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Blood Reviews
Volume 21, Issue 4
, Pages 173-182
, July 2007
Farnesyltransferase inihibitors in hematologic malignancies
References
- End DW, Mevellec L, Angibaud P. Farnesyl protein transferase inhibitors: molecular mechanisms and progress in the clinic. Curr Top Med Chem. In press.
- . Farnesyl protein transferase inhibitors and other therapies targeting the Ras signal transduction pathway. Invest New Drugs. 1999;17:241–258
- . Ras protein farnesyltransferase: A strategic target for anticancer therapeutic development. J Clin Oncol. 1999;17:3631–3652
- . Proteins regulating Ras and its relatives. Nature. 1993;366:643–654
- . Protein prenylation: key to ras function and cancer intervention?. Cell Growth Differ. 1992;3:461–469
- . ras and human tumors. Semin Cancer Biol. 1992;3:241–247
- . ras oncogenes in human cancer: a review. Cancer Res. 1989;49:4682–4689
- . Targeting the Ras signaling pathway: a rational, mechanism-based treatment for hematologic malignancies?. Blood. 2000;96:1655–1669
- . Farnesyltransferase inhibitors in hematologic malignancies: new horizons in therapy. Blood. 2003;102:3880–3889
- . Protein kinase B (c-Akt) in phosphatidylinositol-3-OH kinase signal transduction. Nature. 1995;376:599–602
- Activation of phosphatidylinositol 3-kinase is sufficient for cell cycle entry and promotes cellular changes characteristic of oncogenic transformation. Mol Cell Biol. 1998;18:5699–5711
- Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res. 2001;61:131–137
- . Farnesyltransferase inhibitors: promises and realities. Curr Opin Pharmacol. 2002;2:388–393
- . Farnesyltransferase inhibitors in myelodysplastic syndrome. Curr Hematol Rep. 2005;4:186–190
- . Farnesyl protein transferase inhibition: a novel approach to anti-tumor therapy. the discovery and development of SCH 66336. Curr Med Chem. 2001;8:1419–1436
- . Farnesyl protein transferase inhibitors as targeted therapies for hematologic malignancies. Semin Hematol. 2001;38:16–23
- . Cell growth inhibition by farnesyltransferase inhibitors is mediated by a gain of geranylgeranylated RhoB. Mol Cell Biol. 1999;19:1831–1840
- The farnesyl transferase inhibitor SCH 66336 induces a G(2) –
>
M or G(1) pause in sensitive human tumor cell lines. Exp Cell Res. 2001;262:17–27 - . The farnesyltransferase inhibitor, FTI-2153, blocks bipolar spindle formation and chromosome alignment and causes prometaphase accumulation during mitosis of human lung cancer cells. J Biol Chem. 2001;276:16161–16167
- . Farnesyltransferase inhibitors alter the prenylation and growth-stimulating function of RhoB. J Biol Chem. 1997;272:15591–15594
- Phase I and pharmacokinetic study of farnesyl protein transferase inhibitor R115777 in advanced cancer. J Clin Oncol. 2000;18:927–941
- . The influence of farnesyl protein transferase inhibitor R115777 (Zarnestra) alone and in combination with purine nucleoside analogs on acute myeloid leukemia progenitors in vitro. Eur J Haematol. 2004;73:418–426
- . Mutant N-ras induces myeloproliferatives disorders and apoptosis in bone marrow repopulated mice. Blood. 1999;93:2043–2056
- Clinical and biologic activity of the farnesyltransferase inhibitor R115777 in adults with refractory and relapsed acute leukemias: a phase 1 clinical-laboratory correlative trial. Blood. 2001;97:3361–3369
- Zarnestra (R115777) in patients with relapsed and refractory acute myelogenous leukemia (AML): results of a multicenter phase 2 study. Blood. 2003;102(Pt1):176a;Abstract 614
- Tipifarnib (ZARNESTRATM) in previously untreated poor-risk AML of the elderly: updated results of a multicenter phase 2 trial. Blood. 2004;104(pt1):249a;Abstract 874
- Identification of molecular predictors of response to ZARNESTRATM (tipifarnib, R115777) in relapsed and refractory acute myeloid leukemia. Blood. 2004;104:246a;Abstract 861
- Dose ranging pharmacodynamic study of tipifarnib (R115777) in patients with relapsed and refractory hematologic malignancies. J Clin Oncol. 2004;22:4764–4770
