Kinase Targeted Antimalarial Agents
激酶靶向抗疟药
基本信息
- 批准号:9918203
- 负责人:
- 金额:$ 95.77万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2019
- 资助国家:美国
- 起止时间:2019-12-16 至 2021-11-30
- 项目状态:已结题
- 来源:
- 关键词:AffectAffinityAnopheles GenusAntimalarialsArtemisininsBindingBiological AssayBiologyCSNK1A1 geneCessation of lifeChemicalsClinicalCollectionCombined Modality TherapyCommunitiesCountryCulicidaeDataDevelopmentDiseaseDrug TargetingDrug resistanceErythrocytesGoalsHealthHumanHuman BitesIncidenceInfectionInvestmentsLeadLibrariesLife Cycle StagesLuciferasesMalariaMapsMedicineMorbidity - disease rateParasitesPathologyPharmaceutical PreparationsPhasePhenotypePhosphotransferasesPlasmodiumPlasmodium falciparumPlasmodium falciparum genomePlasmodium vivaxPrivate SectorProtein KinasePublic SectorPublishingReportingResearchResistanceSeriesTechnologyTreesasexualbasecandidate selectionclinical candidatecombatdesigndisorder controldrug developmentgenome sequencingimprovedin vivoinhibitor/antagonistkinase inhibitorknockout genemembermortalitynext generationnovelnovel therapeuticsopen sourcephosphoproteomicsprogramsprotein kinase inhibitorscaffoldscreeningsmall moleculetool
项目摘要
Project Summary
The genome of Plasmodium falciparum, the species responsible for most mortality in malaria, is
predicted to encode 86-99 protein kinases. Of these, 36 kinases are expressed in the asexual
stage of the parasite’s life-cycle, which is responsible for the pathology associated with the
disease. Using our proprietary KinaseSeeker technology, we have recently developed assays
against 11 Plasmodium falciparum kinases, which are expressed in the asexual stage. Screening
a small-molecule kinase inhibitor library has revealed several chemically tractable chemotypes
that bind P. falciparum kinases with sub-micromolar affinity.
In this application, using a target-based approach, we aim to utilize the chemotypes identified
from our screening data, as starting points for development of potent and selective antimalarial
agents. In addition, we will use the already commercialized P. falciparum kinase assays, to
identify targets for potential kinase inhibitors that have been shown to be active in phenotypic
screens against the parasite. The different series of compounds will then be further optimized for
potency and selectivity to deliver leads for new antimalarials and improve human health.
项目总结
项目成果
期刊论文数量(0)
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会议论文数量(0)
专利数量(0)
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{{ truncateString('REENA ZUTSHI', 18)}}的其他基金
Split-luciferase Epigenetic Assays for Drug Discovery
用于药物发现的分裂荧光素酶表观遗传学分析
- 批准号:
10482555 - 财政年份:2022
- 资助金额:
$ 95.77万 - 项目类别:
Enabling Toxoplasma gondii Kinome Directed Drug Discovery
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- 资助金额:
$ 95.77万 - 项目类别:
Tools for Accelerating R&D for Historically Understudied Protein Kinases
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9264156 - 财政年份:2017
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Enabling Malarial Kinome Directed Drug Discovery
实现疟疾激酶组定向药物发现
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8714538 - 财政年份:2014
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8123053 - 财政年份:2011
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$ 95.77万 - 项目类别:
Rapid Kinase Profiling with Luminescent Reporters
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- 资助金额:
$ 95.77万 - 项目类别:
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使用发光报告基因快速分析激酶
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7745380 - 财政年份:2009
- 资助金额:
$ 95.77万 - 项目类别:
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