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Aldo-keto reductase family1,member10(AKR1B10)属醛酮还原酶超家族(AKRs)中AKR1家族的成员之一。醛酮还原酶在不同的生物体中可能参与了不同的生物学过程,包括羰基解毒、渗透调节、激素代谢、脂质合成、糖尿病并发症、肿瘤的形成等。目前,AKR1B10已被证明在肿瘤细胞中特异性表达,而在正常组织细胞中分布较窄。因此,以其为靶点的抗肿瘤药物研究近年来被广泛关注。本文从来源于天然和化学合成2个方向的AKR1B10抑制剂进行分类与总结,并对其化学结构及结构修饰对于抑制活性和选择性的影响进行综述。
Aldo-keto reductase family 1, member 10 (AKR1B10) is a member of the AKR1 family of aldehyde-keto reductase superfamilies (AKRs). Aldehyde ketoreductases may participate in different biological processes in different organisms, including carbonyl detoxification, osmotic adjustment, hormone metabolism, lipid synthesis, diabetic complications, tumor formation and so on. At present, AKR1B10 has been shown to be specifically expressed in tumor cells, whereas it is relatively narrow in normal tissue cells. Therefore, the research of antitumor drugs targeting it has been widely concerned in recent years. In this paper, we classify and summarize the AKR1B10 inhibitors derived from natural and chemical synthesis in two directions, and review the impact of their chemical structure and structure modification on the inhibitory activity and selectivity.