Department of Chemistry, University of Toronto, Mississauga, Canada.
Anticancer Drugs. 2011 Feb;22(2):115-27. doi: 10.1097/CAD.0b013e328341185b.
Aberrantly activated signal transducer and activator of transcription 3 (Stat3) protein plays a master regulatory role in the progression and survival of human cancers through the upregulation of target protooncogenes. Numerous human cancers, including breast, ovarian, prostate, leukemia, lymphoma, multiple myeloma, and brain cancers have been shown to harbor constitutively active Stat3 protein resulting in the expression of protooncogenes. The transcriptionally active Stat3-Stat3 protein homodimer has been extensively targeted as a means to suppress the aberrant Stat3 function in human cancer. This review will outline the recent progress made toward identifying drug-like compounds capable of effectively inhibiting aberrant Stat3 signaling through the disruption of Stat3 protein-protein interactions.
异常激活的信号转导子和转录激活子 3（Stat3）蛋白通过上调靶原癌基因在人类癌症的进展和存活中发挥主要调节作用。许多人类癌症，包括乳腺癌、卵巢癌、前列腺癌、白血病、淋巴瘤、多发性骨髓瘤和脑癌，已经显示出含有组成性激活的 Stat3 蛋白，导致原癌基因的表达。转录活性的 Stat3-Stat3 蛋白同源二聚体已被广泛作为抑制人类癌症中异常 Stat3 功能的手段。这篇综述将概述最近在鉴定能够通过破坏 Stat3 蛋白-蛋白相互作用有效抑制异常 Stat3 信号的类药化合物方面取得的进展。
