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

Research output: Contribution to journalReview article

Original languageEnglish
Article number115664
JournalBioorganic and Medicinal Chemistry
Volume28
Issue number20
DOIs
Published15 Oct 2020

King's Authors

Abstract

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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