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FASN inhibition as a potential treatment for endocrine-resistant breast cancer

Aleksandra Gruslova1, Bryan McClellan2, Henriette U Balinda1

  • 1UT Health San Antonio MD Anderson Cancer Center, San Antonio, TX, USA.

Breast Cancer Research and Treatment
|April 24, 2021
PubMed
Abstract

Insights

Fatty acid synthase (FASN) inhibition with TVB-3166 effectively reduces estrogen receptor-positive breast cancer cell proliferation and tumor growth. This approach shows promise for overcoming endocrine therapy resistance in breast cancer patients.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Estrogen receptor (ERα) positive breast cancers often develop resistance to endocrine therapy.
  • Fatty acid synthase (FASN) is implicated in tumor progression and therapy resistance.

Purpose of the Study:

  • To investigate the efficacy of the FASN inhibitor TVB-3166 in endocrine-resistant breast cancer.
  • To determine the impact of FASN inhibition on ERα expression and cellular processes.

Main Methods:

  • Assessed TVB-3166 effects on tamoxifen-resistant cell lines, xenografts, and patient explants.
  • Analyzed ERα expression, subcellular localization, palmitoylation, and ubiquitination.
  • Investigated the role of endoplasmic reticulum stress in FASN inhibition's mechanism.

Main Results:

  • TVB-3166 significantly inhibited proliferation in resistant cells and tumor growth in vivo.
  • FASN inhibition reduced ERα levels and altered its localization, particularly in resistant cells.
  • TVB-3166 treatment induced endoplasmic reticulum stress, mediating ERα level reduction.

Conclusions:

  • FASN inhibition via TVB-3166 is a potential therapeutic strategy for endocrine-resistant breast cancer.
  • Preclinical data support further clinical development of FASN inhibitors for this indication.
Keywords:
Breast cancerER stressEndocrine resistanceEndoplasmic reticulumEstrogen receptorFASNFatty acid synthase

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