- Tipifarnib (ZARNESTRA, R115777) as Maintenance Therapy for Adults in Complete Remission (CR) following Induction and Consolidation Therapies for Poor-Risk Acute Myelogenous Leukemia (AML): A Phase II Trial. Blood. 2005;106:780a;Abstract 2783
- Phase I study of continuous oral administration of lonafarnib (SarasarTM) in patients with advanced hematologic malignancies. Blood. 2002;100:789a;Abstract 3120
- Continuous oral lonafarnib (SarasarTM) for the treatment of patients with advanced hematologic malignancies: a phase II study. Blood. 2002;100:793a;Abstract 3132
- Farnesyltransferase inhibitor R115777 in myelodysplastic syndrome: clinical and biologic activities in the phase 1 setting. Blood. 2003;102:4527–4534
- Phase II study of R115777, a farnesyl transferase inhibitor, in myelodysplastic syndrome. J Clin Oncol. 2004;22:1287–1292
- High-risk myelodysplastic syndrome (MDS): first results of international phase 2 study with oral farnesyltransferase inhibitor R115777 ZARNESTRATM). Blood. 2004;104(pt 1):23a;Abstract 68
- Phase I study using alternate week administration of the farnesyl transferase inhibitor R115777 (Zarnestra) in patients with myelodysplastic syndrome. Blood. 2004;104(Pt 1):402a;Abstract 1436
- Continuous oral lonafarnib (Sarasar) for the treatment of patients with myelodysplastic syndrome. Blood. 2003;102:421a;Abstract 1531
- Activity of the farnesyl protein transferase inhibitor SCH66336 agains BCR/ABL_induced murine leukemia and primary cells from patients with chronic myeloid leukemia. Blood. 2001;97:1404–1412
- . Treatment of Bcr/Abl-positive acute lymphoblastic leukemia in P190 transgenic mice with the farnesyl transferase inhibitor SCH66336. Blood. 2001;97:1399–1403
- . Overcoming STI571 resistance with the farnesyl transferase inhibitor SCH66336. Blood. 2002;100:1068–1071
- . ABL-specific tyrosine kinase inhibitor, STI571 in vitro, affects Ph-positive acute lymphoblastic leukemia and chronic myelogenous leukemia in blastic crisis. Leukemia. 2001;15:989–990
- Efficacy of the farnesyl transferase inhibitor R115777 in chronic myeloid and other hematologic malignancies. Blood. 2003;101:1692–1697
- Tipifarnib (ZARNESTRA) and Imatinib (GLEEVEC) combination therapy in patients with advanced chronic myelogenous leukemia (CML): preliminary results of a phase I study. Blood. 2003;102:909a;Abstract 3384
- Pilot study of lonafarnib, a farnesyl transferase inhibitor, in patients with chronic myeloid leukemia in the chronic or accelerated phase that is resistant or refractory to imatinib therapy. Cancer. 2006;106:346–352
- A phase I study of tipifarnib in combination with imatinib mesylate (IM) for patients (Pts) with chronic myeloid leukemia (CML) in chronic phase (CP) who failed IM therapy. Blood. 2004;104(Pt 1):176;Abstract 1011
- Farnesyl transferase inhibitor R115777 induces apoptosis of human myeloma cells. Leukemia. 2002;16:1664–1667
- Effect of farnesyl transferase inhibitor R115777 on the growth of fresh and cloned myeloma cells in vitro. Blood. 2003;102:3349–3353
- The farnesyl transferase inhibitor, FTI-277, inhibits growth and induces apoptosis in drug-resistant myeloma tumor cells. Leukemia. 2003;17:451–457
- . R115777 induces Ras-independent apoptosis of myeloma cells via multiple intrinsic pathways. Mol Cancer Ther. 2004;3:179–186
- Farnesyltransferase inhibitor tipifarnib is well tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic/tumor survival pathways in patients with advanced multiple myeloma. Blood. 2004;103:3271–3277
- . The combination of the farnesyl transferase inhibitor lonafarnib and the proteasome inhibitor bortezomib induces synergistic apoptosis in human myeloma cells that is associated with down-regulation of p-AKT. Blood. 2005;106:4322–4329
- . Myelofibrosis with myeloid metaplasia. N Engl J Med. 2000;342:1255–1265
- . In vitro antiproliferative activity of the farnesyltransferase inhibitor R115777 in hematopoietic progenitors from patients with myelofibrosis with myeloid metaplasia. Leukemia. 2003;17:849–855
PII: S0268-960X(06)00075-0
doi: 10.1016/j.blre.2006.12.001
© 2006 Elsevier Ltd. All rights reserved.
Next »
Blood Reviews
Volume 21, Issue 4
, Pages 173-182
, July 2007
