Abstract

Background: Docosahexaenoic acid (DHA) is an essential polyunsaturated fatty acid compound present in deep water fishes and dietary supplements, with a wide spectrum of potential health benefits, ranging from neurological to anti-inflammatory. Methods: Due to the fact that DHA is considered a breast cancer risk reducer, we examined the impact of DHA on MCF-7 breast cancer cells’ viability and its inhibitory properties on protein tyrosine phosphatase 1B (PTP1B), a pro-oncogenic phosphatase. Results: We found that DHA is able to lower both the enzymatic activity of PTP1B phosphatase and the viability of MCF-7 breast cancer cells. We showed that unsaturated DHA possesses a significantly higher inhibitory activity toward PTP1B in comparison to similar fatty acids. We also performed a computational analysis of DHA binding to PTP1B and discovered that it is able to bind to an allosteric binding site. Conclusions: Utilizing both a recombinant enzyme and cellular models, we demonstrated that DHA can be considered a potential pharmacological agent for the prevention of breast cancer.

Highlights

  • Breast cancer is a common malignant female cancer affecting women worldwide

  • We examined the effect of Docosahexaenoic acid (DHA) on the enzymatic activity of protein tyrosine phosphatase 1B (PTP1B)

  • We found that DHA was able to decrease the enzymatic activity of PTP1B at concentrations in the micromolar range (Figure 2)

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Summary

Introduction

Breast cancer is a common malignant female cancer affecting women worldwide. Its therapy involves surgical intervention and radiotherapy completed with adjuvant chemotherapy. Protein tyrosine phosphatase 1B (PTP1B) is involved in the dephosphorylation process of tyrosine kinases responsible for breast cancer development, i.e., HER1/EGFR, Src, JAK, as well as of signal transducer and activator of transcription (STAT). PTP1B is considered a potentially important target for the treatment or prevention of breast cancer. Viability and its inhibitory properties on protein tyrosine phosphatase 1B (PTP1B), a pro-oncogenic phosphatase. Results: We found that DHA is able to lower both the enzymatic activity of PTP1B phosphatase and the viability of MCF-7 breast cancer cells. We showed that unsaturated DHA possesses a significantly higher inhibitory activity toward PTP1B in comparison to similar fatty acids. Conclusions: Utilizing both a recombinant enzyme and cellular models, we demonstrated that DHA can be considered a potential pharmacological agent for the prevention of breast cancer

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