| Smoothened抑制剂的耐药机制及克服耐药性的策略研究 |
| |
| 引用本文： | 张婉婉, 张磊, 徐云根, 张晶晶. Smoothened抑制剂的耐药机制及克服耐药性的策略研究[J]. 药学进展, 2020, 44(12): 932-941. |
| |
| 作者姓名： | 张婉婉 张磊 徐云根 张晶晶 |
| |
| 作者单位： | 1.中国药科大学药物化学系, 江苏 南京 211198 |
| |
| 摘 要： | Hedgehog （HH）信号通路在胚胎的发育、干细胞调节及组织稳态过程中发挥着重要作用，HH通路的异常则与多种肿瘤的发生和发展密切相关。Smoothened （SMO）蛋白是HH通路的主要跨膜蛋白，抑制SMO蛋白可以有效地抑制HH通路，从而有效抑制肿瘤的发生和发展。目前已有3个SMO抑制剂被美国食品药品监督管理局（Food and Drug Administration，FDA）批准上市。然而，这些药物的临床使用往往伴随着耐药的产生。综述SMO抑制剂的主要耐药机制以及克服其耐药性的常用策略。
|
| 关 键 词： | HH通路 SMO蛋白 耐药 机制 |
| 收稿时间： | 2020-05-18 |
Research on the Resistance Mechanisms of Smoothened Inhibitors and Strategies to Overcome Resistance |
| |
| ZHANG Wanwan, ZHANG Lei, XU Yungen, ZHANG Jingjing. Research on the Resistance Mechanisms of Smoothened Inhibitors and Strategies to Overcome Resistance[J]. Progress in Pharmaceutical Sciences, 2020, 44(12): 932-941. |
| |
| Authors: | ZHANG Wanwan ZHANG Lei XU Yungen ZHANG Jingjing |
| |
| Affiliation: | 1.Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 211198, China |
| |
| Abstract: | The Hedgehog (HH) signaling pathway plays an important role in embryonic development, stem cell biology and tissue homeostasis. The aberration of HH signaling pathway is closely related to the development of various cancers. Smoothened (SMO) is the main transducer of the HH signaling pathway and inhibition of SMO can effectively inhibit HH pathway, thereby effectively inhibiting the development of tumors. Up to now, three SMO inhibitors have been approved by U.S. Food and Drug Administration (FDA). However, their clinical application has been limited by drug resistance. The main resistance mechanisms of SMO inhibitors are outlined and the way for future endeavors is pointed. |
| |
| Keywords: | Hedgehog signaling pathway Smoothened drug resistance mechanism |
|
| 点击此处可从《药学进展》浏览原始摘要信息 |
|
点击此处可从《药学进展》下载全文 |
