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Review

Farnesyltransferase inhibitors: recent advances

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Pages 175-186 | Published online: 02 Mar 2005

Bibliography

  • SAWYERS CL: Rational therapeutic intervention in cancer: kinases as drug targets. Curr. Opin. Genet. Dev. (2002) 12:111–115.
  • REISS Y, STRADLEY SJ, GIERASCH LM,BROWN MS, GOLDSTEIN JL: Sequence requirement for peptide recognition by rat brain p2lras protein farnesyltransferase. Proc. Nati Acad. Sci. USA (1991) 88:732–736.
  • CASEY PJ, THISSEN JA, MOOMAW JF:Enzymic modification of proteins with a geranylgeranyl isoprenoid. Proc. Nati Acad. Sci. USA (1991) 88:8631–8635.
  • BARBACID M: Ras genes. Anna. Rev Biochem. (1987) 56:779–827.
  • COX AD, DER CJ: Farnesyltransferase inhibitors: promises and realities. Curt: Opin. Pharmacol. (2002) 2:388–393.
  • ••Recommendable review on farnesyltransferase .
  • PRENDERGAST GC, PANE N: Farnesyltransferase inhibitors: mechanism and applications. Expert Opin. Investig. Drugs (2001) 10:2105–2116.
  • NAGASU T, YOSHIMATSU K, ROWELL C, LEWIS MD, GARCIA AM: Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956. Cancer Res. (1995) 55:5310–5314.
  • WHYTE DB, KIRSCHMEIER P, HOCKENBERRY TN et al.: K- and N-Ras are geranylgeranylated in cells treated with farnesyl protein transferase inhibitors. Biol Chem. (1997) 272:14459–14464.
  • •Alternative prenylation of K-Ras and N-Ras by GGT when treated with FTI.
  • KOHL NE, OMER CA, CONNER MW et al.: Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice. Nat . Medicine (New York) (1995) 1:792–797.
  • LAVELLE F: American association for cancer research 1998: promises and prospects for the next century. Expert Opin. Investig. Drugs (1998) 7:1015–1021.
  • END DW, SMETS G, TODD AV et aL: Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R-115777 in vivo and in vitro. Cancer Res. (2001) 61:131–137.
  • HEAD JE, JOHNSTON SRD: Protein farnesyltransferase inhibitors. Expert Opin. Emerging Drugs (2003) 8:163–178.
  • ••Recommendable review on the clinicalstatus of FTIs.
  • CAPONIGRO F, CASALE M, BRYCE J: Farnesyl transferase inhibitors in clinical development. Expert Opin. Investig. Drugs (2003) 12:943–954.
  • ••Recommendable review on the clinicalstatus of FTIs.
  • ADJEI AA, ERLICHMAN C, DAVIS JN et al.: A Phase I trial of the farnesyl transferase inhibitor SCH-66336: evidence for biological and clinical activity. Cancer Res. (2000) 60:1871–1877.
  • KARP JE, LANCET JE, KAUFMANN SH et al.: Clinical and biologic activity of the farnesyltransferase inhibitor R-115777 in adults with refractory and relapsed acute leukemias: a Phase I clinical-laboratory correlative trial. Blood (2001) 97:3361–3369.
  • CORTES JE, KURZROCK R, KANTARJIAN HM: Farnesyltransferase inhibitors: novel compounds in development for the treatment of myeloid malignancies. &min. Hematol (2002) 39:26–30.
  • CORTES J, ALBITAR M, THOMAS D et al.: Efficacy of the farnesyl transferase inhibitor R-115777 in chronic myeloid leukemia and other hematologic malignancies. Blood (2003) 101: 1692-1697.
  • SHI B, YAREMKO B, HAJIAN G et al.: The farnesyl protein transferase inhibitor SCH-66336 synergizes with taxanes M vitro and enhances their antitumor activity in vivo. Cancer Chemother: Pharmacol (2000) 46:387–393.
  • ••Synergism of SCH-66336 with taxanes.
  • BERNHARD EJ, MCKENNA WG, HAMILTON AD et al.: Inhibiting Ras prenylation increases the radiosensitivity of human tumor cell lines with activating mutations of ras oncogenes. Cancer Res. (1998) 58:1754–1761.
