A peptidomimetic inhibitor of farnesyl:protein transferase blocks the anchorage-dependent and -independent growth of human tumor cell lines.

PubWeight™: 2.04‹?› | Rank: Top 2%

🔗 View Article (PMID 7585592)

Published in Cancer Res on November 15, 1995

Authors

L Sepp-Lorenzino1, Z Ma, E Rands, N E Kohl, J B Gibbs, A Oliff, N Rosen

Author Affiliations

1: Program in Cell Biology and Genetics, Memorial Sloan-Kettering Cancer Center, New York, New York 10021, USA.

Articles citing this

Ras oncogenes: split personalities. Nat Rev Mol Cell Biol (2008) 7.91

TGF-beta signaling blockade inhibits PTHrP secretion by breast cancer cells and bone metastases development. J Clin Invest (1999) 5.30

A mechanism of repression of TGFbeta/ Smad signaling by oncogenic Ras. Genes Dev (1999) 5.13

Targeting protein prenylation for cancer therapy. Nat Rev Cancer (2011) 2.60

Defective repression of c-myc in breast cancer cells: A loss at the core of the transforming growth factor beta growth arrest program. Proc Natl Acad Sci U S A (2001) 2.55

Inhibition of Ras for cancer treatment: the search continues. Future Med Chem (2011) 2.14

Active oral regimen for elderly adults with newly diagnosed acute myelogenous leukemia: a preclinical and phase 1 trial of the farnesyltransferase inhibitor tipifarnib (R115777, Zarnestra) combined with etoposide. Blood (2008) 1.81

A phase 2 study of the farnesyltransferase inhibitor tipifarnib in poor-risk and elderly patients with previously untreated acute myelogenous leukemia. Blood (2006) 1.59

Inhibitors of Ras/Raf-1 interaction identified by two-hybrid screening revert Ras-dependent transformation phenotypes in human cancer cells. Proc Natl Acad Sci U S A (2002) 1.52

Farnesyl transferase inhibitors cause enhanced mitotic sensitivity to taxol and epothilones. Proc Natl Acad Sci U S A (1998) 1.35

Resistance of K-RasBV12 proteins to farnesyltransferase inhibitors in Rat1 cells. Proc Natl Acad Sci U S A (1996) 1.33

Cell growth inhibition by farnesyltransferase inhibitors is mediated by gain of geranylgeranylated RhoB. Mol Cell Biol (1999) 1.29

The synergistic combination of the farnesyl transferase inhibitor lonafarnib and paclitaxel enhances tubulin acetylation and requires a functional tubulin deacetylase. Cancer Res (2005) 1.28

Combinatorial modulation of protein prenylation. ACS Chem Biol (2007) 1.25

The crystal structure of human protein farnesyltransferase reveals the basis for inhibition by CaaX tetrapeptides and their mimetics. Proc Natl Acad Sci U S A (2001) 1.25

Phase I trial of tipifarnib in children with newly diagnosed intrinsic diffuse brainstem glioma. Neuro Oncol (2008) 1.15

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) 1.14

Outlier kinase expression by RNA sequencing as targets for precision therapy. Cancer Discov (2013) 1.13

Identification of novel peptide substrates for protein farnesyltransferase reveals two substrate classes with distinct sequence selectivities. J Mol Biol (2009) 1.13

Rho2 is a target of the farnesyltransferase Cpp1 and acts upstream of Pmk1 mitogen-activated protein kinase signaling in fission yeast. Mol Biol Cell (2006) 1.12

Effect of a farnesyl transferase inhibitor (R115777) on ductal carcinoma in situ of the breast in a human xenograft model and on breast and ovarian cancer cell growth in vitro and in vivo. Breast Cancer Res (2006) 1.09

Fast, hungry and unstable: finding the Achilles' heel of small-cell lung cancer. Trends Mol Med (2007) 1.08

CAAX-box protein, prenylation process and carcinogenesis. Am J Transl Res (2009) 1.07

Geranylgeranyltransferase I as a target for anti-cancer drugs. J Clin Invest (2007) 1.04

Loss of oncogenic ras expression does not correlate with loss of tumorigenicity in human cells. Proc Natl Acad Sci U S A (1996) 1.03

Targeting the RAS oncogene. Expert Opin Ther Targets (2013) 1.02

Targeting the protein prenyltransferases efficiently reduces tumor development in mice with K-RAS-induced lung cancer. Proc Natl Acad Sci U S A (2010) 1.02

Hematopoietic cell fate and the initiation of leukemic properties in primitive primary human cells are influenced by Ras activity and farnesyltransferase inhibition. Mol Cell Biol (2004) 1.00

Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections. Medchemcomm (2013) 0.97

Farnesyl protein transferase inhibitors and other therapies targeting the Ras signal transduction pathway. Invest New Drugs (1999) 0.95

Multi-institutional phase 2 study of the farnesyltransferase inhibitor tipifarnib (R115777) in patients with relapsed and refractory lymphomas. Blood (2011) 0.95

Farnesyltransferase inhibitors induce dramatic morphological changes of KNRK cells that are blocked by microtubule interfering agents. Proc Natl Acad Sci U S A (1998) 0.95

Manumycin A inhibits triple-negative breast cancer growth through LC3-mediated cytoplasmic vacuolation death. Cell Death Dis (2013) 0.94

Farnesyltransferase inhibitors induce cytochrome c release and caspase 3 activation preferentially in transformed cells. Proc Natl Acad Sci U S A (1998) 0.93

A novel role of farnesylation in targeting a mitotic checkpoint protein, human Spindly, to kinetochores. J Cell Biol (2015) 0.91

Farnesyltransferase inhibitors reverse taxane resistance. Cancer Res (2006) 0.90

Geranylgeranyl diphosphate depletion inhibits breast cancer cell migration. Invest New Drugs (2010) 0.88

Ras inhibition enhances autophagy, which partially protects cells from death. Oncotarget (2013) 0.88

Cytotoxicity of farnesyltransferase inhibitors in lymphoid cells mediated by MAPK pathway inhibition and Bim up-regulation. Blood (2011) 0.87

New targets for therapy in breast cancer: farnesyltransferase inhibitors. Breast Cancer Res (2004) 0.86

Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas. J Neurooncol (2011) 0.85

K-Ras-independent effects of the farnesyl transferase inhibitor L-744,832 on cyclin B1/Cdc2 kinase activity, G2/M cell cycle progression and apoptosis in human pancreatic ductal adenocarcinoma cells. Neoplasia (2000) 0.84

Unraveling the mechanism of the farnesyltransferase enzyme. J Biol Inorg Chem (2004) 0.84

Targeted therapies for pancreatic cancer. Br Med Bull (2008) 0.84

Measurement of protein farnesylation and geranylgeranylation in vitro, in cultured cells and in biopsies, and the effects of prenyl transferase inhibitors. Nat Protoc (2011) 0.84

Farnesyl transferase expression determines clinical response to the docetaxel-lonafarnib combination in patients with advanced malignancies. Cancer (2011) 0.83

Photochemical modulation of Ras-mediated signal transduction using caged farnesyltransferase inhibitors: activation by one- and two-photon excitation. Chembiochem (2012) 0.83

Promotion of tumor development in prostate cancer by progerin. Cancer Cell Int (2010) 0.82

Transformation by Hras(G12V) is consistently associated with mutant allele copy gains and is reversed by farnesyl transferase inhibition. Oncogene (2013) 0.82

Substrate specificity determinants in the farnesyltransferase beta-subunit. Proc Natl Acad Sci U S A (1997) 0.82

Mechanisms of Chromosome Congression during Mitosis. Biology (Basel) (2017) 0.82

Phase II trial of R115777 (NSC #70818) in patients with advanced colorectal cancer: a Southwest Oncology Group study. Invest New Drugs (2006) 0.81

Phase I and pharmacological study of the farnesyltransferase inhibitor tipifarnib (Zarnestra, R115777) in combination with gemcitabine and cisplatin in patients with advanced solid tumours. Br J Cancer (2005) 0.81

Ras inhibition enhances autophagy, which partially protects cells from death. Oncotarget (2013) 0.80

Working together: Farnesyl transferase inhibitors and statins block protein prenylation. Mol Cell Pharmacol (2009) 0.79

A yeast-based genomic strategy highlights the cell protein networks altered by FTase inhibitor peptidomimetics. Mol Cancer (2010) 0.79

Activated Ras as a Therapeutic Target: Constraints on Directly Targeting Ras Isoforms and Wild-Type versus Mutated Proteins. ISRN Oncol (2013) 0.78

Combined p21-activated kinase and farnesyltransferase inhibitor treatment exhibits enhanced anti-proliferative activity on melanoma, colon and lung cancer cell lines. Mol Cancer (2013) 0.78

Farnesyl transferase inhibitors induce extended remissions in transgenic mice with mature B cell lymphomas. Mol Cancer (2008) 0.78

Manumycin and gliotoxin derivative KT7595 block Ras farnesylation and cell growth but do not disturb lamin farnesylation and localization in human tumour cells. Br J Cancer (1997) 0.77

