1. Overview of all-trans-retinoic acid (ATRA) and its analogues: Structures, activities, and mechanisms in acute promyelocytic leukaemia
- Author
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Wenqiang Cao, Li Han, Zhao Qianqian, Lei Tian, Xiaodong Ren, Yuling Ma, Hui Nan, Liu Yuzhi, Qiao Guaiping, Li Juan, Liang Chengyuan, and Hong Liu
- Subjects
medicine.drug_class ,Cellular differentiation ,Retinoic acid ,Antineoplastic Agents ,Tretinoin ,01 natural sciences ,03 medical and health sciences ,chemistry.chemical_compound ,Leukemia, Promyelocytic, Acute ,Drug Discovery ,medicine ,Humans ,Retinoid ,Receptor ,neoplasms ,PI3K/AKT/mTOR pathway ,030304 developmental biology ,Cell Proliferation ,Pharmacology ,0303 health sciences ,010405 organic chemistry ,Chemistry ,organic chemicals ,TOR Serine-Threonine Kinases ,Organic Chemistry ,Autophagy ,Cancer ,General Medicine ,medicine.disease ,biological factors ,0104 chemical sciences ,Cancer research ,Acute promyelocytic leukaemia - 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.
- Published
- 2020