  • DOLL RJ: Inhibition of farnesyl protein transferase - a review of the recent patent literature. IDrugs (2001) 4:1382–1388.
  • NJOROGE FG, TAVERAS AG, KELLY Jet al.: (+) 4 [2 [4 (8 Chloro-3,10-dibromo-6,11-dihydro-5H-benzo [5,6]cyclohepta [1,2-b[- pyridin 11(h) yl) 1 piperidiny11-2-oxo-ethyl]-1-piperidinecarboxamide (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent. J Med. Chem. (1998) 41:4890–4902.
  • ESKENS FA, AWADA A, CUTLER DL et al.: Phase I and pharmacokinetic study of the oral farnesyl transferase inhibitor SCH-66336 given twice daily to patients with advanced solid tumors. Journal Clin. Omni (2001) 19:1167–1175.
  • WANG E-J, CASCIANO CN, CLEMENT RP, JOHNSON WW: The farnesyl protein transferase inhibitor SCH-66336 is a potent inhibitor of MDR1 product P-glycoprotein. Cancer Res. (2001) 61:7525–7529.
  • PETERS DG, HOOVER RR, GERLACH MJ et al.: Activity of the farnesyl protein transferase inhibitor SCH-66336 against BCR/ABL-induced murine leukemia and primary cells from patients with chronic myeloid leukemia. Blood (2001) 97:1404–1412.
  • TAVERAS AG, KIRSCHMEIER P, BAUM CM: SCH-66336 (Sarasar) and other benzocycloheptapyridyl farnesyl protein transferase inhibitors: discovery, biology and clinical observations. Carr: Topics Med. Chem. (Sharjah, United Arab Emirates) (2003) 3:1103–1114.
  • •Review of the history and SAR of SCH-66336.
  • HOOVER RR, MAHON F-X, MELO JV, DALEY GQ: Overcoming STI-571 resistance with the farnesyl transferase inhibitor SCH-66336. Blood (2002) 100:1068–1071.
  • SMALLEY KSM, EISEN TG: Farnesyl transferase inhibitor SCH-66336 is cytostatic, pro-apoptotic and enhances chemosensitivity to cisplatin in melanoma cells. Int. J. Cancer (2003) 105:165–175.
  • BISHOP WR, PAI JJK, ARMSTRONG L et al.: Tricyclic farnesyl protein transferase inhibitors: antitumor activity and effects on protein prenylation. Farnesyltransferase Inhib. Cancer Ther: (2001) 87–101.
  • HUANG C-Y, ROKOSZ LL, STAUFFER TM et al.: Structural optimization of a farnesyl protein transferase inhibitor derived from a small-molecule combinatorial library. 225th ACS National Meeting. New Orleans, LA, USA (23–27 March 2003) MEDI131.
  • NJOROGE FG, VIBULBHAN B, PINTO P et al: Trihalobenzocycloheptapyridine analogues of SCH-66336 as potent inhibitors of farnesyl protein transferase. Bioorg. Med. Chem. (2003) 11:139–143.
  • TAVERAS AG, CHAO J, AKI C et al: SCH-66336 and beyond: discovering next-generation inhibitors of farnesyl protein transferase. 222nd ACS National Meeting. Chicago, IL, USA (26–30 August 2001) MEDI004.
  • VENET M, END D, ANGIBAUD P: Farnesyl protein transferase inhibitor Zarnestra R-115777 - history of a discovery. Curr. Topics Med. Chem. (Sharjah, United Arab Emirates) (2003) 3:1095–1102.
  • •Review of the history and SAR of R-115777.
  • CRUL M, DE KLERK GJ, SWART M et al.: Phase I clinical and pharmacologic study of chronic oral administration of the farnesyl protein transferase inhibitor R-115777 in advanced cancer. J. Clin. Omni (2002) 20:2726–2735.
  • KELLAND LR: Farnesyl transferase inhibitors in the treatment of breast cancer. Expert Opin. Invesug. Drugs (2003) 12:413–421.
  • •Review of FTIs and breast cancer treatment.
