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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Published inBioorganic & medicinal chemistry Vol. 28; no. 20; p. 115664
Main Authors Borthwick, Alan D., Goncalves, Maria B., Corcoran, Jonathan P.T.
Format Journal Article
LanguageEnglish
Published England Elsevier Ltd 15.10.2020
Elsevier Science
Subjects
AC-261066
Alpha agonist
Beta agonist
C286
Nerve injury
RAR586
Retinoic acid receptor
Review
SAR
C286
Retinoic acid receptor
Beta agonist
SAR
RAR586
AC-261066
Nerve injury
Alpha agonist
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Summary:[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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2020.115664