy for breast cancer

Endocrine-Related Cancer

Volumn 8, Issue 3, 2001, Pages 227-235

  Johnston, S R D ^a   Kelland, L R ^a  

^a ROYAL MARSDEN HOSPITAL   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

(ALPHA HYDROXYFARNESYL)PHOSPHONIC ACID; 2 [[2 [[2 [(2 AMINO 3 MERCAPTOPROPYL)AMINO] 3 METHYLPENTYL]OXY] 1 OXO 3 PHENYLPROPYL]AMINO] 4 (METHYLSULFONYL)BUTANOIC ACID ISOPROPYL ESTER; 3 BENZYL 7 CYANO 2,3,4,5 TETRAHYDRO 1 (1H IMIDAZOL 4 YLMETHYL) 4 (2 THIENYLSULFONYL) 1H 1,4 BENZODIAZEPINE; BIOLOGICAL MARKER; BMS 186511; CAPECITABINE; CISPLATIN; DOCETAXEL; DOXORUBICIN; FLUOROURACIL; L 778123; LONAFARNIB; N [[5 [(2 AMINO 3 MERCAPTOPROPYL)AMINO][1,1' BIPHENYL] 2 YL]CARBONYL]METHIONINE METHYL ESTER; PACLITAXEL; PRODRUG; PROTEIN FARNESYLTRANSFERASE; PROTEIN FARNESYLTRANSFERASE INHIBITOR; RAS PROTEIN; TIPIFARNIB; TRASTUZUMAB; UNCLASSIFIED DRUG; VINBLASTINE;

ADVANCED CANCER; APOPTOSIS; BREAST CARCINOMA; CANCER CHEMOTHERAPY; CANCER COMBINATION CHEMOTHERAPY; CELL STRAIN MCF 7; CELL TRANSFORMATION; CLINICAL TRIAL; CONFERENCE PAPER; CYTOSTASIS; DOSE RESPONSE; DRUG EFFICACY; DRUG INDUCED DISEASE; DRUG MECHANISM; DRUG POTENTIATION; DRUG STRUCTURE; DRUG TARGETING; ENZYME INHIBITION; GENE MUTATION; HUMAN; NONHUMAN; ONCOGENE RAS; PROTEIN PROCESSING; SIGNAL TRANSDUCTION;

ALKYL AND ARYL TRANSFERASES; ANIMALS; ANTINEOPLASTIC AGENTS; BREAST NEOPLASMS; ENZYME INHIBITORS; FEMALE; HUMANS; PROTEIN PROCESSING, POST-TRANSLATIONAL; RAS PROTEINS;

EID: 0034795435     PISSN: 13510088     EISSN: None     Source Type: Journal    
DOI: 10.1677/erc.0.0080227     Document Type: Conference Paper

References (61)

