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ACS Med Chem Lett. 2017 Sep 14;8(10):1072-1076. doi: 10.1021/acsmedchemlett.7b00282. eCollection 2017.

Serotonin Analogues as Inhibitors of Breast Cancer Cell Growth.

Author information

  • 1Division of Chemical Biology and Medicinal Chemistry, College of Pharmacy, University of Texas at Austin, Austin, Texas 78712, United States.
  • 2Department of Chemistry, University of Texas at Austin, Austin, Texas 78712, United States.
  • 3Graduate Program in Cell and Molecular Biology, University of Texas at Austin, Austin, Texas 78712, United States.
  • 4Department of Nutritional Sciences, Dell Pediatric Research Institute, University of Texas at Austin, Austin, Texas 78723, United States.
  • 5Section of Translational Breast Cancer Research, University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
  • 6Department of Breast Medical Oncology, University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
  • 7Division of Pharmacology & Toxicology, College of Pharmacy, University of Texas at Austin, Dell Pediatric Research Institute, Austin, Texas 78723, United States.

Abstract

Serotonin (5-hydroxytryptamine, 5-HT) is a critical local regulator of epithelial homeostasis in the breast and exerts its actions through a number of receptors. Dysregulation of serotonin signaling is reported to contribute to breast cancer pathophysiology by enhancing cell proliferation and promoting resistance to apoptosis. Preliminary analyses indicated that the potent 5-HT1B/1D serotonin receptor agonist 5-nonyloxytryptamine (5-NT), a triptan-like molecule, induced cell death in breast cancer cell lines. Thus, we synthesized a series of novel alkyloxytryptamine analogues, several of which decreased the viability of various human cancer cell lines. Proteomic and metabolomic analyses showed that compounds 6 and 10 induced apoptosis and interfered with signaling pathways that regulate protein translation and survival, such as the Akt/mTOR pathway, in triple-negative breast cancer cells.

KEYWORDS:

Breast cancer; serotonin receptor; tryptamine

PMID:
29057053
PMCID:
PMC5641961
[Available on 2018-10-12]
DOI:
10.1021/acsmedchemlett.7b00282
[PubMed]
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