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Inhibitors of Ras farnesyltransferases

F Tamanoi1

  • 1Department of Microbiology and Molecular Genetics, University of California, Los Angeles 90024.

Trends in Biochemical Sciences
|September 1, 1993
PubMed

Insights

Farnesyltransferase inhibitors, identified from natural compounds and substrate analogues, show promise for blocking Ras proteins and understanding cholesterol metabolism.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Farnesyltransferase is an enzyme crucial for post-translational modification of proteins.
  • It utilizes farnesylpyrophosphate, a cholesterol precursor, in its catalytic process.
  • The Ras oncogene product is a known substrate for farnesyltransferase.

Purpose of the Study:

  • To identify and characterize inhibitors of farnesyltransferase.
  • To explore the therapeutic potential of these inhibitors in blocking Ras protein function.
  • To advance the understanding of protein prenyltransferases and cholesterol metabolism regulation.

Main Methods:

  • Discovery of inhibitors through microbial screening for natural compounds.
  • Development of inhibitors based on substrate analogue design.
  • Biochemical assays to characterize enzyme inhibition and protein modification.

Main Results:

  • Identification of novel farnesyltransferase inhibitors via two distinct approaches.
  • Demonstration of inhibitor efficacy in blocking Ras protein modification.
  • Insights into the mechanism of action and potential applications of the inhibitors.

Conclusions:

  • Farnesyltransferase inhibitors represent a promising therapeutic strategy.
  • These compounds aid in characterizing protein prenyltransferases.
  • Further research can elucidate their role in regulating cholesterol metabolism.

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