Illuminating the Druggable GPCR-ome
Illuminating the Druggable 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
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
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.
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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
DOI:
10.1038/s41593-020-0661-3
发表时间:
2020-07-06
期刊:
NATURE NEUROSCIENCE
影响因子:
25
作者:
[Nagai, Yuji, Miyakawa, Naohisa, Minamimoto, Takafumi]
通讯作者:
Minamimoto, Takafumi
共 9 条
Mechanistic insights into LSD actions at 5-HT2A serotonin receptors
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批准号:10550420
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项目类别:
-
资助金额:$66.45万
-
财政年份:2023
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负责人:Bryan L. Roth
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依托单位:
STRUCTURE AND FUNCTION OF MRG-FAMILY RECEPTORS
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批准号:10419804
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项目类别:
-
资助金额:$58.26万
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财政年份:2022
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负责人:Bryan L. Roth
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依托单位:
STRUCTURE AND FUNCTION OF MRG-FAMILY RECEPTORS
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批准号:10593175
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项目类别:
-
资助金额:$56.69万
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财政年份:2022
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负责人:Bryan L. Roth
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依托单位:
Mechanistic insights into LSD actions at 5-HT2A serotonin receptors
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批准号:10356900
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项目类别:
-
资助金额:$63.95万
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财政年份:2018
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负责人:Bryan L. Roth
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依托单位:
Mechanistic insights into LSD actions at 5-HT2A serotonin receptors
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批准号:9496860
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项目类别:
-
资助金额:$64.68万
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财政年份:2018
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负责人:Bryan L. Roth
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依托单位:
Mechanistic insights into LSD actions at 5-HT2A serotonin receptors
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批准号:10112869
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项目类别:
-
资助金额:$63.55万
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财政年份:2018
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负责人:Bryan L. Roth
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依托单位:
Molecular Details of Psychoactive Drug Actions
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批准号:10557802
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项目类别:
-
资助金额:$61.12万
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财政年份:2017
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负责人:Bryan L. Roth
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依托单位:
Illuminating the Druggable GPCR-ome
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批准号:10011803
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项目类别:
-
资助金额:$224.3万
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财政年份:2017
-
负责人:Bryan L. Roth
-
依托单位:
Illuminating the druggable GPCR-ome
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批准号:9451604
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项目类别:
-
资助金额:$230.13万
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财政年份:2017
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负责人:Bryan L. Roth
-
依托单位:
Illuminating the Druggable GPCR-ome
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批准号:10249123
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项目类别:
-
资助金额:$224.1万
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财政年份:2017
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负责人:Bryan L. Roth
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依托单位:
NIMH Psychoactive Drug Screening Program
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批准号:9497680
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项目类别:
-
资助金额:$283.83万
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财政年份:2017
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负责人:Bryan L. Roth
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依托单位:
Molecular Details of Psychoactive Drug Actions
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批准号:10366918
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项目类别:
-
资助金额:$62.9万
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财政年份:2017
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负责人:Bryan L. Roth
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依托单位:
Illuminating the Druggable GPCR-ome
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批准号:9762094
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项目类别:
-
资助金额:$224.39万
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财政年份:2017
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负责人:Bryan L. Roth
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依托单位:
NIMH Psychoactive Drug Screening Program
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批准号:9335707
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项目类别:
-
资助金额:$266.8万
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财政年份:2016
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负责人:Bryan L. Roth
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依托单位:
NIMH Psychoactive Drug Screening Program
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批准号:9113406
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项目类别:
-
资助金额:$259.48万
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财政年份:2015
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负责人:Bryan L. Roth
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依托单位:
Structure-Function of Opioid Receptors
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批准号:8828150
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项目类别:
-
资助金额:$137.03万
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财政年份:2014
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负责人:Bryan L. Roth
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依托单位:
Scalable technologies for illuminating the druggable GPCR-ome
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批准号:9115364
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项目类别:
-
资助金额:$21.32万
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财政年份:2014
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负责人:Bryan L. Roth
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依托单位:
Structure-Function of Opioid Receptors
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批准号:8667564
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项目类别:
-
资助金额:$153.19万
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财政年份:2014
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负责人:Bryan L. Roth
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依托单位:
Scalable technologies for illuminating the druggable GPCR-ome
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批准号:8898224
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项目类别:
-
资助金额:$39.69万
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财政年份:2014
-
负责人:Bryan L. Roth
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依托单位:
Scalable technologies for illuminating the druggable GPCR-ome
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批准号:8781263
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项目类别:
-
资助金额:$40.95万
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财政年份:2014
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负责人:Bryan L. Roth
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依托单位:
海外基金