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Illuminating the Druggable GPCR-ome

Illuminating the Druggable GPCR-ome
阐明可药物化的 GPCR-ome
批准号:
10612133
负责人:
Bryan L. Roth
金额:
$74.95万
依托单位国家:
美国
项目类别:
财政年份:
2017
资助国家:
美国
项目状态:
已结题
起止时间:
2017-09-15 至 2023-08-31

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中文摘要
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英文摘要
Abstract PROJECT SUMMARY G protein coupled receptors (GPCRs) represent essential molecular targets for a large number of approved as well as investigational medications. Of the 380 or so non-olfactory GPCRs in the human genome around 100 are understudied and/or orphan receptors (oGPCRs). The oGPCRs represent potential therapeutic targets although discovering drugs that modulate them is challenging. Here we will solve the structures of 15-20 oGPCRs using cryogenic electron microscopy (cryo-EM). The solved structures then will serve as templates for structure-guided drug discovery targeting these oGPCRs.
期刊论文(24)
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DOI: 10.1038/s41586-023-06913-9
发表时间: 2024-02
期刊: NATURE
影响因子: 64.8
作者: [Wang, Shuai, Deleon, Chelsea, Sun, Wenfei, Quake, Stephen R., Roth, Bryan L., Suedhof, Thomas C.]
通讯作者: Suedhof, Thomas C.
DOI: 10.1038/nchembio.2334
发表时间: 2017-05
期刊: Nature chemical biology
影响因子: 14.8
作者: [Lansu K, Karpiak J, Liu J, Huang XP, McCorvy JD, Kroeze WK, Che T, Nagase H, Carroll FI, Jin J, Shoichet BK, Roth BL]
通讯作者: Roth BL
DOI: 10.1016/j.cell.2017.07.009
发表时间: 2017-07-27
期刊: Cell
影响因子: 64.5
作者: [Wacker D, Stevens RC, Roth BL]
通讯作者: Roth BL
DOI: 10.1021/acs.jcim.7b00343
发表时间: 2017-11-27
期刊: Journal of chemical information and modeling
影响因子: 5.6
作者: [Butler KV, MacDonald IA, Hathaway NA, Jin J]
通讯作者: Jin J
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