Drug interactions of paclitaxel and docetaxel and their relevance for the design of combination therapy. Invest New Drugs (2001) 0.77

Small molecule inhibitors in acute myeloid leukemia: from the bench to the clinic. Expert Rev Hematol (2014) 0.76

8-Hydroxyquinoline-based inhibitors of the Rce1 protease disrupt Ras membrane localization in human cells. Bioorg Med Chem (2015) 0.76

Millepachine, a potential topoisomerase II inhibitor induces apoptosis via activation of NF-κB pathway in ovarian cancer. Oncotarget (2016) 0.75

Use of molecular studies for treatment of metastatic pleomorphic large cell pancreatic cancers-a novel strategy. J Gastrointest Oncol (2016) 0.75

Articles by these authors

Helper-independent transformation by unintegrated Harvey sarcoma virus DNA. J Virol (1978) 7.75

Cloning of the gene and cDNA for mammalian beta-adrenergic receptor and homology with rhodopsin. Nature (1986) 7.06

Intrinsic GTPase activity distinguishes normal and oncogenic ras p21 molecules. Proc Natl Acad Sci U S A (1984) 6.45

Crystal structure of an Hsp90-geldanamycin complex: targeting of a protein chaperone by an antitumor agent. Cell (1997) 5.73

Cloning of bovine GAP and its interaction with oncogenic ras p21. Nature (1988) 5.56

Studies on the nucleic acid sequences of Kirsten sarcoma virus: a model for formation of a mammalian RNA-containing sarcoma virus. J Virol (1973) 5.28

Cellular origin and role of mink cell focus-forming viruses in murine thymic lymphomas. Nature (1982) 5.23

Molecular cloning of infectious integrated murine leukemia virus DNA from infected mouse cells. Proc Natl Acad Sci U S A (1980) 4.71

Origin of mink cytopathic focus-forming (MCF) viruses:comparison with ecotropic and xenotropic murine leukemia virus genomes. Virology (1981) 4.62

PDGF induction of tyrosine phosphorylation of GTPase activating protein. Nature (1989) 4.36

Structure of endogenous murine leukemia virus DNA in mouse genomes. Proc Natl Acad Sci U S A (1980) 4.24

Tumors secreting human TNF/cachectin induce cachexia in mice. Cell (1987) 4.19

Transposition and amplification of oncogene-related sequences in human neuroblastomas. Cell (1983) 4.13

Long terminal repeat of murine retroviral DNAs: sequence analysis, host-proviral junctions, and preintegration site. J Virol (1982) 4.06

PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancer. Oncogene (2011) 3.59

Mutant ras-encoded proteins with altered nucleotide binding exert dominant biological effects. Proc Natl Acad Sci U S A (1986) 3.59

Differential expression of myc family genes during murine development. Nature (1986) 3.57

Multiferroic BaTiO3-CoFe2O4 Nanostructures. Science (2004) 3.49

Human N-myc is closely related in organization and nucleotide sequence to c-myc. Nature (1986) 3.40

RNA-dependent DNA polymerase activity in five RNA viruses: divalent cation requirements. Proc Natl Acad Sci U S A (1970) 3.25

Cyclin D expression is controlled post-transcriptionally via a phosphatidylinositol 3-kinase/Akt-dependent pathway. J Biol Chem (1998) 3.25

Cloning of cDNAs for cellular proteins that bind to the retinoblastoma gene product. Nature (1991) 3.20

Identification of effector residues and a neutralizing epitope of Ha-ras-encoded p21. Proc Natl Acad Sci U S A (1986) 3.11

Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature (1990) 3.11

Sequence dependence of protein isoprenylation. J Biol Chem (1991) 3.10

Conserved aspartic acid residues 79 and 113 of the beta-adrenergic receptor have different roles in receptor function. J Biol Chem (1988) 3.10

Molecular analysis of the envelope gene and long terminal repeat of Friend mink cell focus-inducing virus: implications for the functions of these sequences. J Virol (1984) 3.09

S. cerevisiae genes IRA1 and IRA2 encode proteins that may be functionally equivalent to mammalian ras GTPase activating protein. Cell (1990) 3.09

Friend murine leukemia virus-induced leukemia is associated with the formation of mink cell focus-inducing viruses and is blocked in mice expressing endogenous mink cell focus-inducing xenotropic viral envelope genes. J Exp Med (1981) 3.03

