摘要
蛋白酪氨酸磷酸酶1B(PTP-1B)是胰岛素和瘦素信号转导通路的负调节因子。小鼠PTP-1B基因敲除及反义核苷酸治疗实验表明PTP-1B是治疗糖尿病和肥胖症的潜在靶标。按PTP-1B小分子抑制剂的结构类别对近年来文献报道的代表性小分子PTP-1B抑制剂进行综述。指出采用小分子抑制PTP-1B酶可能成为治疗胰岛素抵抗、2型糖尿病以及肥胖症的新途径。
Protein tyrosine phosphatase 1B（PTP-1B） has been implicated as one of the key negative regulators of insulin and leptin signal transduction pathways. Recent PTP-1B gene knock-out studies and antisense oligonucleotide（ASO） treatment in mice have identified PTP-1B as a potential target for chemotherapy of diabetes and obesity. Therefore, inhibiting PTP-1B with small molecules represents a novel therapeutic approach for insulin resistance, type 2 diabetes, and obesity. Representative small-molecule PTP-1B inhibitors are discussed herein according to their structural features.
出处
《中国药物化学杂志》
CAS
CSCD
2006年第1期54-59,共6页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(30400568)
关键词
药物化学
构效关系
综述
蛋白酪氨酸磷酸酶1B
小分子抑制剂
medicinal chemistry
structure-activity relationship
review
protein tyrosine phosphatase 1B
small-molecule inhibitors
