Chapter 6 – Geranylgeranyltransferase-1 Inhibitors

No abstract is available for this paper.

• Publication year

  2011

• Venue

  The Enzymes

• Publication date

  2011-12-31

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/B978-0-12-415922-8.00006-9
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar

• No claims are published for this paper.

• No concepts are published for this paper.

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• Targeting protein prenylation for cancer therapy

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• A Tagging-via-substrate Approach to Detect the Farnesylated Proteome Using Two-dimensional Electrophoresis Coupled with Western Blotting*

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• Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents.

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• Evaluation of Alkyne‐Modified Isoprenoids as Chemical Reporters of Protein Prenylation

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• Dissecting the roles of DR4, DR5 and c-FLIP in the regulation of Geranylgeranyltransferase I inhibition-mediated augmentation of TRAIL-induced apoptosis

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• Discovery of geranylgeranyltransferase-I inhibitors with novel scaffolds by the means of quantitative structure-activity relationship modeling, virtual screening, and experimental validation.

  2009cited by this paper
• Analysis of the eukaryotic prenylome by isoprenoid affinity tagging.

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• In vivo antitumor effect of a novel inhibitor of protein geranylgeranyltransferase-I

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• Blockade of Protein Geranylgeranylation Inhibits Cdk2-Dependent p27Kip1 Phosphorylation on Thr187 and Accumulates p27Kip1 in the Nucleus: Implications for Breast Cancer Therapy

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• Caution! Analyze transcripts from conditional knockout alleles

  2009cited by this paper
• Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase.

  2009cited by this paper
• Inhibitors of Protein Geranylgeranyltransferase I and Rab Geranylgeranyltransferase Identified from a Library of Allenoate-derived Compounds*

  2008cited by this paper
• Protein geranylgeranyltransferase-I of Trypanosoma cruzi.

  2008cited by this paper
• Farnesyltransferase inhibitors: a detailed chemical view on an elusive biological problem.

  2008cited by this paper
• Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: structure-activity relationships of ethylenediamine-analogue scaffolds and homology model validation.

  2008cited by this paper
• Towards Complete Sets of Farnesylated and Geranylgeranylated Proteins

  2007cited by this paper
• GGTase-I deficiency reduces tumor formation and improves survival in mice with K-RAS-induced lung cancer.

  2007cited by this paper
• Geranylgeranyltransferase I Inhibitors Target RalB To Inhibit Anchorage-Dependent Growth and Induce Apoptosis and RalA To Inhibit Anchorage-Independent Growth

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• Protein isoprenylation in biology and disease: general overview and perspectives from studies with genetically engineered animals.

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• RhoA and RhoC -siRNA inhibit the proliferation and invasiveness activity of human gastric carcinoma by Rho/PI3K/Akt pathway.

  2007cited by this paper
• Structure-based design of imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase.

  2006cited by this paper
• Synthesis and evaluation of potent, highly-selective, 3-aryl-piperazinone inhibitors of protein geranylgeranyltransferase-I.

  2006cited by this paper
• Thematic review series: Lipid Posttranslational Modifications. Fighting parasitic disease by blocking protein farnesylation Published, JLR Papers in Press, December 7, 2005.

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• Thematic review series: Lipid Posttranslational Modifications. Farnesyl transferase inhibitors Published, JLR Papers in Press, November 8, 2005.

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• Targeted inhibition of farnesyltransferase in locally advanced breast cancer: a phase I and II trial of tipifarnib plus dose-dense doxorubicin and cyclophosphamide.

  2006cited by this paper
• Thematic review series: Lipid Posttranslational Modifications. Structural biology of protein farnesyltransferase and geranylgeranyltransferase type I Published, JLR Papers in Press, February 13, 2006.

  2006cited by this paper
• A Novel Protein Geranylgeranyltransferase-I Inhibitor with High Potency, Selectivity, and Cellular Activity*

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  2006cited by this paper
• Phase I and pharmacological study of the farnesyltransferase inhibitor tipifarnib (Zarnestra®, R115777) in combination with gemcitabine and cisplatin in patients with advanced solid tumours

  2005cited by this paper
• O-082 A randomized phase III trial comparing ionafarnib/carboplatin/paclitaxel versus carboplatin/paclitaxel (CP) in chemotherapy-naive patients with advanced or metastatic non-small cell lung cancer (NSCLC)

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• Protein farnesyltransferase in embryogenesis, adult homeostasis, and tumor development.

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• Tools to analyze protein farnesylation in cells

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• Protein farnesylation: implications for normal physiology, malignant transformation, and cancer therapy.

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• Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.

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• Anti-RhoA and anti-RhoC siRNAs inhibit the proliferation and invasiveness of MDA-MB-231 breast cancer cells in vitro and in vivo.

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• Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.

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• Protein Farnesyltransferase Inhibitor (SCH 66336) Abolishes NF-κB Activation Induced by Various Carcinogens and Inflammatory Stimuli Leading to Suppression of NF-κB-regulated Gene Expression and Up-regulation of Apoptosis*

  2004cited by this paper
• Phase III trial of gemcitabine plus tipifarnib compared with gemcitabine plus placebo in advanced pancreatic cancer.

