Septerna

None Laurel Oldach
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引用次数: 0

Abstract

There are hundreds of G protein–coupled receptors (GPCRs) in the human genome, regulating just about every physiological system. While roughly a third of marketed drugs target a GPCR, many of the receptors have remained out of reach for drug hunters, in part because of challenges involved in studying them . After the heyday of GPCR-targeting drugs in the 1990s and early 2000s, few medicines targeting these proteins have been introduced. But new technologies may be poised to change that. A few years ago, chemistry Nobel laureate Robert J. Lefkowitz was working with scientists in his lab at Duke University in North Carolina to develop a new way to isolate enzymatically active GPCRs. Halfway around the world, at Monash University in Melbourne, Australia, the eminent pharmacology duo Patrick Sexton and Arthur Christopoulos was simultaneously developing techniques to modulate GPCR signaling using structure-based drug design. And in San Francisco, Jeffrey Finer, a
Septerna
人类基因组中有数百个G蛋白偶联受体(gpcr),它们调节着几乎所有的生理系统。虽然大约有三分之一的上市药物靶向GPCR,但许多受体仍然是药物猎人无法触及的,部分原因是研究它们所涉及的挑战。在20世纪90年代和21世纪初gpcr靶向药物的鼎盛时期之后,很少有针对这些蛋白质的药物被引入。但新技术可能会改变这种状况。几年前,诺贝尔化学奖得主罗伯特·j·莱夫科维茨(Robert J. Lefkowitz)在北卡罗来纳州杜克大学(Duke University)的实验室里与科学家们合作,开发了一种分离酶活性gpcr的新方法。在地球的另一端,澳大利亚墨尔本的莫纳什大学,著名的药理学二人组Patrick Sexton和Arthur Christopoulos正在同时开发利用基于结构的药物设计来调节GPCR信号的技术。在旧金山,一位名叫杰弗里
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