Farnesyl Protein Transferase Inhibitors and Other Therapies Targeting the Ras Signal Transduction Pathway

Calcium's Role in Mechanotransduction during Muscle Development

2014 • 14,293 citations

Genetic Alterations during Colorectal-Tumor Development

1988 • 6,691 citations

ras GENES

1987 • 3,818 citations

The MAPK signaling cascade

1995 • 3,300 citations

Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase

1998 • 3,026 citations

A synthetic inhibitor of the mitogen-activated protein kinase cascade.

1995 • 2,723 citations

Most human carcinomas of the exocrine pancreas contain mutant c-K-ras genes

1988 • 2,121 citations

SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin‐1

1995 • 2,080 citations

Activation of MAP kinase kinase is necessary and sufficient for PC12 differentiation and for transformation of NIH 3T3 cells

1994 • 1,999 citations

All ras proteins are polyisoprenylated but only some are palmitoylated

1989 • 1,806 citations

Transformation of Mammalian Cells by Constitutively Active MAP Kinase Kinase

1994 • 1,370 citations

Raf-1 activates MAP kinase-kinase

1992 • 1,308 citations

Association of Sos Ras exchange protein with Grb2 is implicated in tyrosine kinase signal transduction and transformation

1993 • 1,236 citations

A Cytoplasmic Protein Stimulates Normal N- ras p21 GTPase, But Does Not Affect Oncogenic Mutants

1987 • 1,197 citations

Detection of high incidence of K-ras oncogenes during human colon tumorigenesis

1987 • 1,074 citations

Increasing complexity of Ras signaling

1998 • 1,069 citations

Complexes of Ras⋅GTP with Raf-1 and Mitogen-Activated Protein Kinase Kinase

1993 • 987 citations

The GAP-related domain of the neurofibromatosis type 1 gene product interacts with ras p21

1990 • 984 citations

Activation of Raf as a Result of Recruitment to the Plasma Membrane

1994 • 979 citations

Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo

1999 • 970 citations

Human EJ bladder carcinoma oncogene is homologue of Harvey sarcoma virus ras gene

1982 • 928 citations

K- and N-Ras Are Geranylgeranylated in Cells Treated with Farnesyl Protein Transferase Inhibitors

1997 • 848 citations

Inhibition of purified p21ras farnesyl:protein transferase by Cys-AAX tetrapeptides

1990 • 815 citations

Rho, Rac and Cdc42 GTPases regulate the organization of the actin cytoskeleton

1997 • 802 citations

Growth factors induce nuclear translocation of MAP kinases (p42mapk and p44mapk) but not of their activator MAP kinase kinase (p45mapkk) in fibroblasts

1993 • 668 citations

Aberrant regulation of ras proteins in malignant tumour cells from type 1 neurofibromatosis patients

1992 • 648 citations

Benzodiazepine Peptidomimetics: Potent Inhibitors of Ras Farnesylation In Animal Cells

1993 • 631 citations

Altered Growth of Human Colon Cancer Cell Lines Disrupted at Activated Ki- ras

1993 • 627 citations

T24 human bladder carcinoma oncogene is an activated form of the normal human homologue of BALB- and Harvey-MSV transforming genes

1982 • 617 citations

Intrinsic GTPase activity distinguishes normal and oncogenic ras p21 molecules.

1984 • 607 citations

Selective Inhibition of ras -Dependent Transformation by a Farnesyltransferase Inhibitor

1993 • 578 citations

Isoprenoid addition to Ras protein is the critical modification for its membrane association and transforming activity.

1992 • 542 citations

Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice

1995 • 533 citations

Posttranslational modification of proteins by isoprenoids in mammalian cells

1990 • 515 citations

Post-translational processing of p21ras is two-step and involves carboxyl-methylation and carboxy-terminal proteolysis.

1989 • 462 citations

Ras C-terminal processing enzymes—New drug targets?

1991 • 461 citations

Antitumor activity of a phosphorothioate antisense oligodeoxynucleotide targeted against C-raf kinase

1996 • 444 citations

Extracellular signals and reversible protein phosphorylation: What to Mek of it all

1993 • 426 citations

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

1995 • 393 citations

Protein farnesyltransferase and geranylgeranyltransferase share a common α subunit

1991 • 371 citations

Direct Demonstration of Geranylgeranylation and Farnesylation of Ki-Ras in Vivo

1997 • 361 citations

Microtubule-associated protein 2 kinases, ERK1 and ERK2, undergo autophosphorylation on both tyrosine and threonine residues: implications for their mechanism of activation.

