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Synthesis of non-brain-permeant inhibitor of LZK

Synthesis of non-brain-permeant inhibitor of LZK
LZK非透脑抑制剂的合成
批准号：
10001308
负责人：
Matthew Hall
金额：
$13.27万
依托单位：
NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES
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
来源：
https://reporter.nih.gov/project-details/10001308
关键词：
Animal ModelAnimalsBrainChemicalsCollaborationsDiseaseExtramural ActivitiesGenomicsGoalsHead and Neck CancerInformaticsModelingMusPharmaceutical ChemistryPhosphotransferasesPlasmaProcessResearchTestingUnited States National Institutes of HealthWorkdrug discoveryinhibitor/antagonistkinase inhibitornew therapeutic targetscreeningsmall moleculesmall molecule inhibitorsmall molecule therapeuticstherapeutic development

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中文摘要
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英文摘要
LZK has been identified as a novel therapeutic target in head and neck cancer. This project aims to synthesize small molecule inhibitors of the LZK kinase that are non-brain permeant to enable proof-of-concept animal studies. During this period, the previously synthesized LZK inhibitors were tested in a PK mouse study, and they all still showed a high brain to plasma ratio. As such, a tolerability screen is now underway to examine whether these inhibitors are indeed toxic to mice. If not, then these compounds can still be used in advanced animal models.
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