Related Experiment Video

Updated: Jul 13, 2026

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase
11:01

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

Published on: November 23, 2016

Novel antagonists of the thioesterase domain of human fatty acid synthase

Robyn D Richardson1, Jeffrey W Smith

  • 1Cancer Research Center and Center on Proteolytic Pathways, Burnham Institute for Medical Research, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA.

Molecular Cancer Therapeutics
|July 11, 2007
PubMed

Insights

Novel compounds targeting fatty acid synthase (FAS) show promise as anticancer therapeutics. These inhibitors block fatty acid synthesis, leading to cancer cell death and reduced tumor growth.

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Oncology

Background:

  • Fatty acid synthase (FAS) is frequently overexpressed in various cancers.
  • FAS is a validated therapeutic target for cancer treatment.
  • Inhibiting FAS can impede tumor cell proliferation, induce apoptosis, and suppress tumor growth.

Purpose of the Study:

  • To identify novel pharmacophores targeting the thioesterase domain of FAS.
  • To develop new anticancer agents by inhibiting FAS.

Main Methods:

  • High-throughput fluorogenic screening was employed.
  • Identification and characterization of novel FAS inhibitors.

Main Results:

  • A novel pharmacophore, 5-(furan-2-ylmethylene) pyrimidine-2,4,6-trione, was identified.
  • These compounds act as competitive inhibitors of the FAS thioesterase domain.
  • Inhibition of de novo fatty acid synthesis and induction of FAS-dependent cancer cell death were observed.

Conclusions:

  • The identified FAS antagonists represent a promising pharmacologic lead for anticancer drug development.
  • Targeting the thioesterase domain of FAS offers a viable strategy for cancer therapy.

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