  • CUNNINGHAM D, DE GRAMONT A, SCHEITHAUER W, AL E: Randomized double-blind placebo controlled trial of the farnesil transferase inhibitor R-115777 (Zarnestra) in advanced refractory colorectal cancer. Proc. Am. Soc. Clin. Omni (2002) 21(126a):A502.
  • VAN CUTSEM E, KARASEK P, OETTLE H, AL E: Phase III trial comparing gemcitabine + R -115777 (Zarnestra) versus gemcitabine + placebo in advanced pancreatic cancer. Proc. Am. Soc. Clin. Omni (2002) 21(130a):A517.
  • ANGIBAUD P, BOURDREZ X, DEVINE A et al.: 5-Imidazolylquinolinones, -quinazolinones, and -benzoazepinones as farnesyltransferase inhibitors. Bioorg. Med. Chem. Lett. (2003) 13:1543–1547.
  • ROSE WC, LEE FYF, FAIRCHILD CR et al.: Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. Cancer Res. (2001) 61:7507–7517.
  • •Apoptotic activity of BMS-214662.
  • CAMACHO LH, SOIGNET SL, PEZZULLI S et al: Dose escalation study of oral farnesyl transferase inhibitor BMS-214662 in patients with solid tumors. Proc. Am. Soc. Chi). Oncol (2001) 20(79a):A311.
  • RYAN DP, EDER JP, SUPKO JG, AL E: Phase I clinical trial of the farnesyl transferase inhibitor BMS-214662 in patients with advanced solid tumors. Proc. Am. Soc. Clin. Oncol (2000) 19(185a):A720.
  • MACKAY HJ, HOEKSTRA R, ESKENS FA, AL E: A Phase I dose escalating study of BMS-214662 in combination with cisplatin in patients with advanced solid tumors. Proc. Am. Soc. Clin. Omni (2001) 20(80a):A315.
  • DY GK, BRUZEK LAURA M, GROGHAN GA: A Phase I trial of the novel farnesyl protein transferase inhibitor BMS-214662 in combination with pactlitaxel and carboplatin in patients with advanced cancer. Proc. Am. Association Cancer Res. (2002) 43:A2736.
  • CORTES J, KURZROCK R, O'BRIEN S, AL E: Phase I study of a farnesyl transferase inhibitor BMS-214662 in patients with refractory or relapsed acute leukaemias. Blood (2001) 98(594a):A2489.
  • LEFTHERIS K, KLINE T, NATARAJAN S et al.: Peptide-based P21ras farnesyl transferase inhibitors: systematic modification of the tetrapeptide CA1A2X motif. Bioorg. Med. Chem. Lett. (1994) 4:887–892.
  • LEFTHERIS K, KLINE T, VITE GD et al.: Development of highly potent inhibitors of ras farnesyltransferase possessing cellular and in vivo activity. J. Med. Chem. (1996) 39:224–236.
  • HUNT JT, LEE VG, LEFTHERIS K et al: Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase. J. Med. Chem. (1996) 39:353–358.
  • SINGH SB, LINGHAM RB: Current progress on farnesyl protein transferase inhibitors. Carr: Opin. Drug Discov. Dev. (2002) 5:225–244.
  • LOBELL RB, LIU D, BUSER CA et al.: Preclinical and clinical pharmacodynamic assessment of L-778123, a dual inhibitor of farnesyl: protein transferase and geranylgeranyl: protein transferase Type-I. MM. Cancer The]: (2002) 1:747–758.
  • •The first demonstration of GGT inhibition in humans. No inhibition of K-Ras prenylation.
  • BRITTEN CD, ROWINSKY EK, SOIGNET S et al.: A Phase I and pharmacological study of the farnesyl protein transferase inhibitor L-778123 in patients with solid malignancies. Gin. Cancer Res. (2001) 7:3894–3903.
  • HAHN SM, BERNHARD EJ, REGINE W et al: A Phase I trial of the farnesyltransferase inhibitor L-778123 and radiotherapy for locally advanced lung and head and neck cancer. Gin. Cancer Res. (2002) 8:1065–1072.
  • •Combination of radiotherapy and L-778123.
  • EVANS TL, FIDIAS P, SKARIN A et al:A Phase II study of efficacy and tolerability of the farnesyl-protein transferase inhibitor L-778123 as first-line therapy in patients with advanced non-small cell lung cancer. Proc. Am. Soc. Clin. OncoL (2002) 21:13b.
