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Review

Retinoids as Chemo-Preventive and Molecular-Targeted Anti-Cancer Therapies

1
Center for Translational Cancer Research, Helen F. Graham Cancer Center & Research Institute, Newark, DE 19713, USA
2
Department of Biological Sciences, University of Delaware, Newark, DE 19713, USA
3
CA*TX Inc., Princeton, NJ 08540, USA
4
Department of Pharmacology & Experimental Therapeutics, Thomas Jefferson University, Philadelphia, PA 19107, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Laura Paleari
Int. J. Mol. Sci. 2021, 22(14), 7731; https://doi.org/10.3390/ijms22147731
Received: 22 June 2021 / Revised: 11 July 2021 / Accepted: 13 July 2021 / Published: 20 July 2021
(This article belongs to the Special Issue Cancer Prevention with Molecular Target Therapies 2.0)
Retinoic acid (RA) agents possess anti-tumor activity through their ability to induce cellular differentiation. However, retinoids have not yet been translated into effective systemic treatments for most solid tumors. RA signaling is mediated by the following two nuclear retinoic receptor subtypes: the retinoic acid receptor (RAR) and the retinoic X receptor (RXR), and their isoforms. The identification of mutations in retinoid receptors and other RA signaling pathway genes in human cancers offers opportunities for target discovery, drug design, and personalized medicine for distinct molecular retinoid subtypes. For example, chromosomal translocation involving RARA occurs in acute promyelocytic leukemia (APL), and all-trans retinoic acid (ATRA) is a highly effective and even curative therapeutic for APL patients. Thus, retinoid-based target discovery presents an important line of attack toward designing new, more effective strategies for treating other cancer types. Here, we review retinoid signaling, provide an update on retinoid agents and the current clinical research on retinoids in cancer, and discuss how the retinoid pathway genotype affects the ability of retinoid agents to inhibit the growth of colorectal cancer (CRC) cells. We also deliberate on why retinoid agents have not shown clinical efficacy against solid tumors and discuss alternative strategies that could overcome the lack of efficacy. View Full-Text
Keywords: retinoic acid; cancer stem cells; adenomatous polyposis coli; aldehyde dehydrogenase; molecular targeted therapies retinoic acid; cancer stem cells; adenomatous polyposis coli; aldehyde dehydrogenase; molecular targeted therapies
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MDPI and ACS Style

Hunsu, V.O.; Facey, C.O.B.; Fields, J.Z.; Boman, B.M. Retinoids as Chemo-Preventive and Molecular-Targeted Anti-Cancer Therapies. Int. J. Mol. Sci. 2021, 22, 7731. https://doi.org/10.3390/ijms22147731

AMA Style

Hunsu VO, Facey COB, Fields JZ, Boman BM. Retinoids as Chemo-Preventive and Molecular-Targeted Anti-Cancer Therapies. International Journal of Molecular Sciences. 2021; 22(14):7731. https://doi.org/10.3390/ijms22147731

Chicago/Turabian Style

Hunsu, Victoria O., Caroline O.B. Facey, Jeremy Z. Fields, and Bruce M. Boman 2021. "Retinoids as Chemo-Preventive and Molecular-Targeted Anti-Cancer Therapies" International Journal of Molecular Sciences 22, no. 14: 7731. https://doi.org/10.3390/ijms22147731

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