Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China.
Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China.
Eur J Med Chem. 2021 Aug 5;220:113451. doi: 10.1016/j.ejmech.2021.113451. Epub 2021 Apr 15.
All-trans-retinoic acid (ATRA) is effective for preventing cancer and treating skin diseases and acute promyelocytic leukaemia (APL). These pharmacological effects of ATRA are mainly mediated by retinoid X receptors (RXRs) and retinoic acid receptors (RARs). This article provides a comprehensive overview of the clinical progress on and the molecular mechanisms of ATRA in the treatment of APL. ATRA can promote the transcriptional activation of differentiation-related genes and regulate autophagy by inhibiting mTOR, which results in anti-APL effects. In detail, the structures, pharmacological effects, and clinical studies of 68 types of ATRA analogues are described. These compounds have excellent antitumour therapeutic potential and could be used as lead compounds for further development and research.
全反式维甲酸（ATRA）在预防癌症、治疗皮肤病和急性早幼粒细胞白血病（APL）方面均有疗效。ATRA 的这些药理学作用主要通过视黄醇 X 受体（RXRs）和维甲酸受体（RARs）介导。本文全面概述了 ATRA 在治疗 APL 中的临床进展和分子机制。ATRA 可通过抑制 mTOR 促进分化相关基因的转录激活和调控自噬，从而发挥抗 APL 作用。详细介绍了 68 种 ATRA 类似物的结构、药理学作用和临床研究。这些化合物具有良好的抗肿瘤治疗潜力，可作为进一步开发和研究的先导化合物。