  • BELL IM, GALLICCHIO SN, ABRAMS M et al: Design and biological activity of (S) 4 (5 Il1 (3 chlorobenzy1)-2-oxopyrrolidin-3-ylaminolmethyllimidazol-1-ylmethyflbenzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency. Med. Chem. (2001) 44:2933–2949.
  • MACTOUGH SC, DESOLMS SJ, SHAW AW et al.: Diaryl ether inhibitors of farnesyl-protein transferase. Bioorg. Med. Chem. Lett. (2001) 11:1257–1260.
  • DINSMORE CJ, BOGUSKY MJ, CULBERSON JC et al.: Conformational restriction of flexible ligands guided by the transferred noe experiment: potent macrocyclic inhibitors of farnesyltransferase. Am. Chem. Soc. (2001) 123:2107–2108.
  • •First description of the macrocydic analogues of L-778123.
  • BELL IM, GALLICCHIO SN, ABRAMS M et al: 3-Aminopyrrolidinones farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency. J. Med. Chem. (2002) 45:2388–2409.
  • LEONARD DM: Ras farnesyltransferase: a new therapeutic target. J. Med. Chem. (1997) 40:2971–2990.
  • GIRAUD E, LUTTMANN C, LAVELLE F et al: Multivariate data analysis using D-optimal designs, partial least squares, and response surface modeling: a directional approach for the analysis of farnesyltransferase inhibitors. J. Med. Chem. (2000) 43:1807–1816.
  • TROTTER BW, QUIGLEY AG, LUMMA WC et al: 2-Arylindole-3-acetamides FPP-competitive inhibitors of farnesyl protein transferase. Bioorg. Med. Chem. Lett. (2001) 11:865–869.
  • ADJEI AA, CROGHAN GA, ERLICHMAN C et al.: A Phase I trial of the farnesyl protein transferase inhibitor R-115777 in combination with gemcitabine and cisplatin in patients with advanced cancer. Clin. Cancer Res. (2003) 9:2520–2526.
  • HANAHAN D, WEINBERG RA: The hallmarks of cancer. Cell (2000) 100:57–70.
  • DALEY GQ: Towards combination target-directed chemotherapy for chronic myeloid leukemia: role of farnesyl transferase inhibitors. Semin. Hematol (2003) 40:11–14.
  • ASHAR HR, JAMES L, GRAY K et al.: Farnesyl transferase inhibitors block the farnesylation of CENP-E and CENP-F and alter the association of CENP-E with the microtubules. J. Biol. Chem. (2000) 275:30451–30457.
  • DIAMOND RH, CRESSMAN DE, LAZ TM, ABRAMS CS, TAUB R: PRL-1, a unique nuclear protein tyrosine phosphatase, affects cell growth. Ma Cell. Biol. (1994) 14:3752–3762.
  • CATES CA, MICHAEL RL, STAYROOK KR et al.: Prenylation of oncogenic human PTP(CAAX) protein tyrosine phosphatases. Cancer Lett. (1996) 110:49–55.
  • LIU M, BRYANT MS, CHEN J et al.:Antitumor activity of SCH-66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. Cancer Res. (1998) 58:4947–4956.
  • BARRINGTON RE, SUBLER MA, RANDS E et al.: A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis. MoL Cell. Biol. (1998) 18:85–92.
  • GU WZ, TAHIR SK, WANG YC et al.: Effect of novel CAAX peptidomimetic farnesyltransferase inhibitor on angiogenesis M vitro and in vivo. Eur: J. Cancer (1999) 35:1394–1401.
  • YOKOYAMA K, TROBRIDGE P, BUCKNER FS et al.: The effects of protein farnesyltransferase inhibitors on trypanosomatids: inhibition of protein farnesylation and cell growth. Mel Biochem. Parasite] (1998) 94:87–97.
  • •First description of FTI as a potential treatment for parasitic infection.
  • OHKANDA J, LOCKMAN JW, YOKOYAMA K et al.: Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity. Bieerg. Med. Chem. Lett. (2001) 11:761–764.

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