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[G蛋白偶联受体。2012年诺贝尔化学奖授予罗伯特·J·莱夫科维茨和布莱恩·科比尔卡]

[G-protein coupled receptors. Nobel Prize 2012 for chemistry to Robert J. Lefkowitz and Brian Kobilka].

作者信息

Bockaert Joël

机构信息

CNRS UMR 5203, Institut de génomique fonctionnelle, Inserm U661, Université de Montpellier 1 et 2, 34000 Montpellier, France.

出版信息

Med Sci (Paris). 2012 Dec;28(12):1133-7. doi: 10.1051/medsci/20122812026. Epub 2012 Dec 21.

Abstract

The 2012 Nobel Prize for chemistry has been won by Robert J. Lefkowitz and Brian Kobilka for their work on G protein-coupled receptors (GPCRs). Those receptors (3% of human genome) evolutionary are derived from one 1 or 2 ancestors and are able to recognize external message as different as light, odorants, gustative molecules and intercellular messages such as hormones and neurotransmitters. They are targets of 30-40% of therapeutic drugs. Robert J. Lefkowitz has been one of the leaders of the field from more than 40 years and has built several key concepts of the domain. Brian Kobilka was successful, in 2007, in producing a crystal structure of the β2-adrenergic receptor. This paved the way for the production of a series of almost 50 GPCR crystal structures both in inactive and active forms.

摘要

罗伯特·J·莱夫科维茨和布莱恩·科比尔卡因在G蛋白偶联受体(GPCRs)方面的研究成果而荣获2012年诺贝尔化学奖。这些受体(占人类基因组的3%)在进化上源自一个或两个祖先,能够识别诸如光、气味分子、味觉分子等不同的外部信息以及诸如激素和神经递质等细胞间信息。它们是30% - 40%治疗药物的作用靶点。罗伯特·J·莱夫科维茨在该领域担任领军人物超过40年,并建立了该领域的几个关键概念。布莱恩·科比尔卡于2007年成功获得了β2肾上腺素能受体的晶体结构。这为一系列近50种处于非活性和活性形式的GPCR晶体结构的产生铺平了道路。

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