Transmission blocking inhibitors of Malaria
Transmission blocking inhibitors of Malaria
批准号:
10691133
负责人:
Alexey Zakharov
金额:
$14.62万
依托单位国家:
美国
项目类别:
财政年份:
--
资助国家:
美国
项目状态:
未结题
起止时间:
至
关键词:
Anopheles GenusAntimalarialsAreaArtemisininsBiologicalBiological AssayBiological ProcessBloodCessation of lifeChildChloroquineCollectionCombined Modality TherapyCulicidaeDevelopmentDrug resistanceEvaluationEventFertilizationGlucosephosphate DehydrogenaseGlucosephosphate Dehydrogenase DeficiencyInterruptionLeadLibrariesLiverMalariaMorbidity - disease rateParasitesPathway interactionsPatientsPeriodicityPersonsPharmaceutical PreparationsPlasmodiumPlasmodium falciparumPlasmodium vivaxPregnant WomenPrimaquinePublic HealthRelapseReporterReportingRiskRodentScientistSporozoitesVertebratesWorkbasedisease transmissioninhibitormalaria transmissionminiaturizemortalitynanoluciferasenovelnovel therapeuticsresponsescreeningside effectsmall moleculesmall molecule librariestooltransmission processvector mosquito
中文摘要
疟疾仍然是一个巨大的公共卫生负担。为了维持最近在减少疟疾相关发病率和死亡率方面取得的进展,需要在开发有可能阻断疾病传播的抗疟疾药物方面取得进一步进展。为了确定铅开发候选对象以及寄生虫传播到蚊子媒介NCGC所必需的新生物途径,科学家们优化并缩小了新的受精检测方法,使其达到1536孔的格式,从而提供了对化合物进行高通量评估以对抗早期蚊子阶段的机会。初步研究已经筛选了询问板机制(MIPE)化合物文库,包含2,480个带有注释作用机制的小分子,鉴定了135个化合物,用2微米以下的IC50抑制受精。验证这些命中的工作正在进行中,以及筛选经批准的药物集合以进行再利用努力。
英文摘要
Plasmodium malaria remains a tremendous public health burden. In order to sustain recent progress in decreasing malaria related morbidity and mortality further progress in development of antimalarials with potential to interrupt disease transmission are required. To identify lead development candidates as well as novel biological pathways essential for parasite transmission to the mosquito vector NCGC scientists have optimized and miniaturized the novel fertilization assay to 1536-well format, providing the opportunity to conduct high-throughput evaluation of compounds against early mosquito stages. Initial studies have already screened the Mechanism of Interrogation PlatE (MIPE) compound library, with 2,480 small molecules with annotated mechanisms of action, identifying 135 compounds that inhibited fertilization with IC50s under 2 uM. Work is proceeding with validating these hits as well as screening approved drug collections for repurposing efforts.
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会议论文
Triple drug combination screening
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批准号:10691136
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项目类别:
-
资助金额:$14.62万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
NCATS Malaria Active Collection
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批准号:10691135
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项目类别:
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资助金额:$14.62万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Screening for small molecule inhibitors of B. burgdorferi HtrA
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批准号:10919702
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项目类别:
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资助金额:$24.08万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Identification of ALPK1 inhibitors
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批准号:10919704
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项目类别:
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资助金额:$10.0万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Screening for small molecule inhibitors of B. burgdorferi HtrA
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批准号:10691142
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项目类别:
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资助金额:$25.96万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Identification of ALPK1 inhibitors
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批准号:10691144
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项目类别:
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资助金额:$9.0万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Improving 15-LOX-2 small molecule inhibitors through medicinal chemistry and structure-guided design
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批准号:10919696
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项目类别:
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资助金额:$12.58万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Improving 15-LOX-2 small molecule inhibitors through medicinal chemistry and structure-guided design
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批准号:10691131
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项目类别:
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资助金额:$14.62万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Antifungal Antagonism Screening
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批准号:10919697
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项目类别:
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资助金额:$24.08万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Naeglearia fowleri proline tRNA synthetase inhibitors
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批准号:10691134
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项目类别:
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资助金额:$14.62万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Identification of Myc translation inhibitors
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批准号:10919694
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项目类别:
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资助金额:$24.08万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Antifungal Antagonism Screening
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批准号:10691132
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项目类别:
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资助金额:$25.96万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Identification of Myc translation inhibitors
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批准号:10691129
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项目类别:
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资助金额:$25.96万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
海外基金