Discovery of inhibitors of BK polyomavirus
Discovery of inhibitors of BK polyomavirus
批准号:
9200219
负责人:
Glen Andrew Coburn
金额:
$34.71万
依托单位国家:
美国
项目类别:
财政年份:
2016
资助国家:
美国
项目状态:
已结题
起止时间:
2016-07-02 至 2018-06-30
关键词:
AdultAllograftingAntiviral AgentsAutomobile DrivingBK VirusBiological AssayCell LineCollaborationsCystitisDevelopmentDoseDrug KineticsEvaluationFailureFeasibility StudiesFundingGenomeGoalsGrowthImmuneImmune systemImmunocompetentImmunosuppressionImmunosuppressive AgentsIndividualInfectionInflammationKidneyKidney DiseasesKidney TransplantationKineticsLeadLibrariesLuciferasesLytic PhaseMichiganOralPatientsPharmaceutical ChemistryPharmaceutical PreparationsPhasePolyomavirusPolyomavirus InfectionsPopulationPropertyRefractoryReporterReporter GenesRiskSeriesSmall Business Innovation Research GrantStenosisStructure-Activity RelationshipT-LymphocyteTechnologyTestingTherapeutic immunosuppressionTransplant RecipientsTransplantationUniversitiesUrineVaccinesViremiaVirusVirus ReplicationVirus Sheddingcandidate selectioncell mediated immune responsecytotoxiccytotoxicityhigh riskhigh throughput screeningimmune functionimmunosuppressedimprovedindexinginhibitor/antagonistinnovationinterestkidney epithelial celllatent infectionlead seriesnovelnovel therapeuticspreventprogramsreconstitutionresponserestorationsmall molecule librariessuccesstv watchingurinary
中文摘要
项目总结
迫切需要新的BK多瘤病毒(BK)抑制剂来预防病毒诱导的BK多瘤病毒的发生
移植后肾病、同种异体移植失败和出血性膀胱炎。第一阶段SBIR的目标是
可行性研究是确定特定抑制BKPyV复制的类药物化合物。在这个过程中
在第一阶段资助期内,我们将通过一个包含100,000种具有最佳药物性质的化合物的库来执行一项热门搜索活动
属性。从化验中产生的高质量命中将接受后续测试,以调查其效力,
选择性和作用机理。其中最有趣的化合物将受到药物化学的影响
推动了探索结构-活性关系(SAR)的点击到主导的努力。这个项目的总体目标是发现一个
或更新的铅系列,其定义为一种化学型抑制剂,显示出易处理的SAR,有效的抗病毒
对现有BKPyV毒株的活性和最小的细胞毒性。这些努力的成功将引发
提交第二阶段申请,将计划从早期的潜在客户优化提升到候选人
选择。
英文摘要
PROJECT SUMMARY
Novel inhibitors of BK polyomavirus (BKPyV) are urgently needed to prevent the occurrence of virus-induced
nephropathy, allograft failure and hemorrhagic cystitis following transplantation. The objective of this Phase I SBIR
feasibility study is to identify drug-like compounds that specifically inhibit BKPyV replication. During the course of this
Phase I funding period, we will execute a hit finding campaign with a library of 100,000 compounds with optimal drug-like
properties. Quality hits that emerge from the assay will be subjected to follow-on testing that will investigate the potency,
selectivity, and mechanism of action. The most interesting of these compounds will be subjected to medicinal chemistry
driven hit-to-lead efforts to explore structure-activity relationships (SAR). The overall goal of this project is to discover one
or more novel lead series, which is defined as a chemotype inhibitor that demonstrates tractable SAR, potent antiviral
activity against the available BKPyV strains and minimal cytotoxicity. Success in these endeavors will trigger the
submission of a Phase II application that will advance the program from Early Lead Optimization through to Candidate
Selection.
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海外基金