1. A phase I trial of the farnesyl transferase inhibitor SCH66336; evidence for biological and clinical activity
2. Comparison of potential markers of farnesyltransferase inhibition
3. Farnesyl transferase inhibitors block the farnesylation of CENP-E and CENP-F and alter the association of CNEP-E with the microtubules
4. Phase I trial of weekly paclitaxel and BMS 214662 in patients with advanced solid tumors
5. Ras genes
6. The farnesyltransferase inhibitor FFI-277 radiosensitizes H-ras transformed rat embryo fibroblasts
7. Inhibiting Ras prenylation increases the radiosensitivity of human tumor cell lines with activating mutations of ms oncogenes
8. Novel tricyclic inhibitors of farnesyl protein transferase
9. Ras protein activation in human malignancy
10. Aberrant function of the Ras signal transduction pathway in human breast cancer
11. Overexpression of the Ras-related TC21/R-Ras2 protein may contribute to the development of human breast cancers
12. Cell growth inhibition by farnesyltransferase inhibitors is mediated by gain of geranylgeranylated RhoB
13. Activation of the PI3′K-AKT pathway masks the pro-apoptotic effects of famesyltransferase inhibitors
14. Characterisation of the antitumor effects of the selective farnesyl protein transferase inhbitor R115777 in vivo and in vitro
15. Phase I and pharmacokinetic study of the oral farnesyl transferase inhibitor SCH 66336 given twice daily in patients with advanced solid tumors
16. Proliferation of human malignant astrocytomas is dependent on Ras activation
17. A phase I pharmacokinetic and biological study of the farnesyl transferase inhibitor R115777 and capecitabine in patients with advanced solid malignancies
18. Phase I clinical and pharmacokinetic trial of the farnesylytransferase inhibitor R115777 on a 21-day dosing schedule
19. Phase I and pharmacokinetic study of SCH66336, a novel FPTI using a 2-week on, 2-week off schedule
20. Farnesyl transferase inhibitors: A novel targeted therapy for cancer
21. Clinical activity with the farnesyl transferase inhibitor R 115777 in patients with advanced breast cancer - Relationship with tumour phenotype
22. Isoprenoid addition to ras protein is the critical modification for its membrane association and transforming activity
23. Preclinical antitumor activity and pharmacodynamic studies with the farnesyly protein transferase inhbitor R115777 in human breast cancer
24. The PI3-kinase/Akt signaling pathway delivers an anti-apoptotic signal
25. Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice
26. Phase I study of farnesyltransferase inhibitor SCH66336 with paclitaxel in solid tumours; dose-finding, pharmacokinetics, efficacy/safety
27. The activation of phosphatidylinositol 3-kinase by Ras
28. A divergence in the MAP kinase regulatory network defined by MEK kinase and Raf
29. Farnesylytransferase inhibitors induce apoptosis of ras-transformed cells denied substratum attachment
30. Requirement for Ras in Raf activation is overcome by targeting Raf to the plasma membrane
31. Ras farnesyltransferase; a new therapeutic target
32. Anti-tumour activity of SCH66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumour xenograft models and wap-ras transgenic mice
33. Function and regulation of Ras
34. Activators and effectors of ras p21 proteins
35. Bisubstrate inhibitors of farnesyltransferase; a novel class of specific inhibitors of ras transformed cells
36. Cell signalling; Raf gets it together
37. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells
38. Farnesyl transferase inhibitors cause enhanced mitotic sensitivity to taxol and epothilones
39. Sequence dependence of protein isoprenylation
40. Treatment with farnesyl-protein transferase inhibitor induces regression of mammary tumors in transforming growth factor (TGF) alpha and TGF alpha/neu transgenic mice by inhibition of mitogenic activity and induction of apoptosis
41. A phase I clinical and pharmacokinetic trial of the farnesyl transferase inhibitor R115777 + docetaxel; a promising combination in patients with solid tumours
42. Farnesylytransferase inhibition causes morphological reversion of ras-transformed cells by a complex mechanism that involves regulation of actin cytoskeleton
43. Design and structural requirements of potent peptidomimetics inhibitors of p21 fas farnesyltransferase
44. 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
45. Inhibition of purified p21Ras farnesyl: Protein transferase by Cys-AAX tetrapeptides
46. The small GTP-binding protein Rho regulates the assembly of focal adhesions and actin stress fibres in response to growth factors
47. Incidence of activating ras oncogene mutations associated with primary and metastatic breast cancer
48. Ras protein farnesyltransferase: A strategic target for anticancer therapeutic development
49. Phase I and pharmacokinetic study with the novel farnesyltransferase inhibitor R115777
50. A phase I pharmacokinetic and biologic correlative study of R115777 and trastuzumab (Herceptin) in patients with advanced cancer
51. A farnesyl-protein transferase inhibitor induces p21 expression and G1 block in p53 wild-type tumor cells
52. A peptidomimetic inhibitor of farnesyl protein transferase blocks the anchorage-dependent and -independent growth of human tumor cell lines
53. A phase I and PK study of farnesyl transferase inhibitor L-788,123 administered as a seven day continuous infusion in combination with paclitaxel
54. The farnesyl protein transferase inhibitor SCH66336 synergises with taxanes in vitro and enhances their antitumor activity in vivo
55. Isolation of transforming sequence from a human bladder cancer cell line
56. Interaction of the farnesyl protein transferase inhibitor R115777 with cytotoxic chemotherapeutics in vitro and in vivo
57. Use of chemotherapy plus a monoclonal antibody against HER2 for metasatic breast cancer that overexpresses HER2
58. Correlations among p53, HER2/neu and ras overexpression and aneuploidy by multiparameter flow cytometry in human breast cancer; evidence for a common phenotypic evolutionary pattern in infiltrating ductal carcinomas
59. Farnesyltransferase inhibitors induce cytochrome c release and caspase 3 activation preferentially in transformed cells
60. Frequent loss of H-ras allele correlates with aggressive human primary breast carcinomas
61. Phase I and pharmacokinetic study of farnesyl protein transferase inhibitor R115777 in advanced cancer