Recent advances in the design of RAR α and RAR β agonists as orally bioavailable drugs. A review

[Display omitted] Retinoic acid receptors (RARs) α, β, and γ are members of the nuclear receptor superfamily. Compounds which bind to and activate the RARs are termed retinoids which regulate a wide variety of biological processes such as vertebrate embryonic morphogenesis and organogenesis, cell gr...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2020-10, Vol.28 (20), p.115664, Article 115664
Hauptverfasser: Borthwick, Alan D., Goncalves, Maria B., Corcoran, Jonathan P.T.
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creator Borthwick, Alan D.
Goncalves, Maria B.
Corcoran, Jonathan P.T.
description [Display omitted] Retinoic acid receptors (RARs) α, β, and γ are members of the nuclear receptor superfamily. Compounds which bind to and activate the RARs are termed retinoids which regulate a wide variety of biological processes such as vertebrate embryonic morphogenesis and organogenesis, cell growth arrest, differentiation, and apoptosis, as well as their disorders. Although many synthetic selective RARα, RARβ, and RARγ agonists have been designed and prepared, these have generally been lipophilic acids without good drug-like properties and with low oral bioavailability. Recently this has been changing and drug design approaches to highly potent and selective RARα and RARβ agonists with low lipophilicity that are orally bioavailable and less toxic have been developed, that have a range of potential therapeutic uses. This review covers these new advances.
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subjects AC-261066
Alpha agonist
Beta agonist
C286
Nerve injury
RAR586
Retinoic acid receptor
Review
SAR
title Recent advances in the design of RAR α and RAR β agonists as orally bioavailable drugs. A review
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