1991 • 344 citations

Farnesol modification of Kirsten-ras exon 4B protein is essential for transformation.

1990 • 333 citations

Crystal Structure of Protein Farnesyltransferase at 2.25 Angstrom Resolution

1997 • 328 citations

Rab geranylgeranyl transferase. A multisubunit enzyme that prenylates GTP-binding proteins terminating in Cys-X-Cys or Cys-Cys.

1992 • 323 citations

Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice.

1998 • 314 citations

Purification of component A of Rab geranylgeranyl transferase: Possible identity with the choroideremia gene product

1992 • 296 citations

High frequency of Ki‐ras codon 12 mutations in pancreatic adenocarcinomas

1989 • 295 citations

Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice.

1994 • 287 citations

Polylysine and CVIM Sequences of K-RasB Dictate Specificity of Prenylation and Confer Resistance to Benzodiazepine Peptidomimetic in Vitro

1995 • 285 citations

Selective inhibition of mutant Ha-ras mRNA expression by antisense oligonucleotides.

1992 • 257 citations

Purification of ras GTPase activating protein from bovine brain.

1988 • 255 citations

Cell Growth Inhibition by Farnesyltransferase Inhibitors Is Mediated by Gain of Geranylgeranylated RhoB

1999 • 255 citations

Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956.

1995 • 241 citations

Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts

1998 • 229 citations

Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion.

1995 • 226 citations

Peptidomimetic inhibitors of Ras farnesylation and function in whole cells.

1993 • 222 citations

Farnesyltransferase Inhibitors Alter the Prenylation and Growth-stimulating Function of RhoB

1997 • 214 citations

p21ras activation via hemopoietin receptors and c-kit requires tyrosine kinase activity but not tyrosine phosphorylation of p21ras GTPase-activating protein.

1992 • 213 citations

Limonene-induced regression of mammary carcinomas.

1992 • 210 citations

Structure and biological activity of human homologs of the raf/mil oncogene.

1985 • 203 citations

The effect of Mg2+ on the guanine nucleotide exchange rate of p21N-ras.

1986 • 203 citations

Specific inhibition of K-ras expression and tumorigenicity of lung cancer cells by antisense RNA

1991 • 188 citations

Oncogenic Ras activates c-Jun via a separate pathway from the activation of extracellular signal-regulated kinases.

1994 • 185 citations

Structure-activity relationships among monoterpene inhibitors of protein isoprenylation and cell proliferation

1994 • 182 citations

Disruption of Oncogenic K-Ras4B Processing and Signaling by a Potent Geranylgeranyltransferase I Inhibitor

1995 • 176 citations

Pharmacological effects of SB 220025, a selective inhibitor of P38 mitogen-activated protein kinase, in angiogenesis and chronic inflammatory disease models.

1998 • 172 citations

Antisense oligonucleotides adsorbed to polyalkylcyanoacrylate nanoparticles specifically inhibit mutated Ha-ras-mediated cell proliferation and tumorigenicity in nude mice.

1994 • 171 citations

Nonidentical subunits of p21H-ras farnesyltransferase. Peptide binding and farnesyl pyrophosphate carrier functions

1991 • 168 citations

Inhibition of DMBA-induced mammary cancer by the monoterpene d-limonene

1984 • 167 citations

Anti-carcinogenic activity of d-limonene during the initiation and promotion/progression stages of DMBA-induced rat mammary carcinogenesis

1988 • 164 citations

Prevention of orthotopic human lung cancer growth by intratracheal instillation of a retroviral antisense K-ras construct.

1993 • 162 citations

A dominant-negative mutant of raf blocks mitogen-activated protein kinase activation by growth factors and oncogenic p21ras.

1993 • 161 citations

Cloning and Characterization of a Mammalian Prenyl Protein-specific Protease

1999 • 161 citations

The inhibition of protein prenyltransferases by oxygenated metabolites of limonene and perillyl alcohol

1995 • 159 citations

Liposome-mediated in vivo gene transfer of antisense K-ras construct inhibits pancreatic tumor dissemination in the murine peritoneal cavity.

