Anticancer activity of farnesyltransferase and geranylgeranyltransferase i inhibitors: prospects for drug development

Bibliography

• BARBACID M: ras Genes. Ann. Rev. Biochem. (1987) 56:779–827.
   PubMed Web of Science ®Google Scholar
• SEBTI SM, HAMILTON AD: Inhibition of Ras prenylation: a novel approach to cancer chemotherapy. Pharmacol. Ther. (1997) 74:103–114.
   PubMed Web of Science ®Google Scholar
• GIBBS JB, OLIFF A: The potential of farnesyltransferase inhibitors as cancer chemotherapeutics. Ann. Rev. Phar-macol. Toxicol (1997) 37:143–166.
   PubMed Web of Science ®Google Scholar
• ZHANG FL, CASEY PJ: Protein prenylation: molecular mechanisms and functional consequences. Ann. Rev. Biochem. (1996) 65:241–269.
   PubMed Web of Science ®Google Scholar
• REISS Y, GOLDSTEIN JL, SEABRA MC, CASEY PJ, BROWN MS: Inhibition of purified p211as farnesyl: protein transferase by Cys-AAX tetrapeptides. Cell (1990) 62:81–88.
   PubMed Web of Science ®Google Scholar
• LERNER EC, QIAN Y, BLASKOVICH MA et al: Ras CAAXpeptidomimetic FTI-277 selectively blocks oncogenic Ras signalling by inducing cytoplasmic accumulation of inactive Ras/Raf complexes. J. Biol. Chem. (1995) 270:26802–26806.
   PubMed Web of Science ®Google Scholar
• LERNER EC, QIAN Y, HAMILTON AD, SEBTI SM: Disrup-tion of oncogenic K-Ras4B processing and signalling by a potent geranylgeranyltransferase I inhibitor. J. Biol. Chem. (1995) 270:26770–26773.
   PubMed Web of Science ®Google Scholar
• NIGAM M, SEONG C, QIAN Y, HAMILTON AD, SEBTI SM: Potent inhibition of human tumor p21 ras farnesyl transferase by A1A2-lacking CA1A2X peptidomimetics. J. Biol. Chem. (1993) 268:20695–20698.
   PubMed Web of Science ®Google Scholar
• QIAN Y, BLASKOVICH MA, SALEEM M et al.: Design and structural requirements of potent peptidomimetic in-hibitors of p2lras farnesyl transferase. J. Biol. Chem. (1994) 269:12410–12413.
   PubMed Web of Science ®Google Scholar
• SUN J, QIAN Y, HAMILTON AD, SEBTI SM: Ras CAAX pepti-domimetic FTI-276 selectively blocks in nude mice the growth of a human lung carcinoma with a K-Ras muta-tion and a p53 deletion. Cancer Res. (1995) 55:4243–4247.
   PubMed Web of Science ®Google Scholar
• VOGT A, QIAN Y, BLASKOVICH M et al: A non-peptide mimetic of Ras CAAX: selective inhibition of farnesyl-transferase and Ras processing. J. Biol. Chem. (1995) 270:660–664.
   PubMed Web of Science ®Google Scholar
• JAMES GL, GOLDSTEIN JL, BROWN MS et al.: Benzodi-azepine peptidomimetics: potent inhibitors of Ras far-nesylation in animal cells. Science (1993) 260:1937–1942.
   PubMed Web of Science ®Google Scholar
• KOHL NE, MOSSER SD, DESOLMS SJ et al.: Selective inhibi-tion of Ras-dependent transformation by a farnesyl-transferase inhibitor. Science (1993) 260:1934–1937.
   PubMed Web of Science ®Google Scholar
• GARCIA AM, ROWELL C, ACKERMANN K, KOWALCZYK JJ,LEWIS MD: Peptidomimetic inhibitors of Ras farnesyla-tion and function in whole cells. J. Biol. Chem. (1993) 268:18415–18418.
   PubMed Web of Science ®Google Scholar
• BISHOP WR, BOND R, PETRIN J et al.: Novel tricyclic in-hibitors of farnesyl protein transferase: biochemical and characterization and inhibition of Ras modifica-tion in transfected Cos cells. J. Biol. Chem. (1995) 270:30611–30618.
   PubMed Web of Science ®Google Scholar
• KOHL NE, OMER CA, CONNER MW et al.: Inhibition of far-nesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice. Nature Med. (1995) 1:792–796.
   PubMed Web of Science ®Google Scholar
• NAGASU T, YOSHIMATSU K, ROWELL C, LEWIS MD, GAR-CIA AM: Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956. Cancer Res. (1995) 55:5310–5314.
   PubMed Web of Science ®Google Scholar
• PATEL DV, GORDON EM, SCHMIDT RJ et al: Phosphinyl acid-based bisubstrate analog inhibitors of ras farnesyl protein transferase. J. Med. Chem. (1995) 38:435–442.
   PubMed Web of Science ®Google Scholar
• SEPP-LORENZINO L, MA Z, RANDS E et al: A peptidomi-metic inhibitor of farnesylprotein transferase blocks the anchorage-dependent and -independent growth of human tumor cell lines. Cancer Res. (1995) 55:5302–5309.
   PubMed Web of Science ®Google Scholar
• KOHL NE, WILSON FR, MOSSER SD et al.: Protein farnesyl-transferase inhibitors block the growth of ras-dependent tumors in nude mice. Proc. Natl. Acad. Sci. USA (1994) 91:9141–9145.
