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Review
. 2022 Mar 15;12(3):938-960.
eCollection 2022.

Retinoids as anti-cancer agents and their mechanisms of action

Ying Jin  1 , Soek Sin Teh  2 , Harrison Lik Nang Lau  2 , Jianbo Xiao  3 , Siau Hui Mah  1   4
Affiliations
Review

Retinoids as anti-cancer agents and their mechanisms of action

Ying Jin et al. Am J Cancer Res. .

Abstract

Retinoids (vitamin A) have been reported extensively for anti-cancer properties due to their high receptor-binding affinities and gene regulation abilities. However, the anti-cancer potential of retinoids has not been reviewed in recent years. Thus, this review focused on the anti-cancer effects of retinoids and their synergistic effects with other drugs, together with their mechanisms of action in different types of cancers reported in the past five years. The retinoids were well studied in breast cancer, melanoma, and colorectal cancer. Synthetic retinoids have shown higher selectivity, stronger effectiveness, and lower toxicity than endogenous retinoids. Interestingly, the combination treatment of endogenous retinoids with chemotherapy drugs showed enhanced anti-cancer effects. The mechanisms of action reported for retinoids mainly involved the RAR/RXR signaling pathway. However, limited clinical studies were conducted in recent years. Thus, retinoids which are highly potential anti-cancer agents are worth further study in clinical, especially as a combination therapy with chemotherapy drugs.

Keywords: All-trans-retinoic acid; RAR/RXR signaling pathway; combination treatment; vitamin A.

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Conflict of interest statement

None.

Figures

Figure 1
Figure 1
The chemical structures and molecular formula of endogenous and synthetic retinoids.
Figure 2
Figure 2
Retinoid metabolism pathway from the diet intake to intestine, lymphatic system, liver, blood plasma and target cell. LRAT: lecithin retinol acyltransferase; RBP: retinol-binding proteins; TTR: transthyretin; STRA6: stimulated by retinoic acid 6; RDH: retinol dehydrogenase; ADH: alcohol dehydrogenase; RALDH: retinol dehydrogenase.
Figure 3
Figure 3
RAR/RXR signaling pathway within target cell. RARE: retinoic acid response element; NCoR: nuclear receptor corepressor; HDAC: histone deacetylase.
See this image and copyright information in PMC

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