当前位置: X-MOL 学术Drug. Discov. Today › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Microtransplantation of human brain receptors into oocytes to tackle key questions in drug discovery
Drug Discovery Today ( IF 7.4 ) Pub Date : 2018-11-03 , DOI: 10.1016/j.drudis.2018.10.015
Ruud Zwart , Francesca Mazzo , Emanuele Sher

It is important in drug discovery to demonstrate that activity of novel drugs found by screening on recombinant receptors translates to activity on native human receptors in brain areas affected by disease. In this review, we summarise the development and use of the microtransplantation technique. Native receptors are reconstituted from human brain tissues into oocytes from the frog Xenopus laevis where they can be functionally assessed. Oocytes microtransplanted with hippocampal tissue from an epileptic patient were used to demonstrate that new antiepileptic agents act on receptors in diseased tissue. Furthermore, frozen post-mortem human tissues were used to show that drugs are active on receptors in brain areas associated with a disease; but not in areas associated with side effects.



中文翻译:

将人脑受体微移植到卵母细胞中以解决药物发现中的关键问题

在药物开发中,重要的是要证明通过筛选重组受体发现的新药的活性转化为对受疾病影响的大脑区域中天然人类受体的活性。在这篇综述中,我们总结了微移植技术的发展和使用。天然受体从人脑组织中重组到青蛙非洲爪蟾的卵母细胞中,可以在功能上对其进行评估。用来自癫痫患者的海马组织微移植的卵母细胞来证明新的抗癫痫药作用于患病组织中的受体。此外,冷冻的死后人体组织被用来证明药物对与疾病相关的大脑区域的受体具有活性。但不适用于与副作用相关的区域。

更新日期:2018-11-03
down
wechat
bug