   PubMed Web of Science ®Google Scholar
• SATLER I, TAMANOI F: Regulation of the Ras Signalling Net-work. Burgess AW, Maruta H (Ed.), RG Landes, Austin, Texas (1996)95–137.
   Google Scholar
• LERNER EC, HAMILTON AD, SEBTI SM: Inhibition of rasphenylation - a signalling target for novel anti-cancer drug design. Anti-Cancer Drug Design (1997) 12(4):229–238.
   PubMedGoogle Scholar
• QIAN Y, SEBTI SM, HAMILTON AD: Farnesyltransferaseas a target for anti-cancer drug design. Biopolymers (Pep. Sci.) (1997) 43:25–41.
   PubMed Web of Science ®Google Scholar
• JAMES G, GOLDSTEIN JL, BROWN MS: Resistance of K-RASB (V12) proteins to farnesyltransferase inhibitors in Ratl cells. Proc. Natl. Acad. Sci. USA (1996) 93(9):4454–4458.
   PubMed Web of Science ®Google Scholar
• JAMES GL, GOLDSTEIN JL, BROWN MS: Polylysine andCVIIVI sequences of K-RasB dictate specificity of preny-lation and confer resistance to benzodiazepine pepti-domimetic in vitro. J. Biol. Chem. (1995) 270(11): 6221–6226.
   PubMed Web of Science ®Google Scholar
• LERNER EC, ZHANG TT, KNOWLES D et al. Inhibition of the prenylation of K-Ras, but not H- or N-Ras, is highly resistant to CAAX peptidomimetics and requires both a farnesyltransferase and a geranylgeranyltransferase I inhibitor in human tumor cell lines. Oncogene (1997) 15 (11) 1283–1288
   PubMed Web of Science ®Google Scholar
• ROWELL CA, KOWALCZYK JJ, LEWIS MD, GARCIA AM: Di-rect demonstration of geranylgeranylation and fame-sylation of KI-Ras in vivo. J. Biol. Chem. (1997) 272(22)14093–14097.
   Google Scholar
• WHYTE DB, KIRSCHMEIER P, HOCKENBERRY TN et al.: K-and N-Ras are geranylgeranylated in cells treated with farnesyl protein transferase inhibitors. J. Biol. Chem. (1997) 272(22):14459–14464.
   PubMed Web of Science ®Google Scholar
• SUN I, QIAN Y, HAMILTON AD, SEBTI SM: Both farnesyl-transferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic k-ras prenyla-tion but each alone is sufficient to suppress human tu-mor growth in nude mice xenografts. Oncogene. (In Press.)
   Google Scholar
• PRENDERGAST GC, DAVIDE JP, DESOLMS SJ et al.: Fame-syltransferase inhibition causes morphological rever-sion of ras-transformed cells by a complex mechanism that involves regulation of the actin cytoskeleton. Mol. Cell Biol (1994) 14:4193–4202.
   PubMed Web of Science ®Google Scholar
• MCGUIRE T, QIAN Y, HAMILTON AD, SEBTI SM: Platelet derived growth factor receptor tyrosine phosphoryla-tion requires protein geranylgeranylation and not far-nesylation. J. Biol. Chem. (1996) 271:27402–27407.
   PubMed Web of Science ®Google Scholar
• FINDER JD, LITZ JL, BLASKOVICH MA et al.: Inhibition of protein geranylgeranylation causes a superinduction of nitric oxide synthase-2 by IL-113 in pulmonary artery smooth muscle cells. J. Biol. Chem. (1997) 272:13484–13488.
   PubMed Web of Science ®Google Scholar
• VOGT A, SUN J, QIAN Y, HAMILTON AD, SEBTI SM: The geranylgeranyltransferase I inhibitor GGTI-298 arrests human tumor cells in GO/G1 and induces p21WAF/CIP/SDII in a-p53 independent manner. J. Biol. Chem. (1997) 272:27224–27229.
   PubMed Web of Science ®Google Scholar
• VOGT A, QIAN Y, MCGUIRE TF, HAMILTON AD, SEBTI SM: Protein geranylgeranylation, not farnesylation, is re-quired for the G1 to S phase transition in mouse fibro-blasts. Oncogene (1996) 13 (9) :1991–1999.
   PubMed Web of Science ®Google Scholar
• MIQUEL K, PRADINES A, SUN J et al.: GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells. Cancer Res. (1997) 57 (101846–1850.
   Google Scholar
• CLARK GJ, KINCH MS, ROGERS-GRAHAM K eta].: The Ras-related protein Rheb is farnesylated and antagonizes Ras signalling and transformation. J. Biol. Chem. (1997) 272 (16):10608–10615.
   Google Scholar
• LEBOWITZ PF, DU W, PRENDERGAST GC: Prenylation of RhoB is required for its cell transforming function but not its ability to activate serum response element-dependent transcription. J. Biol. Chem. (1997) 272(26)16093–16095.
   Google Scholar
• LEBOWITZ PF, CASEY PJ, PRENDERGAST GC, THISSEN JA: Farnesyltransferase inhibitors alter the prenylation and growth-stimulating function of RhoB. J. Biol. Chem. (1997) 272(25):15591–15594.
   PubMed Web of Science ®Google Scholar