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Small-Molecule Targeted Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
The retinoids are natural and synthetic derivatives of vitamin A that regulate a variety of important cellular functions. Retinol (Figure 6.106), also known as vitamin A1, is a vitamin found in many food types and used as a dietary supplement to treat and prevent vitamin A deficiency. In the body retinol is converted to retinal and then retinoic acid which acts on cell-surface receptors to control processes including cell growth and metabolism (Figure 6.105). In particular, it is a regulator of epithelial and bone tissue cell growth and differentiation, and so analogues have been developed for use in skin-related proliferative diseases such as psoriasis and bone tissue disorders. Through the activation of tumor-suppressor genes, it is also known to play a role in maintaining vision and immune function. Retinol was discovered in 1909, isolated in 1931 and first synthesized in 1947, and dietary sources rich in the molecule include dairy products, meat, and fish. All-trans-retinoic acid (RA) works by activating the Nuclear Retinoic Acid receptors (RARs), while 9-cis-retinoic acid activates the non-classical nuclear Retinoid X Receptors (RXRs) along with the RARs. Altogether, there are six genes encoding the retinoid receptors: RARa, RARb, and RARg, and RXRa, RXRb, and RXRg (Figure 6.105).
HVEM has a broader expression than PD-L1 and constitutes a negative prognostic marker and potential treatment target for melanoma
Published in OncoImmunology, 2019
Nausicaa Malissen, Nicolas Macagno, Samuel Granjeaud, Clémence Granier, Vincent Moutardier, Caroline Gaudy-Marqueste, Nadia Habel, Marion Mandavit, Bernard Guillot, Christine Pasero, Eric Tartour, Robert Ballotti, Jean-Jacques Grob, Daniel Olive
This HVEM signature is essentially a mixture of genes involved in melanoma proliferation (MITF, CAPN3, MLANA, GNPTAB, CPN1, SOX10, and GYPC40,41) and of genes involved in invasive melanoma features (CITED1, 42ACP5, 43LZTS1, 44GAB2, 45SNX10, 46 and RXRG26,36); among these, it is interesting to note that targeting RXR signaling may delay relapse in melanoma47 and that the MXI1 hypoxia responsive48 gene is a putative tumor suppressor gene involved in melanoma progression.35