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

ABSTRACT: Retinoic acid receptors (RARs) ?, ?, and ? 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 RAR?, RAR?, and RAR? 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 RAR? and RAR? 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.

SUBMITTER: Borthwick AD

PROVIDER: S-EPMC7588594 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature

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

Borthwick Alan D AD Goncalves Maria B MB Corcoran Jonathan P T JPT

Bioorganic & medicinal chemistry 20200729 20

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 witho ...[more]

PMID: 33069074

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