Abstract
Nuclear receptors (NRs) are important pharmaceutical targets because they are key regulators of many metabolic and inflammatory diseases, including diabetes, dyslipidemia, cirrhosis, and fibrosis. As ligands play a pivotal role in modulating nuclear receptor activity, the discovery of novel ligands for nuclear receptors represents an interesting and promising therapeutic approach. The search for novel NR agonists and antagonists with enhanced selectivities prompted the exploration of the extraordinary chemical diversity associated with natural products. Recent studies involving nuclear receptors have disclosed a number of natural products as nuclear receptor ligands, serving to re-emphasize the translational possibilities of natural products in drug discovery. In this review, the natural ligands of nuclear receptors will be described with an emphasis on their mechanisms of action and their therapeutic potentials, as well as on strategies to determine potential marine natural products as nuclear receptor modulators.
Highlights
Natural products, including compounds from plants, microbes, and marine species, have become major resources for bioactive agents and play a key role in the discovery of lead compounds for new drug research
In the follow-up study, cell-based bioassays were used to attain characteristics of luffariellolide in activating nuclear receptors, and the results have shown that luffariellolide was a selective agonist for all three Retinoic Acid Receptor (RAR), but not for other Nuclear receptors (NRs), including the heterodimer partner RXRα
Nuclear receptors have been engaged in hit compound discovery as important targets involved in disease
Summary
Natural products, including compounds from plants, microbes, and marine species, have become major resources for bioactive agents and play a key role in the discovery of lead compounds for new drug research. The high hit rates in lead drug screening and large-scale structural diversity make marine natural products ideal candidates for drug discovery. Many nuclear receptors already have one or more ligands currently used as medicines, and nuclear receptors represent well-validated drug targets for several human diseases, including metabolic syndrome and hormone-dependent cancers (Table 1). A major goal in nuclear receptor-targeting drug development has been to obtain ligands that exhibit regulatory activity in a receptor-selective manner with reduced adverse side effects. Strategies to determine potential marine natural products as nuclear receptor modulators, the interaction between marine natural products and nuclear receptors, and potential marine natural products for drug development will be discussed and explored
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