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2012年诺贝尔化学奖颁给了Robert J.Lefkowitz和Brian K.Kobilka,基于他们在G蛋白偶联受体(G-protein-coupled receptors,GPCRs)研究领域的杰出贡献.Robert J.Lefkowitz是现代GPCRs研究的奠基人.他开创了利用放射配体研究受体功能的先河,证实了受体的存在,率先得到受体克隆,发现了G蛋白偶联受体激酶与β-arrestins介导受体的减敏与内吞,并发现了β-arrestins的信号转导功能.Brian K.Kobilka多年来坚持不懈,开创了很多GPCRs晶体学上的突破性方法,是揭示β2肾上腺素受体晶体结构的第一人,引导了近年来GPCRs受体晶体结构领域的迅猛发展.尤其令人惊叹的是,他展示了β2肾上腺素受体激活瞬间的晶体构象.本文综述了两位杰出科学家探索GPCRs的科研经历及成果,希望读者能够有所借鉴.
The 2012 Nobel Prize in Chemistry was presented to Robert J. Lefkowitz and Brian K. Kobilka for their outstanding contributions in the field of G-protein-coupled receptors (GPCRs). Robert J. Lefkowitz, Founder of GPCRs, pioneered the use of radioligands to study receptor function, confirmed the presence of receptors, took the lead in obtaining receptor clones and found that G protein-coupled receptor kinases interact with beta-arrestins Denervation and endocytosis of β-arrestins and discovered the signal transduction of β-arrestins, Brian K. Kobilka has persevered for many years and pioneered many of the crystallographic breakthroughs in GPCRs that reveal the crystal structure of β2 adrenergic receptors The first person, which led to the rapid development of the GPCRs receptor crystal structure in recent years, was especially amazing in that he showed the crystal conformation of the beta2 adrenergic receptor at the moment of activation. This review summarizes the scientific findings of two prominent scientists in exploring GPCRs Experience and achievements, I hope readers can learn from.