PMID- 33895500 OWN - NLM STAT- MEDLINE DCOM- 20210823 LR - 20211204 IS - 1768-3254 (Electronic) IS - 0223-5234 (Linking) VI - 220 DP - 2021 Aug 5 TI - Overview of all-trans-retinoic acid (ATRA) and its analogues: Structures, activities, and mechanisms in acute promyelocytic leukaemia. PG - 113451 LID - S0223-5234(21)00300-7 [pii] LID - 10.1016/j.ejmech.2021.113451 [doi] AB - 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. CI - Copyright (c) 2021 Elsevier Masson SAS. All rights reserved. FAU - Liang, Chengyuan AU - Liang C AD - Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China. Electronic address: chengyuanliang@gmail.com. FAU - Qiao, Guaiping AU - Qiao G AD - Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China. FAU - Liu, Yuzhi AU - Liu Y AD - Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China. FAU - Tian, Lei AU - Tian L AD - Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China. FAU - Hui, Nan AU - Hui N AD - Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China. FAU - Li, Juan AU - Li J AD - Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China. FAU - Ma, Yuling AU - Ma Y AD - Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China. FAU - Li, Han AU - Li H AD - Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China. FAU - Zhao, Qianqian AU - Zhao Q AD - Faculty of Pharmacy, Shaanxi University of Science & Technology, Xi'an, 710021, PR China. FAU - Cao, Wenqiang AU - Cao W AD - Zhuhai Jinan Selenium Source Nanotechnology Co., Ltd., Hengqin New Area, Zhuhai, Guangdong, China. FAU - Liu, Hong AU - Liu H AD - Zhuhai Jinan Selenium Source Nanotechnology Co., Ltd., Hengqin New Area, Zhuhai, Guangdong, China. Electronic address: sesource_liuhong@163.com. FAU - Ren, Xiaodong AU - Ren X AD - Medical College, Guizhou University, Guiyang, 550025, PR China. Electronic address: xdren@gzu.edu.cn. LA - eng PT - Journal Article PT - Review DEP - 20210415 PL - France TA - Eur J Med Chem JT - European journal of medicinal chemistry JID - 0420510 RN - 0 (Antineoplastic Agents) RN - 5688UTC01R (Tretinoin) RN - EC 2.7.1.1 (MTOR protein, human) RN - EC 2.7.11.1 (TOR Serine-Threonine Kinases) SB - IM MH - Antineoplastic Agents/chemistry/*pharmacology MH - Cell Proliferation/drug effects MH - Humans MH - Leukemia, Promyelocytic, Acute/*drug therapy/metabolism/pathology MH - TOR Serine-Threonine Kinases/*antagonists & inhibitors/metabolism MH - Tretinoin/analogs & derivatives/chemistry/*pharmacology OTO - NOTNLM OT - Acute promyelocytic leukaemia (APL) OT - All-trans-retinoic acid (ATRA) OT - Autophagy OT - Cell differentiation OT - Retinoic acid receptors (RARs) COIS- Declaration of competing interest The authors declared that they have no conflicts of interest to this work. EDAT- 2021/04/26 06:00 MHDA- 2021/08/24 06:00 CRDT- 2021/04/25 20:37 PHST- 2020/11/17 00:00 [received] PHST- 2021/04/01 00:00 [revised] PHST- 2021/04/04 00:00 [accepted] PHST- 2021/04/26 06:00 [pubmed] PHST- 2021/08/24 06:00 [medline] PHST- 2021/04/25 20:37 [entrez] AID - S0223-5234(21)00300-7 [pii] AID - 10.1016/j.ejmech.2021.113451 [doi] PST - ppublish SO - Eur J Med Chem. 2021 Aug 5;220:113451. doi: 10.1016/j.ejmech.2021.113451. Epub 2021 Apr 15.