farnesyltransferase inhibitor

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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/06/22 07:49:44」(JST)

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  • (-)-Xanthatin Selectively Induces GADD45γ and Stimulates Caspase-Independent Cell Death in Human Breast Cancer MDA-MB-231 Cells.
  • Takeda S, Matsuo K, Yaji K, Okajima-Miyazaki S, Harada M, Miyoshi H, Okamoto Y, Amamoto T, Shindo M, Omiecinski CJ, Aramaki H.SourceDepartment of Molecular Biology, Daiichi University of Pharmacy , 22-1 Tamagawa-cho, Minami-ku, Fukuoka 815-8511, Japan.
  • Chemical research in toxicology.Chem Res Toxicol.2011 Jun 20;24(6):855-65. Epub 2011 May 13.
  • exo-Methylene lactone group-containing compounds, such as (-)-xanthatin, are present in a large variety of biologically active natural products, including extracts of Xanthium strumarium (Cocklebur). These substances are reported to possess diverse functional activities, exhibiting anti-inflammatory
  • PMID 21568272
  • Discovery and SAR of Methylated Tetrahydropyranyl Derivatives as Inhibitors of Isoprenylcysteine Carboxyl Methyltransferase (ICMT).
  • Judd WR, Slattum PM, Hoang KC, Bhoite L, Valppu L, Alberts G, Brown B, Roth B, Ostanin K, Huang L, Wettstein D, Richards B, Willardsen JA.AbstractA series of tetrahydropyranyl (THP) derivatives has been developed as potent inhibitors of isoprenylcysteine carboxyl methyltransferase (ICMT) for use as anticancer agents. Structural modification of the submicromolar hit compound 3, led to the potent 3-methoxy substituted analog 27. Further SAR development around the THP ring resulted in an additional 10-fold increase in potency, exemplified by analog 75 with an IC¬50 of 1.3 nM. Active and potent compounds demonstrated a dose-dependent increase in Ras cytosolic protein. Potent ICMT inhibitors also reduced cell viability in several cancer cell lines with growth inhibition (GI50) values ranging from 0.3 to >100 ?M. However, none of the cellular effects observed using ICMT inhibitors were as pronounced as those resulting from a farnesyltransferase inhibitor.
  • Journal of medicinal chemistry.J Med Chem.2011 Jun 10. [Epub ahead of print]
  • A series of tetrahydropyranyl (THP) derivatives has been developed as potent inhibitors of isoprenylcysteine carboxyl methyltransferase (ICMT) for use as anticancer agents. Structural modification of the submicromolar hit compound 3, led to the potent 3-methoxy substituted analog 27. Further SAR dev
  • PMID 21661760


  • Nobiletin Induces Inhibitions of Ras Activity and Mitogen-Activated Protein Kinase Kinase/Extracellular Signal-Regulated Kinase Signaling to Suppress Cell Proliferation in C6 Rat Glioma Cells
  • Aoki Koichi,Yokosuka Akihito,Mimaki Yoshihiro [他],Fukunaga Kohji,Yamakuni Tohru
  • Biological and Pharmaceutical Bulletin 36(4), 540-547, 2013
  • … Second, farnesyltransferase inhibitor I, a Ras inhibitor, and U0126, a MEK inhibitor, induced an inhibition of the cell proliferation in C6 cells, while the cell proliferation was inhibited by nobiletin as well. …
  • NAID 130003361386
  • Lysophosphatidylcholine Increases Na^+/Ca^<2+> Exchanger Expression via RhoB-Geranylgeranylation in H9c2 Cells
  • Maeda Sachiko,Sakamoto Kazuho,Matsuoka Isao [他],IWAMOTO Takahiro,KIMURA Junko
  • Journal of pharmacological sciences 109(4), 565-572, 2009-04-20
  • … Conversely, fluvastatin (Flv), a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, decreased NCX1 mRNA and protein expression by inhibiting RhoB. … Furthermore, geranylgeranyltransferase 1 inhibitor (GGTI), but not farnesyltransferase inhibitor (FTI), inhibited the LPC-induced NCX1 mRNA increase. …
  • NAID 10025735890
  • Isolation of a Fission Yeast Mutant Cell Affected in MAP Kinase Signaling and Sterol Biosynthesis
  • Imagawa Kiwamu,Fang Yue,Sugiura Reiko,Zhou Xin,Ma Yan,Kuno Takayoshi
  • The Kobe journal of the medical sciences 55(2), 30-35, 2009-04
  • … Consistently, thevic6 mutant cells exhibited hypersensitivity to miconazole, an inhibitor of ergosterolbiosynthesis and showed aberrant intracellular localization of filipin, suggesting thatthe mutant cells are affected in the sterol biosynthesis. … In addition, overexpression ofthe hmg1+ gene complemented the phenotype of vic1-1/cpp1-v1 mutant cells, an allele ofthe gene encoding a farnesyltransferase, whereas overexpression of the cpp1+ geneexacerbated the temperature-sensitive phenotype of the vic6 mutant cells. …
  • NAID 120001478910


Abstract This article presents an overview of preclinical studies and clinical trials of a number of independently derived farnesyltransferase inhibitors (FTIs). Potential targets and biological modes of action of FTIs are ...






farnesyltransferase inhibitor



farnesyltransferase inhibitor



farnesyltransferase inhibitor



farnesyltransferase inhibitor



  • v.
  • 抑制する、阻害する、阻止する

WordNet   license wordnet

「limit, block, or decrease the action or function of; "inhibit the action of the enzyme"; "inhibit the rate of a chemical reaction"」

PrepTutorEJDIC   license prepejdic

「〈感情・欲望・行動・作用など〉‘を'抑制する / (…しないように)〈人〉‘を'抑制する,妨げる《+『名』+『from』+『名』(do『ing』)》」

WordNet   license wordnet

「control and refrain from showing; of emotions, desires, impulses, or behavior」
bottle up, suppress

WordNet   license wordnet

「limit the range or extent of; "Contact between the young was inhibited by strict social customs"」



  • n.

WordNet   license wordnet

「a substance that retards or stops an activity」

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「抑制する人(物) / 化学反応抑制剤」