Retinoic acid receptor alpha

Gene

Cell biology

Acute promyelocytic leukemia

Biology

Retinoic acid

Retinoid

Apoptosis

Receptor

Autophagy

Signal transduction

Cancer research

Biochemistry

Retinoic acid receptor

Tretinoin

Pharmacology

Chemistry

PI3K/AKT/mTOR pathway

European Journal of Medicinal Chemistry

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.

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