Inhibitors of p90Rsk

描述（由申请人提供）：本工作的长期目标包括了解ser/thr蛋白激酶Rsk家族在促分裂原活化蛋白激酶（MAPK）通路内的信号转导中的作用，并鉴定新类别的潜在抗肿瘤药物。直接目标包括-化学合成一组山奈酚糖苷的类似物，其显示介导Rsk 2的高度选择性抑制-合成通过计算机筛选从NCI库中鉴定的第二类抑制剂的类似物-鉴定具有不同类型化学结构和性质的另外的天然存在的p90 Rsk抑制剂这项工作与公共卫生有关，有效的和选择性的Rsk抑制剂可能表现出可用于治疗某些癌症，特别是乳腺癌的活性。

DESCRIPTION (provided by applicant): The long term goals of this work include the development of an understanding of the role(s) of the ser/thr protein kinase Rsk family in signal transduction within the mitogen-activated protein kinase (MAPK) pathway, and the identification of new classes of potential antitumor agents. The immediate objectives include - chemical synthesis of analogues of a group of kaempferol glycosides shown to mediate highly selective inhibition of Rsk2 - synthesis of analogues of a second class of inhibitors identified from the NCI repository by in silico screening - identification of additional naturally occurring inhibitors of p90 Rsk that have different types of chemical structures and properties This work is relevant to public health in that a potent and selective Rsk inhibitor is likely to exhibit activity useful for the treatment of certain cancers, notably breast cancer.