Nicotinic acetylcholine receptor-based blockade

Applications of molecular targets for cancer therapy

Chih Hsiung Wu, Chia Hwa Lee, Yuan Soon Ho

Research output: Contribution to journalReview article

64 Citations (Scopus)

Abstract

The nicotinic acetylcholine receptor (nAChR) was first characterized in 1970 as a membrane receptor of a neurotransmitter and an ion channel. nAChRs have been shown to be involved in smoking-induced cancer formation in multiple types of human cancer cells. In vitro and in vivo animal studies have shown that homopentameric nAChR inhibitors, such as methyllycaconitine and α-Bgtx, can attenuate nicotine-induced proliferative, angiogenic, and metastatic effects in lung, colon, and bladder cancer cells. Recent publications have shown that α9-nAChR is important for breast cancer formation, and in many in vivo studies, α9-nAChR-specific antagonists (e.g., α-ImI, α-ImI, Vc1.1, RgIA, and It14a) produced an analgesic effect. Vc1.1 functions in a variety of animal pain models and currently has entered phase II clinical trials. For cancer therapy, natural compounds such as garcinol and EGCG have been found to block nicotine- and estrogen-induced breast cancer cell proliferation through inhibition of the α9-nAChR signaling pathway. A detailed investigation of the carcinogenic effects of nAChRs and their specific antagonists would enhance our understanding of their value as targets for clinical translation.

Original languageEnglish
Pages (from-to)3533-3541
Number of pages9
JournalClinical Cancer Research
Volume17
Issue number11
DOIs
Publication statusPublished - Jun 1 2011

Fingerprint

Nicotinic Receptors
Neoplasms
Nicotine
Breast Neoplasms
Therapeutics
Phase II Clinical Trials
Neurotransmitter Receptor
Ion Channels
Urinary Bladder Neoplasms
Colonic Neoplasms
Analgesics
Lung Neoplasms
Estrogens
Animal Models
Smoking
Cell Proliferation
Pain
Membranes

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

Cite this

Nicotinic acetylcholine receptor-based blockade : Applications of molecular targets for cancer therapy. / Wu, Chih Hsiung; Lee, Chia Hwa; Ho, Yuan Soon.

In: Clinical Cancer Research, Vol. 17, No. 11, 01.06.2011, p. 3533-3541.

Research output: Contribution to journalReview article

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