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K-Map: connecting kinases with therapeutics for drug repurposing and development

机译:K-Map:将激酶与治疗药物联系起来以实现药物的重新开发

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Availability and implementation K-Map has been implemented in python scripting language and the website is freely available at: http://tanlab.ucdenver.edu/kMap . Protein kinases play important roles in regulating signal transduction in eukaryotic cells. Due to evolutionary conserved binding sites in the catalytic domain of the kinases, most inhibitors that target these sites promiscuously inhibit multiple kinases. Quantitative analysis can reveal complex and unexpected interactions between protein kinases and kinase inhibitors, providing opportunities for identifying multi-targeted inhibitors of specific diverse kinases for drug repurposing and development. We have developed K-Map—a novel and user-friendly web-based program that systematically connects a set of query kinases to kinase inhibitors based on quantitative profiles of the kinase inhibitor activities. Users can use K-Map to find kinase inhibitors for a set of query kinases (obtained from high-throughput ‘omics’ experiments) or to reveal new interactions between kinases and kinase inhibitors for rational drug combination studies.
机译:可用性和实现K-Map已以python脚本语言实现,该网站可从以下网址免费获得:http://tanlab.ucdenver.edu/kMap。蛋白激酶在调节真核细胞的信号转导中起重要作用。由于激酶催化域中进化上保守的结合位点,大多数靶向这些位点的抑制剂会混杂抑制多种激酶。定量分析可以揭示蛋白激酶与激酶抑制剂之间复杂而出乎意料的相互作用,从而为鉴定针对多种用途的特定激酶的多靶点抑制剂提供了机会。我们已经开发了K-Map,这是一个新颖且用户友好的基于Web的程序,该程序可基于激酶抑制剂活性的定量概况,系统地将一组查询激酶与激酶抑制剂连接起来。用户可以使用K-Map为一组查询激酶(从高通量“组学”实验中获得)找到激酶抑制剂,或揭示激酶与激酶抑制剂之间的新相互作用,以进行合理的药物组合研究。

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