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Disease on EC 2.5.1.58 - protein farnesyltransferase

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DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Adenocarcinoma
Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice.
Adenocarcinoma of Lung
Inhibition of farnesyl protein transferase by monoterpene, curcumin derivatives and gallotannin.
Bone Diseases
Clinical Trial of the Protein Farnesylation Inhibitors Lonafarnib, Pravastatin, and Zoledronic Acid in Children With Hutchinson-Gilford Progeria Syndrome.
Survey of plasma proteins in children with progeria pre-therapy and on-therapy with lonafarnib.
Breast Neoplasms
Inhibition of farnesyl protein transferase sensitizes human MCF-7 breast cancer cells to roscovitine-mediated cell cycle arrest.
Preclinical antitumor activity and pharmacodynamic studies with the farnesyl protein transferase inhibitor R115777 in human breast cancer.
The use of molecular markers in farnesyltransferase inhibitor (FTI) therapy of breast cancer.
Carcinogenesis
Crystallographic analysis of CaaX prenyltransferases complexed with substrates defines rules of protein substrate selectivity.
Inhibitors of farnesyl protein transferase and MEK1,2 induce apoptosis in fibroblasts transformed with farnesylated but not geranylgeranylated H-Ras.
Prediction and evaluation of protein farnesyltransferase inhibition by commercial drugs.
Structure of protein geranylgeranyltransferase-I from the human pathogen Candida albicans complexed with a lipid substrate.
Targeting the protein prenyltransferases efficiently reduces tumor development in mice with K-RAS-induced lung cancer.
Carcinoma
Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice.
Effects of SCH 59228, an orally bioavailable farnesyl protein transferase inhibitor, on the growth of oncogene-transformed fibroblasts and a human colon carcinoma xenograft in nude mice.
K- and N-Ras are geranylgeranylated in cells treated with farnesyl protein transferase inhibitors.
Manumycin and gliotoxin derivative KT7595 block Ras farnesylation and cell growth but do not disturb lamin farnesylation and localization in human tumour cells.
Selective cytotoxicity of farnesylamine to pancreatic carcinoma cells and Ki-ras-transformed fibroblasts.
Carcinoma, Hepatocellular
Inhibition of cell growth of human hepatoma cell line (Hep G2) by a farnesyl protein transferase inhibitor: a preferential suppression of ras farnesylation.
Manumycin and gliotoxin derivative KT7595 block Ras farnesylation and cell growth but do not disturb lamin farnesylation and localization in human tumour cells.
Chagas Disease
The protein farnesyltransferase inhibitor Tipifarnib as a new lead for the development of drugs against Chagas disease.
Colonic Neoplasms
Establishment and characterization of acquired resistance to the farnesyl protein transferase inhibitor R115777 in a human colon cancer cell line.
Relationship between flavonoid structure and inhibition of farnesyl protein transferase.
Colorectal Neoplasms
A phase II trial of farnesyl protein transferase inhibitor SCH 66336, given by twice-daily oral administration, in patients with metastatic colorectal cancer refractory to 5-fluorouracil and irinotecan.
Corneal Opacity
Inhibition of corneal inflammation by the topical use of Ras farnesyltransferase inhibitors: selective inhibition of macrophage localization.
Hematologic Neoplasms
Anti-inflammatory activity in vitro and in vivo of the protein farnesyltransferase inhibitor tipifarnib.
Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice.
Cancer therapy. New strategies and treatment modalities for optimizing patient outcomes.
Characterization of a human carcinoma cell line selected for resistance to the farnesyl transferase inhibitor 4-(2-(4-(8-chloro-3,10-dibromo-6,11-dihydro-5H-benzo-(5,6)-cyclohepta(1,2-b)-pyridin-11(R)-yl)-1-piperidinyl)-2-oxo-ethyl)-1-piperidinecarboxamide (SCH66336).
Farnesyl protein transferase inhibitors as targeted therapies for hematologic malignancies.
Farnesyltransferase inhibitors in hematologic malignancies: new horizons in therapy.
Herpes Simplex
Peptidomimetic design.
