李晓丹,胡远艳,徐盼,等.作用于乙酰胆碱受体α9α10亚型的芋螺毒素研究进展[J].中国海洋药物,2015,34(6):88-94. |
作用于乙酰胆碱受体α9α10亚型的芋螺毒素研究进展 |
Development of α*-Conotoxin Targeting Alpha9Alpha10 Nicotinic Acetylcholine Receptor |
投稿时间:2015-01-13 修订日期:2015-03-16 |
DOI: |
中文关键词: α*-芋螺毒素、α9α10 nAChR亚型、药理活性 |
English Keywords:α*-Conotoxin, α9α10 nAChR, Pharmacological activity |
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中文摘要: |
烟碱型乙酰胆碱受体(nAChRs)广泛分布于肌肉、中枢神经系统和外周神经系统中,与各种疾病的发生密切相关。其中, α9α10亚型是近年来发现的新型乙酰胆碱受体家族成员之一,也是全世界生物医学研究者关注的热点之一。研究显示α9α10 nAChR 亚型与人类病理生理状态如慢性疼痛(神经痛)和癌症发展等有关。α-芋螺毒素可以选择性地拮抗神经型或肌肉型 nAChR 的不同亚型。据目前报道,已发现4 种芋螺毒素特异性地作用于α9α10 nAChR 亚型,分别是有α-芋螺毒素RgIA 、 Vc1.1 、 PeIA 和αB-芋螺毒素VxXXIVA 。本文主要对 α9α10 nAChR亚型的药理学功能,以及作用于该亚型的4种α*-芋螺毒素研究进展进行综述。 |
English Summary: |
Nicotinic acetylcholine receptors (nAChRs) are widely distributed in muscle, central nervous system and peripheral nervous system, and closely related with varioushuman diseases of the nervous system. The α9α10 nAChR subtype is a new member of the nAChRs family discovered in recent years and a hotspot in biomedicine, which is related with important human pathophysiological states such as chronic pain and cancer development etc. . α*-Conotoxins are small peptides which acts as antagonists of nAChR subtypes according to the pharmacological activity. So far there are 4 α*-conotoxin, i.e. α-conotoxin RgIA, Vc1.1 , PeIA and αB-conotoxin VxXXIVA targeting α9α10 nAChRs. This review summarizes progress of α9α10 nAChRfunction and characteristics of α*-conotoxins which are active on α9α10 nAChR. . |
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