The RARγ Oncogene: An Achilles Heel for Some Cancers
Abstract
:1. Introduction
2. The Concept of the Cancer Stem Cell
3. Targeted Therapies for Cancer
4. RARγ Is a Fundamental Control on Stem Cell Behavior
5. RARγ Is an Oncogene for Some Cancers
6. Antagonising RARγ Kills Cancer Stem Cells
7. The Oncogenic Action of RARγ
8. Concluding Remarks
Funding
Institutional Review Board Statement
Informed Consent Statement
Conflicts of Interest
References
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Malignancy | RARγ Expression | Impact on Disease |
---|---|---|
Acute myeloid leukemia | RARγ chimeric protein | Not responsive to retinoid-based therapy |
Colorectal carcinoma | Overexpression | Resistance to chemotherapeutics |
Cholangiocarcinoma | Overexpression | Poor prognosis and drug resistance |
Hepatocellular carcinoma | Overexpression | Promotes growth of xenografts |
Renal cell carcinoma | Overexpression | May contribute to disease progression |
Compound | Kd, nM | IC50, nM | ||||
---|---|---|---|---|---|---|
RARα | RARβ | RARγ | DU145 | LNCaP | PC3 | |
Pan-RAR antagonist (AGN194310) | 4.3 | 5 | 2 | 34 | 16 | 18 |
RARγ antagonist (AGN205728) | 2400 | 4248 | 3 | 6 | 3 | 5 |
RARβγ antagonist (AGN194431) | 300 | 6 | 70 | 88 | 99 | 103 |
RARα antagonist (AGN196996) | 3.9 | 4036 | >10 K | 201 | 203 | 235 |
Pan-RAR agonist (ATRA) | ND | ND | ND | 402 | 344 | 419 |
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Brown, G.; Petrie, K. The RARγ Oncogene: An Achilles Heel for Some Cancers. Int. J. Mol. Sci. 2021, 22, 3632. https://doi.org/10.3390/ijms22073632
Brown G, Petrie K. The RARγ Oncogene: An Achilles Heel for Some Cancers. International Journal of Molecular Sciences. 2021; 22(7):3632. https://doi.org/10.3390/ijms22073632
Chicago/Turabian StyleBrown, Geoffrey, and Kevin Petrie. 2021. "The RARγ Oncogene: An Achilles Heel for Some Cancers" International Journal of Molecular Sciences 22, no. 7: 3632. https://doi.org/10.3390/ijms22073632