The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res (2001) 3.02

Minocycline prevents nigrostriatal dopaminergic neurodegeneration in the MPTP model of Parkinson's disease. Proc Natl Acad Sci U S A (2001) 2.95

V600E B-Raf requires the Hsp90 chaperone for stability and is degraded in response to Hsp90 inhibitors. Proc Natl Acad Sci U S A (2005) 2.93

Pharmacologic shifting of a balance between protein refolding and degradation mediated by Hsp90. Proc Natl Acad Sci U S A (1996) 2.90

Yeast and mammalian ras proteins have conserved biochemical properties. Nature (1985) 2.85

Identification of residues required for ligand binding to the beta-adrenergic receptor. Proc Natl Acad Sci U S A (1987) 2.81

Anaplastic lymphoma kinase (ALK) expression in the inflammatory myofibroblastic tumor: a comparative immunohistochemical study. Am J Surg Pathol (2001) 2.80

Ligand binding to the beta-adrenergic receptor involves its rhodopsin-like core. Nature (1987) 2.73

CDC25: a component of the RAS-adenylate cyclase pathway in Saccharomyces cerevisiae. Science (1987) 2.67

Selective inhibition of ras-dependent transformation by a farnesyltransferase inhibitor. Science (1993) 2.60

Activated expression of the N-myc gene in human neuroblastomas and related tumors. Science (1984) 2.46

Biomarker risk assessment and bladder cancer detection in a cohort exposed to benzidine. J Natl Cancer Inst (2001) 2.41

Structural features required for ligand binding to the beta-adrenergic receptor. EMBO J (1987) 2.41

Structure and expression of the murine N-myc gene. Proc Natl Acad Sci U S A (1986) 2.36

Modulation of Hsp90 function by ansamycins sensitizes breast cancer cells to chemotherapy-induced apoptosis in an RB- and schedule-dependent manner. See: E. A. Sausville, Combining cytotoxics and 17-allylamino, 17-demethoxygeldanamycin: sequence and tumor biology matters, Clin. Cancer Res., 7: 2155-2158, 2001. Clin Cancer Res (2001) 2.35

Cloning and characterization of E2F-2, a novel protein with the biochemical properties of transcription factor E2F. Mol Cell Biol (1993) 2.34

N-myc can cooperate with ras to transform normal cells in culture. Proc Natl Acad Sci U S A (1985) 2.33

Restriction endonuclease mapping of ecotropic murine leukemia viral DNAs: size and sequence heterogeneity of the long terminal repeat. Virology (1981) 2.25

Characterization of the retinoblastoma binding proteins RBP1 and RBP2. Oncogene (1993) 2.20

Suppressors of the ras2 mutation of Saccharomyces cerevisiae. Genetics (1986) 2.15

A C-terminal domain of GAP is sufficient to stimulate ras p21 GTPase activity. EMBO J (1989) 2.14

The histone deacetylase inhibitor suberoylanilide hydroxamic acid induces differentiation of human breast cancer cells. Cancer Res (2001) 2.08

A study of sexual behavior among rural residents of China. J Acquir Immune Defic Syndr Hum Retrovirol (1998) 2.02

Herbimycin A induces the 20 S proteasome- and ubiquitin-dependent degradation of receptor tyrosine kinases. J Biol Chem (1995) 1.98

Survival of retinoblastoma in less-developed countries impact of socioeconomic and health-related indicators. Br J Ophthalmol (2010) 1.98

Kinase-deficient Pak1 mutants inhibit Ras transformation of Rat-1 fibroblasts. Mol Cell Biol (1997) 1.94

Species identification and subtyping of Ureaplasma parvum and Ureaplasma urealyticum using PCR-based assays. J Clin Microbiol (2000) 1.94

Activation of pp60c-src protein kinase activity in human colon carcinoma. Proc Natl Acad Sci U S A (1987) 1.92

Age-related changes in human lens crystallins identified by two-dimensional electrophoresis and mass spectrometry. Exp Eye Res (1998) 1.88

Sequence analysis of betaA3, betaB3, and betaA4 crystallins completes the identification of the major proteins in young human lens. J Biol Chem (1997) 1.84

The ras oncogene--an important regulatory element in lower eucaryotic organisms. Microbiol Rev (1989) 1.79

Identification of guanine nucleotides bound to ras-encoded proteins in growing yeast cells. J Biol Chem (1987) 1.74

Subgenomic fragment of molecular cloned Friend murine leukemia virus DNA contains the gene(s) responsible for Friend murine leukemia virus-induced disease. J Virol (1980) 1.73

Fusion of the ALK gene to the clathrin heavy chain gene, CLTC, in inflammatory myofibroblastic tumor. Am J Pathol (2001) 1.72

