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Differential Expression of Nicotine Acetylcholine Receptors Associates with Human Breast Cancer and Mediates Antitumor Activity of αO-Conotoxin GeXIVA

Key Laboratory of Tropical Biological Resources of Ministry of Education, Key Laboratory for Marine Drugs of Haikou, School of Life and Pharmaceutical Sciences, Hainan University, Haikou 570228, Hainan, China
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Mar. Drugs 2020, 18(1), 61; https://doi.org/10.3390/md18010061
Received: 27 December 2019 / Revised: 13 January 2020 / Accepted: 14 January 2020 / Published: 17 January 2020
Nicotinic acetylcholine receptors (nAChRs) are membrane receptors and play a major role in tumorigenesis and cancer progression. Here, we have investigated the differential expression of nAChR subunits in human breast cancer cell lines and breast epithelial cell lines at mRNA and protein levels and the effects of the αO-conotoxin GeXIVA, antagonist of α9α10 nAChR, on human breast cancer cells. Reverse transcription polymerase chain reaction (PCR) demonstrated that all nAChR subunits, except α6, were expressed in the 20 tested cell lines. Real time quantitative PCR (QRT-PCR) suggested that the mRNA of α5, α7, α9 and β4 nAChR subunits were overexpressed in all the breast cancer cell lines compared with the normal epithelial cell line HS578BST. α9 nAChR was highly expressed in almost all the breast cancer cell lines in comparison to normal cells. The different expression is prominent (p < 0.001) as determined by flow cytometry and Western blotting, except for MDA-MB-453 and HCC1395 cell lines. αO-conotoxin GeXIVA that targeted α9α10 nAChR were able to significantly inhibit breast cancer cell proliferation in vitro and merits further investigation as potential agents for targeted therapy. View Full-Text
Keywords: nicotinic acetylcholine receptors (nAChRs); Breast cancer cells; αO-conotoxin GeXIVA; anti-proliferation nicotinic acetylcholine receptors (nAChRs); Breast cancer cells; αO-conotoxin GeXIVA; anti-proliferation
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MDPI and ACS Style

Sun, Z.; Zhangsun, M.; Dong, S.; Liu, Y.; Qian, J.; Zhangsun, D.; Luo, S. Differential Expression of Nicotine Acetylcholine Receptors Associates with Human Breast Cancer and Mediates Antitumor Activity of αO-Conotoxin GeXIVA. Mar. Drugs 2020, 18, 61. https://doi.org/10.3390/md18010061

AMA Style

Sun Z, Zhangsun M, Dong S, Liu Y, Qian J, Zhangsun D, Luo S. Differential Expression of Nicotine Acetylcholine Receptors Associates with Human Breast Cancer and Mediates Antitumor Activity of αO-Conotoxin GeXIVA. Marine Drugs. 2020; 18(1):61. https://doi.org/10.3390/md18010061

Chicago/Turabian Style

Sun, Zhihua, Manqi Zhangsun, Shuai Dong, Yiqiao Liu, Jiang Qian, Dongting Zhangsun, and Sulan Luo. 2020. "Differential Expression of Nicotine Acetylcholine Receptors Associates with Human Breast Cancer and Mediates Antitumor Activity of αO-Conotoxin GeXIVA" Marine Drugs 18, no. 1: 61. https://doi.org/10.3390/md18010061

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