Hsp90B in Bladder Cancer
Hsp90B in Bladder Cancer
批准号:
9922232
负责人:
Brian S J Blagg
金额:
$35.17万
依托单位:
依托单位国家:
美国
项目类别:
财政年份:
2018
资助国家:
美国
项目状态:
已结题
起止时间:
2018-05-08 至 2022-04-30
关键词:
AffinityAnimal ModelAntineoplastic AgentsBindingBinding SitesCardiotoxicityCellsClientClinicalClinical TrialsCollaborationsComplexCrystallizationDataDevelopmentDiseaseDoseDrug DesignDrug TargetingExhibitsFrequenciesGenerationsGoalsHSP 90 inhibitionHeat shock proteinsHeat-Shock Proteins 90Heat-Shock ResponseHepatotoxicityIn VitroIndividualLeadMAPK7 geneMalignant NeoplasmsMalignant neoplasm of urinary bladderMaximum Tolerated DoseMethodsMolecular ChaperonesMolecular ConformationN-terminalPathogenesisPathway interactionsPatientsPeripheral Nervous System DiseasesPharmaceutical PreparationsPharmacologyPlayProtein IsoformsProteinsProteomicsReportingResearch PersonnelRoleScheduleSignal TransductionStructureStudy modelsTimeToxic effectTranslatingValidationantitumor agentbaseclinical candidatedrug developmentin vivoinhibitor/antagonistinterestknock-downmolecular modelingmyelinationnanomolarneuropeptide Ynovel anticancer drugprotein degradationprotein foldingresearch clinical testingscaffoldside effect
中文摘要
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英文摘要
The development of new methods to treat cancer is greatly needed. The Hsp90 protein folding machinery has
been the target of significant interest for the development of anti-cancer agents. However, Hsp90 is responsible for the folding of ~300 protein folding substrates, which may lead to undesired on-target toxicity and may be responsible for many of the Hsp90-targeted drugs that have failed in clinical trials. Through a structure-based approach, an isoform-selective inhibitor of Hsp90 has been identified and shown to exhibit good selectivity and affinity against particular cancers. Consequently, the goal of this application is to optimize this new inhibitory scaffold for great affinity/efficacy, to evaluate the role of a specific Hsp90 isoform in cancer, and to validate this isoform as a target for the treatment of bladder cancer.
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会议论文
Engineering the Next Generation of Safer Hsp90 Inhibitors
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批准号:10587304
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项目类别:
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资助金额:$46.33万
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财政年份:2023
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负责人:Brian S J Blagg
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依托单位:
Development and Evaluation of Purine and Coumarin Based Hsp90 Inhibitors
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批准号:9514012
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资助金额:$35.33万
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财政年份:2018
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Optimization and Investigation of Cruentaren A analogs
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批准号:9454428
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项目类别:
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资助金额:$34.25万
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财政年份:2018
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负责人:Brian S J Blagg
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依托单位:
Optimization and Investigation of Cruentaren A analogs
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批准号:9902368
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项目类别:
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资助金额:$35.3万
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财政年份:2018
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负责人:Brian S J Blagg
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依托单位:
Development and Evaluation of Purine and Coumarin Based Hsp90 Inhibitors
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批准号:9600723
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项目类别:
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资助金额:$44.39万
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财政年份:2018
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负责人:Brian S J Blagg
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依托单位:
Optimization and Investigation of Cruentaren A analogs
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批准号:10078544
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项目类别:
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资助金额:$35.3万
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财政年份:2018
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负责人:Brian S J Blagg
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依托单位:
New paradigms for Hsp90 inhibition
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批准号:9762054
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项目类别:
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资助金额:$34.35万
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财政年份:2017
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负责人:Brian S J Blagg
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依托单位:
New paradigms for Hsp90 inhibition
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批准号:10000886
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项目类别:
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资助金额:$35.41万
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财政年份:2017
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负责人:Brian S J Blagg
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依托单位:
New paradigms for Hsp90 inhibition
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批准号:9379940
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项目类别:
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资助金额:$36.66万
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财政年份:2017
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负责人:Brian S J Blagg
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依托单位:
Grp94-selective inhibitors to treat heredity glaucoma
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批准号:8928624
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项目类别:
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资助金额:$41.23万
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财政年份:2014
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负责人:Brian S J Blagg
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依托单位:
Grp94-selective inhibitors to treat heredity glaucoma
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批准号:8785724
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项目类别:
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资助金额:$43.54万
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财政年份:2014
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负责人:Brian S J Blagg
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依托单位:
Chaperone therapeutics for the treatment of DPN
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批准号:8636503
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项目类别:
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资助金额:$31.44万
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财政年份:2012
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负责人:Brian S J Blagg
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依托单位:
Chaperone therapeutics for the treatment of DPN
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批准号:8297562
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项目类别:
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资助金额:$31.82万
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财政年份:2012
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负责人:Brian S J Blagg
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依托单位:
Chaperone therapeutics for the treatment of DPN
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批准号:8413041
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项目类别:
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资助金额:$30.68万
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财政年份:2012
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负责人:Brian S J Blagg
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依托单位:
Development of Hsp90 inhibitors for the treatment of cancer
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批准号:8456077
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项目类别:
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资助金额:$29.3万
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财政年份:2012
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负责人:Brian S J Blagg
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依托单位:
Development of Hsp90 inhibitors for the treatment of cancer
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批准号:8627592
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项目类别:
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资助金额:$30.29万
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财政年份:2012
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负责人:Brian S J Blagg
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依托单位:
Chaperone therapeutics for the treatment of DPN
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批准号:8824587
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项目类别:
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资助金额:$31.73万
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财政年份:2012
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负责人:Brian S J Blagg
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依托单位:
COBRE: U KS: P1: ID OF HSP90 COCHAPERONES, IMMUNOPHILINS & PROTEINS
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批准号:7720669
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项目类别:
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资助金额:$2.61万
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财政年份:2008
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负责人:Brian S J Blagg
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依托单位:
HSP90 Inhibitors
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批准号:8184864
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项目类别:
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资助金额:$24.43万
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财政年份:2006
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负责人:Brian S J Blagg
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依托单位:
Hsp90 Inhibitors
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批准号:7038182
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项目类别:
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资助金额:$25.32万
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财政年份:2006
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负责人:Brian S J Blagg
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依托单位:
海外基金