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Inhibitors for Extracellular Signal-Regulated Kinase Docking Domains and Uses Therefor

机译:细胞外信号调节激酶停靠域的抑制剂及其用途

摘要

Provided herein are compounds and methods of using compounds that selectively inhibit binding to one or more docking domain regions of an extracellular signal-recognition kinase to inhibit in a cell having an extracellular signal-regulated kinase activity. Such methods may be used to inhibit cell proliferation of a neoplastic cell, to treat a cancer and further may be used in conjunction with administration of an anticancer drug at a reduced dosage to treat a cancer with a concomitant reduction in toxicity to an individual receiving the treatment. Also provided is a method to design and screen for compounds to inhibit binding within the extracellular signal-regulated kinase docking domain region, using at least in part computer-aided drug design modeling.
机译:本文提供了化合物和使用化合物的方法,所述化合物选择性抑制与细胞外信号识别激酶的一个或多个对接结构域区域的结合,以抑制具有细胞外信号调节激酶活性的细胞。这样的方法可以用于抑制赘生性细胞的细胞增殖,以治疗癌症,并且还可以与降低剂量的抗癌药联合使用以治疗癌症,同时对接受该治疗的个体的毒性降低。治疗。还提供了使用至少部分计算机辅助药物设计模型来设计和筛选抑制细胞外信号调节的激酶对接域区域内结合的化合物的方法。

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