Hypersensitivity
Heat-shock protein 40 is the key farnesylation target in meristem size control, abscisic acid signaling, and drought resistance.
Leukemia
Activity of the farnesyl protein transferase inhibitor SCH66336 against BCR/ABL-induced murine leukemia and primary cells from patients with chronic myeloid leukemia.
Stereochemistry-dependent inhibition of RAS farnesylation by farnesyl phosphonic acids.
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Activity of the farnesyl protein transferase inhibitor SCH66336 against BCR/ABL-induced murine leukemia and primary cells from patients with chronic myeloid leukemia.
Leukemia, Myeloid, Acute
The influence of farnesyl protein transferase inhibitor R115777 (Zarnestra) alone and in combination with purine nucleoside analogs on acute myeloid leukemia progenitors in vitro.
[Farnesyltransferase inhibitors: preliminary results in acute myeloid leukemia]
Lung Neoplasms
Combining an FPTase inhibitor with cisplatin facilitates induction of apoptosis in human A549 lung cancer cells.
Lymphoma
Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice.
Malaria
2-Oxo-tetrahydro-1,8-naphthyridines as selective inhibitors of malarial protein farnesyltransferase and as anti-malarials.
A Review on Plasmodium falciparum-Protein Farnesyltransferase Inhibitors as Antimalarial Drug Targets.
Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge.
Novel N-(4-Piperidinyl)benzamide antimalarials with mammalian protein farnesyltransferase inhibitory activity.
Protein farnesyl transferase inhibitors for the treatment of malaria and African trypanosomiasis.
Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
Protein prenyl transferase activities of Plasmodium falciparum.
Structure based binding between protein farnesyl transferase and PRL-PTP of malaria parasite: An interaction study of prenylation process in Plasmodium.
Medulloblastoma
Apoptosis of medulloblastoma cells in vitro follows inhibition of farnesylation using manumycin A.
Multiple Sclerosis
Inhibition of Rho GTPases with protein prenyltransferase inhibitors prevents leukocyte recruitment to the central nervous system and attenuates clinical signs of disease in an animal model of multiple sclerosis.
Neoplasm Metastasis
Targeting the protein prenyltransferases efficiently reduces tumor development in mice with K-RAS-induced lung cancer.
Neoplasms
2'-benzoyloxycinnamaldehyde induces apoptosis in human carcinoma via reactive oxygen species.
A peptidomimetic inhibitor of farnesyl:protein transferase blocks the anchorage-dependent and -independent growth of human tumor cell lines.
A phase I and pharmacological study of the farnesyl protein transferase inhibitor L-778,123 in patients with solid malignancies.
A phase I safety, pharmacological and biological study of the farnesyl protein transferase inhibitor, tipifarnib and capecitabine in advanced solid tumors.
A phase I safety, pharmacological, and biological study of the farnesyl protein transferase inhibitor, lonafarnib (SCH 663366), in combination with cisplatin and gemcitabine in patients with advanced solid tumors.
A Phase I trial of the farnesyl protein transferase inhibitor R115777 in combination with gemcitabine and cisplatin in patients with advanced cancer.
A phase I trial of the novel farnesyl protein transferase inhibitor, BMS-214662, in combination with paclitaxel and carboplatin in patients with advanced cancer.
Andrastins A-D, Penicillium roqueforti Metabolites consistently produced in blue-mold-ripened cheese.
Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice.
Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice.
Antitumor effect of the cinnamaldehyde derivative CB403 through the arrest of cell cycle progression in the G2/M phase.
Bioactive constituents and medicinal importance of genus Alnus.
Caged protein prenyltransferase substrates: tools for understanding protein prenylation.
Cancer therapy. New strategies and treatment modalities for optimizing patient outcomes.
Carcinogen and dietary lipid regulate ras expression and localization in rat colon without affecting farnesylation kinetics.
Characterization of a human carcinoma cell line selected for resistance to the farnesyl transferase inhibitor 4-(2-(4-(8-chloro-3,10-dibromo-6,11-dihydro-5H-benzo-(5,6)-cyclohepta(1,2-b)-pyridin-11(R)-yl)-1-piperidinyl)-2-oxo-ethyl)-1-piperidinecarboxamide (SCH66336).
