Inhibitors of Fatty Acid Synthase for Prostate Cancer

Abstract

Fatty acid synthase (FASN), the enzyme that synthesizes fatty acid in cells, is overexpressed in prostate cancer and a potential therapeutic target. We have identified several novel chemical scaffolds with potential to inhibit FASN. An extensive series of anti-FASN pharmacophores has been synthesized and characterized for their ability to inhibit recombinant FASN, FASN activity in tumor cells, and to kill prostate cancer cell lines. The best inhibitors have increased potency over other FASN inhibitors, including orlistat, the prototype FASN thioesterase inhibitor. The current studies represent a significant advancement of the development of FASN inhibitors and represent and advancement of the translation FASN inhibitors into the clinic.

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Document Details

Document Type
Technical Report
Publication Date
May 01, 2011
Accession Number
ADA545695

Entities

People

  • Jeffrey W. Schmitt
  • Steven J. Kridel
  • W. T. Lowther

Organizations

  • Wake Forest University

Tags

DTIC Thesaurus Topics

  • Amino Acids
  • Cells
  • Chemical Compounds
  • Chemical Stability
  • Chemical Synthesis
  • Chemistry
  • Department Of Defense
  • Fatty Acids
  • Inhibition
  • Inhibitors
  • Intellectual Property
  • Molecules
  • Neoplasms
  • Patent Applications
  • Prostate
  • Prostate Cancer
  • Quinones

Fields of Study

  • Biology

Readers

  • Aerospace Propulsion Engineering.
  • Molecular Biology and Genetics
  • Molecular and Cellular Biochemistry