Chen Jiao, Liu Xiao-Ming, Zhang Yuan
Department of Pediatric Internal Medicine, Xuzhou Children's Hospital, Xuzhou, Jiangsu 221002, P.R. China.
Exp Ther Med. 2018 Jan;15(1):615-619. doi: 10.3892/etm.2017.5483. Epub 2017 Nov 10.
Different types of neuronal nicotinic acetylcholine receptors (nAChRs) are expected to occur , most structure-activity relationship studies have been carried out for just a few neuronal subtypes. The present review enlightens current aspects of venom modulators of nAChRs. Important electronic databases such as PubMed or Google scholar were explored for the collection of latest studies in the field. Clinical and basic research has shown that cholinergic receptors play a role in several disorders of the nervous system such as chronic pain, Alzheimers disease and addiction to nicotine, alcohol and drugs. Unfortunately, the lack of selective modulators for each subtype of nAChR makes their pharmacological characterization difficult, which has slowed the development of therapeutic nAChR modulators with high selectivity and absence of off-target side-effects. Animal venoms have proven to be an excellent natural source of bioactive molecules with activity against ion channels. The present review concludes that the presence of small-molecule nAChR modulators in spider venoms support the use of venoms as a potential source of novel modulators.
预计会出现不同类型的神经元烟碱型乙酰胆碱受体(nAChRs),但大多数构效关系研究仅针对少数神经元亚型进行。本综述阐述了nAChRs毒液调节剂的当前研究情况。为收集该领域的最新研究,检索了诸如PubMed或谷歌学术等重要电子数据库。临床和基础研究表明,胆碱能受体在多种神经系统疾病中起作用,如慢性疼痛、阿尔茨海默病以及对尼古丁、酒精和药物的成瘾。不幸的是,缺乏针对每种nAChR亚型的选择性调节剂使得其药理学特性难以确定,这减缓了具有高选择性且无脱靶副作用的治疗性nAChR调节剂的开发。动物毒液已被证明是具有离子通道活性的生物活性分子的极佳天然来源。本综述得出结论,蜘蛛毒液中存在小分子nAChR调节剂支持将毒液用作新型调节剂的潜在来源。