1995 • 152 citations

The farnesyltransferase inhibitor FTI-277 radiosensitizes H-ras-transformed rat embryo fibroblasts.

1996 • 150 citations

Evidence for a Catalytic Role of Zinc in Protein Farnesyltransferase

1997 • 148 citations

The prevention of nitrosomethylurea-induced mammary tumors by d-limonene and orange oil

1989 • 145 citations

GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells.

1997 • 139 citations

p21^WAF1/CIP1 Is Upregulated by the Geranylgeranyltransferase I Inhibitor GGTI-298 through a Transforming Growth Factor β- and Sp1-Responsive Element: Involvement of the Small GTPase RhoA

1998 • 138 citations

Mammalian Protein Geranylgeranyltransferase-I: Substrate Specificity, Kinetic Mechanism, Metal Requirements, and Affinity Labeling

1995 • 122 citations

Phase I clinical trial of perillyl alcohol administered daily.

1998 • 116 citations

Mutation of H-ras is infrequent in bladder cancer: confirmation by single-strand conformation polymorphism analysis, designed restriction fragment length polymorphisms, and direct sequencing.

1993 • 114 citations

Differential Effects of Monoterpenes and Lovastatin on RAS Processing

1995 • 105 citations

Antisense inhibition of ras p21 expression that is sensitive to a point mutation

1991 • 104 citations

Activation of the transforming growth factor beta signaling pathway and induction of cytostasis and apoptosis in mammary carcinomas treated with the anticancer agent perillyl alcohol.

1999 • 103 citations

Isoprenoid diphosphate utilization by recombinant human farnesyl:protein transferase: Interactive binding between substrates and a preferred kinetic pathway

1993 • 94 citations

Effects of anticarcinogenic monoterpenes on phase II hepatic metabolizing enzymes

1993 • 92 citations

H-Ras Peptide and Protein Substrates Bind Protein Farnesyltransferase as an Ionized Thiolate

1998 • 91 citations

Tricyclic Farnesyl Protein Transferase Inhibitors: Crystallographic and Calorimetric Studies of Structure−Activity Relationships

1999 • 88 citations

Protein Farnesyltransferase: Structure and Implications for Substrate Binding

1998 • 86 citations

Inhibition of protein prenylation by metabolites of limonene

1999 • 84 citations

Inhibition of type I and type II geranylgeranyl-protein transferases by the monoterpene perillyl alcohol in NIH3T3 cells

1997 • 79 citations

Suppression of Ki-ras p21 levels leading to growth inhibition of pancreatic cancer cell lines with Ki-ras mutation but not those without Ki-ras mutation

1997 • 77 citations

Antisense DNA inhibition of tumor growth induced by c-Ha-ras oncogene in nude mice.

1993 • 74 citations

Activated protooncogenes in human lung tumors from smokers.

1991 • 73 citations

Abrogation of c-Raf expression induces apoptosis in tumor cells

1998 • 69 citations

Inhibition of ubiquinone and cholesterol synthesis by the monoterpene perillyl alcohol

1994 • 64 citations

The Geranylgeranyltransferase I Inhibitor GGTI-298 Induces Hypophosphorylation of Retinoblastoma and Partner Switching of Cyclin-dependent Kinase Inhibitors

1999 • 54 citations

Growth inhibitory effect of anti-K-ras adenovirus on lung cancer cells.

1996 • 52 citations

Antisense raf Oligodeoxyribonucleotide Is a Radiosensitizer In Vivo

1999 • 51 citations

Effects of the antitumor agent perillyl alcohol on H-Ras vs. K-Ras farnesylation and signal transduction in pancreatic cells.

1998 • 47 citations

Activation of mitogen-activated protein (MAP) kinase by a MAP kinase-kinase.

1992 • 40 citations

J-104,871, a Novel Farnesyltransferase Inhibitor, Blocks Ras FarnesylationIn Vivoin a Farnesyl Pyrophosphate-Competitive Manner

1998 • 39 citations

Modification of Mutant K-ras Gene Expression in Non-Small Cell Lung Cancer (NSCLC). University of Texas M.D. Anderson Cancer Center, Houston, Texas

1996 • 31 citations

Antisense therapy of cancer.

1994 • 10 citations

Antisense Tumor Therapy: Activated C-Ha-ras Oncogene in the Mouse

2003 • 3 citations