AKR1B10抑制剂的研究进展

Progress in the Studies on AKR1B10 Inhibitors

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 family1 member10（AKR1B10） is a member of AKR1 family, which belongs to the aldehyde ketone reductase superfamily（AKRs）. Aldo-keto reductase may participate in the different biological processes in different organisms, including carbonyl detoxification, osmotic adjustment, hormone metabolism, lipid synthesis, diabetes complications and formation of tumor. Currently, AKR1B10 has proved to be specific expression in tumor cells and narrowly distributed in normal tissue. Therefore, cancer drugs which are targeted with AKR1B10 have already won widely attention. In this study, the research progress in recent years for AKR1B10 inhibitors was summarized. AKR1B10 inhibitors are classified into natural compound inhibitors and chemical synthesis inhibitors. Furthermore, the chemical structure and the related structural modifications for suppressing influenced the active and selective strength of AKR1B10 inhibitors.