Gamma-S crystallin gene (CRYGS) mutation causes dominant progressive cortical cataract in humans. J Med Genet (2005) 1.68

Autophosphorylation of v-Ha-ras p21 is modulated by amino acid residue 12. Proc Natl Acad Sci U S A (1984) 1.68

Polyisoprenylation of Ras in vitro by a farnesyl-protein transferase. J Biol Chem (1990) 1.68

Analysis of pp60c-src protein kinase activity in human tumor cell lines and tissues. J Biol Chem (1986) 1.67

Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic. Cell (1994) 1.67

Analysis of insulin-like growth factor I gene expression in malignancy: evidence for a paracrine role in human breast cancer. Mol Endocrinol (1989) 1.65

Protein domains governing interactions between E2F, the retinoblastoma gene product, and human papillomavirus type 16 E7 protein. Mol Cell Biol (1993) 1.64

Dominant inhibitory Ras mutants selectively inhibit the activity of either cellular or oncogenic Ras. Mol Cell Biol (1991) 1.62

Isolation of transplantable erythroleukemia cells from mice infected with helper-independent Friend murine leukemia virus. Blood (1981) 1.61

Apoptosis induced by an anti-epidermal growth factor receptor monoclonal antibody in a human colorectal carcinoma cell line and its delay by insulin. J Clin Invest (1995) 1.61

Rapid detection of mycoplasma-infected cell cultures. Exp Cell Res (1971) 1.59

Insulin-like growth factor receptor expression and function in human breast cancer. Cancer Res (1990) 1.57

Preferential inhibition of the oncogenic form of RasH by mutations in the GAP binding/"effector" domain. Cell (1991) 1.57

Isolation of variants in phagocytosis of a macrophage-like continuous cell line. J Exp Med (1977) 1.54

Transcription factor E2F binds DNA as a heterodimer. Proc Natl Acad Sci U S A (1993) 1.53

A 2.4-kilobase-pair fragment of the Friend murine leukemia virus genome contains the sequences responsible for friend murine leukemia virus-induced erythroleukemia. J Virol (1983) 1.53

Expression of the lck tyrosine kinase gene in human colon carcinoma and other non-lymphoid human tumor cell lines. Oncogene Res (1988) 1.53

Increased pp60c-src tyrosyl kinase activity in human neuroblastomas is associated with amino-terminal tyrosine phosphorylation of the src gene product. Proc Natl Acad Sci U S A (1985) 1.52

Regulatory function of the Saccharomyces cerevisiae RAS C-terminus. Mol Cell Biol (1987) 1.51

Inhibition of Src kinases by a selective tyrosine kinase inhibitor causes mitotic arrest. Cancer Res (1999) 1.51

A truncated cyclin D1 gene encodes a stable mRNA in a human breast cancer cell line. Oncogene (1994) 1.51

Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells. Cancer Res (2001) 1.50

The strength of B cell immunity in female rhesus macaques is controlled by CD8+ T cells under the influence of ovarian steroid hormones. Clin Exp Immunol (2002) 1.50

A small molecule designed to bind to the adenine nucleotide pocket of Hsp90 causes Her2 degradation and the growth arrest and differentiation of breast cancer cells. Chem Biol (2001) 1.49

Phylogenetic analysis of Ureaplasma urealyticum--support for the establishment of a new species, Ureaplasma parvum. Int J Syst Bacteriol (1999) 1.49

Isolation of amplified and overexpressed DNA sequences from adriamycin-resistant human breast cancer cells. Cancer Res (1987) 1.49

The envelope gene and long terminal repeat sequences contribute to the pathogenic phenotype of helper-independent Friend viruses. J Virol (1984) 1.48

Inhibitors of HSP90 block p95-HER2 signaling in Trastuzumab-resistant tumors and suppress their growth. Oncogene (2009) 1.48

Studies of the novel ketolide ABT-773: transport, binding to ribosomes, and inhibition of protein synthesis in Streptococcus pneumoniae. Antimicrob Agents Chemother (2000) 1.47

Inhibition of the ras p21 GTPase-activating protein-stimulated GTPase activity of c-Ha-ras p21 by smg p21 having the same putative effector domain as ras p21s. J Biol Chem (1990) 1.47

Evaluation of farnesyl:protein transferase and geranylgeranyl:protein transferase inhibitor combinations in preclinical models. Cancer Res (2001) 1.46

Inhibition of v-src-induced transformation by a GTPase-activating protein. Mol Cell Biol (1991) 1.46