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Retinoid Receptor-Selective Agonists and Their Action in Skin

  • Chapter
Retinoids

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 139))

Abstract

Vitamin A (Retinol) and its biologically active metabolites, for example, all trans retinoic acid, (AtRA) are essential for the health of the individual. These natural compounds are involved in a wide range of biological processes, including vertebrate development and morphogenesis, cell proliferation and tissue differentiation, vision, and reproduction (Chambon 1996; Mangelsdorf et al. 1995; Marshall et al. 1996; Morriss-Kay and Sokolova 1996). These biological actions of vitamin A and related compounds (encompassed by the term“retinoids”) are mediated by two families of nuclear receptors, termed retinoic acid receptors (RAR) and retinoid X receptors (RXR).The effects of RA are mediated through binding to RAR isoforms (α, ß, γ) (Brand et al. 1988; Giguere et al. 1987; Krust et al. 1989), while the 9-cis isomer of RA binds to the RXR family (with α, ß, γ isoforms also; Fleischhauer et al. 1992; Leid et al. 1992; Mangelsdorf et al. 1990), in addition to the RAR family (Allenby et al. 1993). The RARs and RXRs are members of the ever expanding superfamily of nuclear receptors, that includes the receptors for estrogen, thyroid hormone, and vitamin D3 (Giguere 1994). In addition to RARs and RXRs, RA can also bind with high affinity to cytoplasmic retinoic acid binding proteins (CRABP 1 and 2). These binding proteins are thought to play a role in both retinoid transport and metabolism.

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Shroot, B., Gibson, D.F.C., Lu, XP. (1999). Retinoid Receptor-Selective Agonists and Their Action in Skin. In: Nau, H., Blaner, W.S. (eds) Retinoids. Handbook of Experimental Pharmacology, vol 139. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-58483-1_19

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