Graduate Institute of Medical Sciences, Taipei Medical University, Taipei 110, Taiwan.
J Oncol. 2011;2011:693424. doi: 10.1155/2011/693424. Epub 2011 Apr 28.
Cigarette smoking bears a strong etiological association with many neovascularization-related diseases, including cancer, cardiovascular disease, and age-related macular degeneration. Cigarette smoke is a complex mixture of many compounds, including nicotine, which is the major active and addictive component of tobacco. Nicotine and its specific metabolized carcinogens directly bind to nicotinic acetylcholine receptors (nAChRs) on cell membranes and trigger the nAChR signal cascade. The nAChRs were originally thought to be ligand-gated ion channels that modulate physiological processes ranging from neurotransmission to cancer signaling. For several decades, the nAChRs served as a prototypic molecule for neurotransmitter receptors; however, they are now important therapeutic targets for various diseases, including Alzheimer's and Parkinson's diseases, schizophrenia, and even cancer. This paper describes recent advances in our understanding of the assembly, activity, and biological functions of nicotinic receptors, as well as developments in the therapeutic application of nicotinic receptor ligands.
吸烟与许多新生血管相关疾病密切相关,包括癌症、心血管疾病和年龄相关性黄斑变性。香烟烟雾是多种化合物的复杂混合物,包括尼古丁,尼古丁是烟草中主要的活性和成瘾成分。尼古丁及其特定的代谢致癌物质直接与细胞膜上的烟碱型乙酰胆碱受体(nAChRs)结合,并触发 nAChR 信号级联反应。nAChRs 最初被认为是配体门控离子通道,调节从神经传递到癌症信号的各种生理过程。几十年来,nAChRs 一直是神经递质受体的典型分子;然而,它们现在是包括阿尔茨海默病和帕金森病、精神分裂症甚至癌症在内的各种疾病的重要治疗靶点。本文描述了我们对烟碱型乙酰胆碱受体组装、活性和生物学功能的理解的最新进展,以及烟碱型乙酰胆碱受体配体治疗应用的发展。