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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
翻译
LZK已被确定为头颈癌的新治疗靶点。该项目旨在合成非脑渗透的LZK激酶的小分子抑制剂，以实现概念验证动物研究。 在此期间，先前合成的LZK抑制剂在PK小鼠研究中进行了测试，并且它们仍然显示出高的脑血浆比。因此，目前正在进行耐受性筛选，以检查这些抑制剂是否确实对小鼠有毒。如果没有，那么这些化合物仍然可以用于高级动物模型。
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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