Targeting Alpha7 Nicotinic Acetylcholine Receptors in Lung Cancer: Insights, Challenges, and Therapeutic Strategies

被引：4

作者：

Arunrungvichian, Kuntarat ^{[1
,2
]}

Vajragupta, Opa ^{[3
]}

Hayakawa, Yoshihiro ^{[4
]}

Pongrakhananon, Varisa ^{[5
,6
]}

机构：

[1] Mahidol Univ, Fac Pharm, Dept Pharmaceut Chem, Bangkok 10400, Thailand

[2] Mahidol Univ, Unit Cpds Lib Drug Discovery, Bangkok 10400, Thailand

[3] Chulalongkorn Univ, Fac Pharmaceut Sci, Res Affairs, Bangkok 10330, Thailand

[4] Univ Toyama, Inst Nat Med, Toyama 9300194, Japan

[5] Chulalongkorn Univ, Fac Pharmaceut Sci, Dept Pharmacol & Physiol, Bangkok 10330, Thailand

[6] Chulalongkorn Univ, Preclin Tox & Efficacy Assessment Med & Chem Res U, Bangkok 10330, Thailand

来源：

ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE | 2023年 / 7卷 / 01期

关键词：

alpha; 7; nAChR; antagonist; cancerprogression; lung cancer; ALPHA-7-NICOTINIC RECEPTOR; CELL-PROLIFERATION; SUBUNIT GENES; HIGH-AFFINITY; EXPRESSION; ACTIVATION; ALPHA-7-NACHR; ANTAGONISTS; INVASION; ANGIOGENESIS;

D O I：

10.1021/acsptsci.3c00138

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Alpha7 nicotinic acetylcholine receptor (alpha 7 nAChR) is an ion-gated calcium channel that plays a significant role in various aspects of cancer pathogenesis, particularly in lung cancer. Preclinical studies have elucidated the molecular mechanism underlying alpha 7 nAChR-associated lung cancer proliferation, chemotherapy resistance, and metastasis. Understanding and targeting this mechanism are crucial for developing therapeutic interventions aimed at disrupting alpha 7 nAChR-mediated cancer progression and improving treatment outcomes. Drug research and discovery have determined natural compounds and synthesized chemical antagonists that specifically target alpha 7 nAChR. However, approved alpha 7 nAChR antagonists for clinical use are lacking, primarily due to challenges related to achieving the desired selectivity, efficacy, and safety profiles required for effective therapeutic intervention. This comprehensive review provided insights into the molecular mechanisms associated with alpha 7 nAChR and its role in cancer progression, particularly in lung cancer. Furthermore, it presents an update on recent evidence about alpha 7 nAChR antagonists and addresses the challenges encountered in drug research and discovery in this field.

引用

页码：28 / 41

页数：14