Clavaric acid: a triterpenoid inhibitor of farnesyl-protein transferase from Clavariadelphus truncatus.
Combination therapy with the farnesyl protein transferase inhibitor SCH66336 and SCH58500 (p53 adenovirus) in preclinical cancer models.
Combining the farnesyltransferase inhibitor lonafarnib with paclitaxel results in enhanced growth inhibitory effects on human ovarian cancer models in vitro and in vivo.
Conformation of a novel tetrapeptide inhibitor NH2-D-Trp-D-Met-Phe(pCl)-Gla-NH2 bound to farnesyl-protein transferase.
Crystal structures of the anticancer clinical candidates R115777 (Tipifarnib) and BMS-214662 complexed with protein farnesyltransferase suggest a mechanism of FTI selectivity.
Current progress on farnesyl protein transferase inhibitors.
Cytotoxic farnesyl glycosides from Pittosporum pancheri.
Dietary fish oil inhibits the expression of farnesyl protein transferase and colon tumor development in rodents.
Enzyme-Driven Membrane-Targeted Chimeric Peptide for Enhanced Tumor Photodynamic Immunotherapy.
Evaluation of farnesyl:protein transferase and geranylgeranyl:protein transferase inhibitor combinations in preclinical models.
Farnesyl protein transferase and tumor cell growth inhibitory activities of lipiferolide isolated from Liriodendron tulipifera.
Farnesyl protein transferase inhibitors as potential cancer chemopreventives.
Farnesyl protein transferase inhibitors as targeted therapies for hematologic malignancies.
Farnesyl transferase inhibitors in myeloid disorders.
Farnesyl transferase inhibitors in myeloid malignancies.
Farnesyl: proteintransferase inhibitors as agents to inhibit tumor growth.
Farnesyltransferase inhibitors (FTIs) in myeloid malignancies.
Farnesyltransferase inhibitors alter the prenylation and growth-stimulating function of RhoB.
Farnesyltransferase inhibitors and anti-Ras therapy.
Farnesyltransferase inhibitors versus Ras inhibitors.
High-performance liquid chromatography/mass spectrometry characterization of Ki4B-Ras in PSN-1 cells treated with the prenyltransferase inhibitor L-778,123.
Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.
Inhibition of DNA synthesis by a farnesyltransferase inhibitor involves inhibition of the p70(s6k) pathway.
Inhibition of farnesyl protein transferase and P21ras memebrane association by d-limonene in human pancreas tumor cells in vitro.
Inhibition of farnesyl protein transferase by monoterpene, curcumin derivatives and gallotannin.
Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice.
Inhibition of protein farnesyltransferase: a possible mechanism of tumor prevention by dehydroepiandrosterone sulfate.
Inhibition of protein farnesyltransferase: a possible mechanism of tumor prevention for dehydroepiandrosterone sulfate.
Inhibition of RAS-targeted prenylation: protein farnesyl transferase inhibitors revisited.
Inhibitors of farnesyl protein transferase and MEK1,2 induce apoptosis in fibroblasts transformed with farnesylated but not geranylgeranylated H-Ras.
Inhibitors of farnesyl:protein transferase--a possible cancer chemotherapeutic.
Inhibitors of farnesylation of Ras from a microbial natural products screening program.
Inhibitors of prenyl transferases.
Inhibitors of protein farnesyltransferase as novel anticancer agents.
Lipophilic bisphosphonates as dual farnesyl/geranylgeranyl diphosphate synthase inhibitors: an X-ray and NMR investigation.
Manumycin A inhibits triple-negative breast cancer growth through LC3-mediated cytoplasmic vacuolation death.
Molecular dynamics analysis of a series of 22 potential farnesyltransferase substrates containing a CaaX-motif.
Mouse mammary tumor virus-Ki-rasB transgenic mice develop mammary carcinomas that can be growth-inhibited by a farnesyl:protein transferase inhibitor.
NMR studies of novel inhibitors bound to farnesyl-protein transferase.
