2. Academic Validation
  3. Overview of all-trans-retinoic acid (ATRA) and its analogues: Structures, activities, and mechanisms in acute promyelocytic leukaemia

Overview of all-trans-retinoic acid (ATRA) and its analogues: Structures, activities, and mechanisms in acute promyelocytic leukaemia

  • Eur J Med Chem. 2021 Aug 5:220:113451. doi: 10.1016/j.ejmech.2021.113451.
Chengyuan Liang 1,  Guaiping Qiao 2,  Yuzhi Liu 2,  Lei Tian 2,  Nan Hui 2,  Juan Li 2,  Yuling Ma 2,  Han Li 2,  Qianqian Zhao 2,  Wenqiang Cao 3,  Hong Liu 4,  Xiaodong Ren 5
Affiliations

Affiliations

  • 1 Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China. Electronic address: chengyuanliang@gmail.com.
  • 2 Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China.
  • 3 Zhuhai Jinan Selenium Source Nanotechnology Co., Ltd., Hengqin New Area, Zhuhai, Guangdong, China.
  • 4 Zhuhai Jinan Selenium Source Nanotechnology Co., Ltd., Hengqin New Area, Zhuhai, Guangdong, China. Electronic address: sesource_liuhong@163.com.
  • 5 Medical College, Guizhou University, Guiyang, 550025, PR China. Electronic address: xdren@gzu.edu.cn.
PMID: 33895500 DOI: 10.1016/j.ejmech.2021.113451
Abstract

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.

Keywords

Acute promyelocytic leukaemia (APL); All-trans-retinoic acid (ATRA); Autophagy; Cell differentiation; Retinoic acid receptors (RARs).

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