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Farnesyltransferase inhibitors in breast cancer therapy.

Abstract
Farnesyltransferase inhibitors (FTIs) belong to a group of agents originally designed to prevent membrane attachment of Ras protein by inhibiting a key step in its post-translational processing. It was thus hypothesized that FTIs would curtail the oncogenic ras-mediated proliferative and antiapoptotic signals that are activated in human tumors. Although the Ras protein is mutated in only < 5% of breast cancers, there are multiple aberrant pathways that lead to activation of wild-type ras signaling. Moreover, FTIs have consistently demonstrated efficacy in tumors regardless of their ras mutational status. Thus, the role of other protein targets in mediating the antitumor effect of FTIs is being elucidated. This article reviews current data on the use of FTIs in breast cancer.
AuthorsGrace K Dy, Alex A Adjei
JournalCancer investigation (Cancer Invest) Vol. 20 Suppl 2 Pg. 30-7 ( 2002) ISSN: 0735-7907 [Print] England
PMID12442347 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
Chemical References
  • Enzyme Inhibitors
  • Neoplasm Proteins
  • Piperidines
  • Pyridines
  • Quinolones
  • Deoxycytidine
  • Capecitabine
  • Alkyl and Aryl Transferases
  • Farnesyltranstransferase
  • lonafarnib
  • tipifarnib
  • Paclitaxel
  • Fluorouracil
Topics
  • Alkyl and Aryl Transferases (antagonists & inhibitors, physiology)
  • Animals
  • Antineoplastic Combined Chemotherapy Protocols (therapeutic use)
  • Breast Neoplasms (drug therapy, enzymology)
  • Capecitabine
  • Clinical Trials as Topic
  • Deoxycytidine (administration & dosage, analogs & derivatives)
  • Drug Screening Assays, Antitumor
  • Drug Synergism
  • Enzyme Inhibitors (pharmacology, therapeutic use)
  • Farnesyltranstransferase
  • Female
  • Fluorouracil (analogs & derivatives)
  • Humans
  • Mice
  • Neoplasm Proteins (antagonists & inhibitors, physiology)
  • Paclitaxel (administration & dosage)
  • Piperidines (administration & dosage)
  • Protein Prenylation (drug effects)
  • Protein Processing, Post-Translational (drug effects)
  • Pyridines (administration & dosage)
  • Quinolones (administration & dosage)
  • Signal Transduction (drug effects)
  • Tumor Cells, Cultured (drug effects)
  • Xenograft Model Antitumor Assays

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