Novel farnesol and geranylgeraniol analogues: A potential new class of anticancer agents directed against protein prenylation.
Phase I and pharmacokinetic study of farnesyl protein transferase inhibitor R115777 in advanced cancer.
Phase I clinical and pharmacologic study of chronic oral administration of the farnesyl protein transferase inhibitor R115777 in advanced cancer.
Phase I pharmacokinetic and pharmacodynamic study of the prenyl transferase inhibitor AZD3409 in patients with advanced cancer.
Potent, selective, and orally bioavailable tricyclic pyridyl acetamide N-oxide inhibitors of farnesyl protein transferase with enhanced in vivo antitumor activity.
Pre-clinical development of farnesyltransferase inhibitors.
Prevention of farnesylation of c-Ha-Ras protein enhances synergistically the cytotoxic action of doxorubicin in cycling but not in quiescent cells.
Protein farnesylation inhibitors cause donut-shaped cell nuclei attributable to a centrosome separation defect.
Protein farnesyltransferase in embryogenesis, adult homeostasis, and tumor development.
Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice.
Ras as a target in cancer therapy.
Ras farnesyltransferase inhibition: a novel and safe approach for cancer chemotherapy.
Relationship between flavonoid structure and inhibition of farnesyl protein transferase.
Scaffold-based analysis of nonpeptide oncogenic FTase inhibitors using multiple similarity matching, binding affinity scoring and enzyme inhibition assay.
Search for protein farnesyltransferase inhibitors of microbial origin: our strategy and results as well as the results obtained by other groups.
Selective inhibition of ras-dependent transformation by a farnesyltransferase inhibitor.
Synergy of the protein farnesyltransferase inhibitor SCH66336 and cisplatin in human cancer cell lines.
Synthesis and biological evaluation of dimeric cinnamaldehydes as potent antitumor agents.
The potential of farnesyltransferase inhibitors as cancer chemotherapeutics.
Neuroblastoma
Inhibition of farnesyl-protein-transferase in neuroblastoma cells by alpha-hydroxyfarnesylphosphonate.
Neuroblastoma: inhibition of progression (Part II). Basic science in pediatric surgery.
Pancreatic Neoplasms
Inhibition of farnesyl protein transferase by monoterpene, curcumin derivatives and gallotannin.
Modified radiosensitivity of pancreatic cancer xenografts by farnesyl protein transferase inhibitor and MEK inhibitor.
Parasitic Diseases
Thematic review series: Lipid Posttranslational Modifications. Fighting parasitic disease by blocking protein farnesylation.
Towards the synthesis of bisubstrate inhibitors of protein farnesyltransferase: Synthesis and biological evaluation of new farnesylpyrophosphate analogues.
Progeria
A protein farnesyltransferase inhibitor ameliorates disease in a mouse model of progeria.
Assessing the efficacy of protein farnesyltransferase inhibitors in mouse models of progeria.
Blocking protein farnesyltransferase improves nuclear blebbing in mouse fibroblasts with a targeted Hutchinson-Gilford progeria syndrome mutation.
Protein farnesyltransferase inhibitors and progeria.
Targeting protein prenylation in progeria.
Reperfusion Injury
FPTIII mitigates peroxisome-mediated oxidative stress in kidneys of spontaneously hypertensive diabetic rats.
Trypanosomiasis, African
Cloning, heterologous expression, and distinct substrate specificity of protein farnesyltransferase from Trypanosoma brucei.
Isothiazole dioxides: synthesis and inhibition of Trypanosoma brucei protein farnesyltransferase.
Protein farnesyl transferase inhibitors for the treatment of malaria and African trypanosomiasis.
Vasospasm, Intracranial
Potential role of Ras in cerebral vasospasm after experimental subarachnoid hemorrhage in rabbits.
Whooping Cough
Activation of a Ca2+-dependent K+ current in mouse fibroblasts by lysophosphatidic acid requires a pertussis toxin-sensitive G protein and Ras.
The CB(1) cannabinoid receptor is coupled to the activation of c-Jun N-terminal kinase.