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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：
UNIV OF NORTH CAROLINA CHAPEL HILL
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
来源：
https://reporter.nih.gov/project-details/10612133
关键词：
ArrestinsAwardCell LineChemicalsChemistryClustered Regularly Interspaced Short Palindromic RepeatsCollaborationsCommunitiesCryoelectron MicroscopyDatabasesDevelopmentDockingDrug TargetingElectron MicroscopyEngineeringEpinephrineFundingG-Protein-Coupled ReceptorsG-substrateGeneticGenetically Engineered MouseGoalsHeart RateHuman GenomeIndividualInformaticsInfrastructureInvestigationLearningLightLipidsMemoryModelingMolecular TargetMusOrphanPharmaceutical ChemistryPharmaceutical PreparationsPharmacologyPhasePhysiologicalPhysiologyPlasmidsProtein FamilyReagentReporterReporter GenesResearchResearch PersonnelResource SharingResourcesRespirationSignal TransductionSpecific qualifier valueStructureSynthesis ChemistryTechnologyTestingTissuesTransducersViralVisionYeastsbasecell typechemical geneticschemical synthesischemokinecomputer infrastructurecomputerized toolscryogenicsdata resourcedata sharingdesigner receptors exclusively activated by designer drugsdrug discoveryexperimental studygenetic approachhuman diseasein vivo Modellarge datasetsmedical schoolsnew technologynovelnovel therapeuticsoptogeneticsprogramspublic health relevancereceptorscreeningtargeted treatmenttherapeutic targettool

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中文摘要
翻译
摘要 项目总结 G蛋白偶联受体(GPCRs)是许多已批准药物和研究药物的基本分子靶点。在人类基因组中的380个左右的非嗅觉GPCR中，约有100个未得到充分研究和/或孤儿受体(OGPCRs)。OGPCRs代表着潜在的治疗靶点，尽管发现调节它们的药物是具有挑战性的。 在这里，我们将使用低温电子显微镜(Cryo-EM)来解决15-20 oGPCRs的结构。然后，解决的结构将作为针对这些oGPCRs的结构导向药物发现的模板。
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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会议论文
Alternative splicing of latrophilin-3 controls synapse formation.
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.
In silico design of novel probes for the atypical opioid receptor MRGPRX2.
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
How Ligands Illuminate GPCR Molecular Pharmacology.
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
Report and Application of a Tool Compound Data Set.
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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