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• Crystal structures of the anticancer clinical candidates R115777 (Tipifarnib) and BMS-214662 complexed with protein farnesyltransferase suggest a mechanism of FTI selectivity.

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• A tagging-via-substrate technology for detection and proteomics of farnesylated proteins.

  2004cited by this paper
• Inhibition of Farnesyltransferase Prevents Collagen-Induced Arthritis by Down-Regulation of Inflammatory Gene Expression through Suppression of p21ras-Dependent NF-κB Activation1

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• Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?

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• Phosphatidylinositol-3-OH kinase/AKT and survivin pathways as critical targets for geranylgeranyltransferase I inhibitor-induced apoptosis

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• Phase III double-blind placebo-controlled study of farnesyl transferase inhibitor R115777 in patients with refractory advanced colorectal cancer.

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• Crystallographic analysis of CaaX prenyltransferases complexed with substrates defines rules of protein substrate selectivity.

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• Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice.

  2003cited by this paper
• Searching for the elusive targets of farnesyltransferase inhibitors

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• Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase.

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• Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor.

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• A Phase I trial of the farnesyl protein transferase inhibitor R115777 in combination with gemcitabine and cisplatin in patients with advanced cancer.

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• Phase I clinical and pharmacologic study of chronic oral administration of the farnesyl protein transferase inhibitor R115777 in advanced cancer.

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• The farnesyltransferase inhibitor, FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status

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• Farnesylation of Cenp-F is required for G2/M progression and degradation after mitosis.

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• 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 Sclerosis1

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• Farnesyltransferase inhibitors reverse Ras-mediated inhibition of Fas gene expression.

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• Farnesylated RhoB Prevents Cell Cycle Arrest and Actin Cytoskeleton Disruption Caused by the Geranylgeranyltransferase I Inhibitor GGTI-298

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• Distinct requirements for Ras oncogenesis in human versus mouse cells.

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• The Farnesyltransferase Inhibitor, FTI-2153, Blocks Bipolar Spindle Formation and Chromosome Alignment and Causes Prometaphase Accumulation during Mitosis of Human Lung Cancer Cells*

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• Signaling events required for transforming growth factor-beta stimulation of connective tissue growth factor expression by cultured human lung fibroblasts.

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• Conformational restriction of flexible ligands guided by the transferred noe experiment: potent macrocyclic inhibitors of farnesyltransferase.

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• Anions Modulate the Potency of Geranylgeranyl-Protein Transferase I Inhibitors*

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• The crystal structure of human protein farnesyltransferase reveals the basis for inhibition by CaaX tetrapeptides and their mimetics

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• Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro.

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• Protein Geranylgeranylation Is Required for Osteoclast Formation, Function, and Survival: Inhibition by Bisphosphonates and GGTI‐298

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• Mouse mammary tumor virus-Ki-rasB transgenic mice develop mammary carcinomas that can be growth-inhibited by a farnesyl:protein transferase inhibitor.

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• TGF-beta1 stimulation of fibronectin transcription in cultured human lung fibroblasts requires active geranylgeranyl transferase I, phosphatidylcholine-specific phospholipase C, protein kinase C-delta, and p38, but not erk1/erk2.

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• Farnesyl Transferase Inhibitors Block the Farnesylation of CENP-E and CENP-F and Alter the Association of CENP-E with the Microtubules*

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• The Phosphoinositide 3-OH Kinase/AKT2 Pathway as a Critical Target for Farnesyltransferase Inhibitor-Induced Apoptosis

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• Protein Farnesylation Is Critical for Maintaining Normal Cell Morphology and Canavanine Resistance in Schizosaccharomyces pombe *

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

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• Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine.

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• Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.

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• Requirement for geranylgeranyl transferase I and acyl transferase in the TGF-beta-stimulated pathway leading to elastin mRNA stabilization.

  1998cited by this paper
• Chromatographic assay and peptide substrate characterization of partially purified farnesyl- and geranylgeranyltransferases from rat brain cytosol.

  1998cited by this paper
• Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice.

  1998cited by this paper
• Potent and selective non-cysteine-containing inhibitors of protein farnesyltransferase.

  1998cited by this paper
• N-Arylalkyl pseudopeptide inhibitors of farnesyltransferase.

  1998cited by this paper
• 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

  1998cited by this paper
• Inhibition of Protein Geranylgeranylation Causes a Superinduction of Nitric-oxide Synthase-2 by Interleukin-1β in Vascular Smooth Muscle Cells*

  1997cited by this paper
• Evidence for a Catalytic Role of Zinc in Protein Farnesyltransferase

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• Crystal Structure of Protein Farnesyltransferase at 2.25 Angstrom Resolution

  1997cited by this paper
• K- and N-Ras Are Geranylgeranylated in Cells Treated with Farnesyl Protein Transferase Inhibitors*

  1997cited by this paper
• Cdc42 regulates anchorage-independent growth and is necessary for Ras transformation

  1997cited by this paper
• 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

  1997cited by this paper

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