Farnesyltransferase inhibitors: targeting the molecular basis of cancer

FUNCTION AND REGULATION OF RAS

1993 • 1,161 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

Coexpression of MMTV/v-Ha-ras and MMTV/c-myc genes in transgenic mice: Synergistic action of oncogenes in vivo

1987 • 796 citations

Human Sos1: a Guanine Nucleotide Exchange Factor for Ras that Binds to GRB2

1993 • 788 citations

Benzodiazepine Peptidomimetics: Potent Inhibitors of Ras Farnesylation In Animal Cells

1993 • 631 citations

Sequence dependence of protein isoprenylation

1991 • 580 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

Bcr-Abl oncoproteins bind directly to activators of the Ras signalling pathway.

1994 • 454 citations

Localization of the src gene product of the Harvey strain of MSV to plasma membrane of transformed cells by electron microscopic immunocytochemistry

1980 • 404 citations

Harvey murine sarcoma virus p21 ras protein: biological and biochemical significance of the cysteine nearest the carboxy terminus.

1984 • 403 citations

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

1995 • 393 citations

Ras CAAX Peptidomimetic FTI-277 Selectively Blocks Oncogenic Ras Signaling by Inducing Cytoplasmic Accumulation of Inactive Ras-Raf Complexes

1995 • 359 citations

Guanine nucleotide-binding and autophosphorylating activities associated with the p21src protein of Harvey murine sarcoma virus

1980 • 356 citations

THE POTENTIAL OF FARNESYLTRANSFERASE INHIBITORS AS CANCER CHEMOTHERAPEUTICS

1997 • 329 citations

Crystal Structure of Protein Farnesyltransferase at 2.25 Angstrom Resolution

1997 • 328 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

Regulators and Effectors of ras Proteins

1991 • 303 citations

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

1994 • 287 citations

Farnesyltransferase inhibitors and cancer treatment: targeting simply Ras?

1997 • 271 citations

Alternative signals to RAS for hematopoietic transformation by the BCR-ABL oncogene

1995 • 261 citations

Selective inhibition of farnesyl-protein transferase blocks ras processing in vivo.

1993 • 257 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

Evidence that Farnesyltransferase Inhibitors Suppress Ras Transformation by Interfering with Rho Activity

1995 • 220 citations

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

1997 • 214 citations

Farnesyl transferase inhibitors cause enhanced mitotic sensitivity to taxol and epothilones

1998 • 212 citations

Characterization of Ha-Ras, N-Ras, Ki-Ras4A, and Ki-Ras4B as in Vitro Substrates for Farnesyl Protein Transferase and Geranylgeranyl Protein Transferase Type I

1997 • 203 citations

Farnesyltransferase Inhibition Causes Morphological Reversion of ras-Transformed Cells by a Complex Mechanism That Involves Regulation of the Actin Cytoskeleton

1994 • 197 citations

Inhibiting Ras prenylation increases the radiosensitivity of human tumor cell lines with activating mutations of ras oncogenes.

1998 • 191 citations

Farnesyl transferase inhibitors induce apoptosis of Ras-transformed cells denied substratum attachment.

1997 • 184 citations

Specific isoprenoid modification is required for function of normal, but not oncogenic, Ras protein.

1992 • 180 citations

A Farnesyltransferase Inhibitor Induces Tumor Regression in Transgenic Mice Harboring Multiple Oncogenic Mutations by Mediating Alterations in Both Cell Cycle Control and Apoptosis

1998 • 173 citations

cDNA cloning and expression of the peptide-binding β subunit of rat p21rasfarnesyltransferase, the counterpart of yeast DPR1/RAM1

1991 • 166 citations

Novel Tricyclic Inhibitors of Farnesyl Protein Transferase

1995 • 157 citations

Resistance of K-RasBV12 proteins to farnesyltransferase inhibitors in Rat1 cells.

1996 • 152 citations

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

1996 • 150 citations

Cocrystal Structure of Protein Farnesyltransferase Complexed with a Farnesyl Diphosphate Substrate^,

1998 • 148 citations

Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice.

1998 • 146 citations

Farnesyltransferase inhibition causes morphological reversion of ras-transformed cells by a complex mechanism that involves regulation of the actin cytoskeleton.

1994 • 142 citations

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

1997 • 139 citations

Characterization of recombinant human farnesyl-protein transferase: Cloning, expression, farnesyl diphosphate binding, and functional homology with yeast prenyl-protein transferases

1993 • 136 citations

Pharmaceutical research in molecular oncology

1994 • 134 citations

A Farnesyl-Protein Transferase Inhibitor Induces p21 Expression and G1 Block in p53 Wild Type Tumor Cells

1998 • 119 citations

The CAAX peptidomimetic compound B581 specifically blocks farnesylated, but not geranylgeranylated or myristylated, oncogenic ras signaling and transformation.

1994 • 113 citations

Pseudopeptide Inhibitors of Ras Farnesyl-Protein Transferase

1994 • 109 citations

Protein Farnesyltransferase: Structure and Implications for Substrate Binding

1998 • 86 citations

GTPase Activating Proteins

1993 • 64 citations

Inhibition of Growth and Invasive Activity of Human Pancreatic Cancer Cells by a Farnesyltransferase Inhibitor, Manumycin

1997 • 55 citations

Chaetomella acutiseta produces chaetomellic acids A and B which are reversible inhibitors of farnesyl-protien transferase

1993 • 52 citations

2-Substituted Piperazines as Constrained Amino Acids. Application to the Synthesis of Potent, Non Carboxylic Acid Inhibitors of Farnesyltransferase

1996 • 49 citations

Tumorigenesis and male sterility in transgenic mice expressing a MMTV/N-ras oncogene.

1990 • 47 citations

Potent and Selective Non-Cysteine-Containing Inhibitors of Protein Farnesyltransferase

1998 • 42 citations

NMR studies of novel inhibitors bound to farnesyl‐protein transferase

1995 • 42 citations

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

1998 • 39 citations

ras Proto-Oncogene Activation in Human Malignancy

1995 • 38 citations

Selective cytotoxicity of farnesylamine to pancreatic carcinoma cells and Ki-ras–transformed fibroblasts

1998 • 29 citations

N-Arylalkyl Pseudopeptide Inhibitors of Farnesyltransferase

1998 • 25 citations

[Growth inhibition of human pancreatic cancer by farnesyl transferase inhibitor].

1996 • 6 citations