Cell:上海科技大学刘志杰团队等解析出大麻素1型受体三维结构

2016-10-24 佚名 生物谷

在一项新的研究中,来自中国科学院生物物理研究所生物大分子国家重点实验室和上海科技大学等机构的研究人员获得迄今为止最为清晰的导致与大麻相关的“high”的大麻素1型受体(cannabinoid receptor 1, CB1)的结构图。CB1的三维结构图揭示出四氢大麻酚(THC)等分子如何结合到CB1上,其中已发现CB1嵌入到很多神经细胞的表面中。这可能解释了旨在模拟大麻制品使用但不会产生“high


在一项新的研究中,来自中国科学院生物物理研究所生物大分子国家重点实验室和上海科技大学等机构的研究人员获得迄今为止最为清晰的导致与大麻相关的“high”的大麻素1型受体(cannabinoid receptor 1, CB1)的结构图。CB1的三维结构图揭示出四氢大麻酚(THC)等分子如何结合到CB1上,其中已发现CB1嵌入到很多神经细胞的表面中。这可能解释了旨在模拟大麻制品使用但不会产生“high”的止痛药能够导致不想到的副作用,这就为开发未来的疗法奠定基础。相关研究结果发表在2016年10月20日那期Cell期刊上,论文标题为“Crystal Structure of the Human Cannabinoid Receptor CB1”。论文通信作者为上海科技大学iHuman研究所刘志杰(Zhi-jie Liu)教授、Raymond Stevens教授、美国东北大学化学与化学生物学系科学家Alexandros Makriyannis和美国斯克里普斯研究所分子治疗与神经科学系科学家Laura M. Bohn。

Stevens说,“随着大麻毒品在美国越来越流行,我们需要理解THC(大麻中的精神活性组分)和合成大麻素等分子如何与这种受体相互作用,特别是我们正看到一些人因使用合成大麻素而出现在急救室中。”

Stevens说,“科学家们感兴趣的是如何能够对THC或合成大麻素加以改变以便具有不同的效应。如今,我们最终解析出CB1的结构,我们能够开始理解对这种药物结构进行的改变如何能够影响这种受体。”

比如,源自大麻的药物已被用来治疗肥胖,但是经过研究,研究人员发现这些治疗分子能够触发抑郁、焦虑,甚至自杀倾向,因此这种药物被撤出市场。当前,研究人员正在观察合成大麻素(如Spice和K2)相关的潜在副作用,其中这些合成大麻素旨在复制与THC相关的“high”,但是会导致使用者被送到急诊室。

刘教授说,“我们需要理解大麻毒品如何在我们体内发挥作用;它能够具有治疗潜力和娱乐性使用,但是大麻素也能够是非常危险的。通过开展基础性科学研究和理解这种受体如何发挥作用,我们就能够利用它在未来帮助人们。”

原始出处

Tian Hua, Kiran Vemuri, Mengchen Pu, Lu Qu, Gye Won Han, Yiran Wu, Suwen Zhao, Wenqing Shui, Shanshan Li, Anisha Korde, Robert B. Laprairie, Edward L. Stahl, Jo-Hao Ho, Nikolai Zvonok, Han Zhou, Irina Kufareva, Beili Wu, Qiang Zhao, Michael A. Hanson, Laura M. Bohn, Alexandros Makriyannis, Raymond C. Stevens, Zhi-Jie Liu.Crystal Structure of the Human Cannabinoid Receptor CB1.Cell.2016

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    2017-09-09 hongbochen
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    2017-03-02 维他命
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    2016-10-26 kcb069
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Nature子刊:首次鉴定出激活人精子的大麻素受体GPR18

在一项新的研究中,来自德国波鸿和波恩的研究人员在精子中检测到一种新型的大麻素受体(cannabinoid receptor)。存在于男性和女性生殖道中的内源性大麻素激活精子:它们触发所谓的顶体反应(acrosome reaction),在这种反应期间,精子释放消化酶,丢掉它的头部前半部分上的帽状结构。如果没有这种反应,精子就不能够穿入卵子中。相关研究结果于2016年8月30日在线发表在Scient