Recent advances in the design of RAR α and RAR β agonists as orally bioavailable drugs. A review
| Autor: | Alan D. Borthwick, Jonathan Corcoran, Maria B. Goncalves |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Nerve injury
Receptors Retinoic Acid Clinical Biochemistry Carboxylic Acids Retinoic acid Administration Oral Biological Availability Pharmaceutical Science Review Article Pharmacology 01 natural sciences Biochemistry chemistry.chemical_compound Drug Discovery Embryonic morphogenesis Humans AC-261066 Beta agonist Receptor Molecular Biology ComputingMethodologies_COMPUTERGRAPHICS Molecular Structure 010405 organic chemistry Chemistry Cell growth Retinoic Acid Receptor alpha Alpha agonist Organic Chemistry Retinoic acid receptor RAR586 C286 0104 chemical sciences 010404 medicinal & biomolecular chemistry Nuclear receptor Apoptosis Drug Design Lipophilicity Molecular Medicine SAR |
| Zdroj: | Bioorganic & Medicinal Chemistry |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2020.115664 |
| Popis: | Graphical 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. |
| Databáze: | OpenAIRE |
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