Inhibitors of p90Rsk

描述（由申请人提供）：这项工作的长期目标包括了解丝氨酸/苏氨酸蛋白激酶Rsk家族在丝裂原活化蛋白激酶（MAPK）信号转导中的作用，以及鉴定新型潜在抗肿瘤药物。近期目标包括-化学合成一组山奈酚苷的类似物，显示介导Rsk2的高度选择性抑制-合成第二类抑制剂的类似物，通过硅筛选从NCI库中鉴定-鉴定具有不同类型化学结构和性质的p90风险的其他自然存在的抑制剂这项工作与公共卫生相关，因为有效和选择性的风险抑制剂是有效的可能表现出对治疗某些癌症有用的活性，特别是乳腺癌。

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.