Abstract
G protein-coupled receptors (GPCRs), which constitute the most populous family of the human proteome, are the target of 35–45% of approved therapeutic drugs. This review focuses on natural products (excluding peptides) that target GPCRs. Natural compounds identified so far as agonists, antagonists or allosteric modulators of GPCRs have been found in all groups of existing living beings according to Whittaker’s Five Kingdom Classification, i.e., bacteria (monera), fungi, protoctists, plants and animals. Terpenoids, alkaloids and flavonoids are the most common chemical structures that target GPCRs whose endogenous ligands range from lipids to epinephrine, from molecules that activate taste receptors to molecules that activate smell receptors. Virtually all of the compounds whose formula is displayed in this review are pharmacophores with potential for drug discovery; furthermore, they are expected to help expand the number of GPCRs that can be considered as therapeutic targets.
Highlights
Genes for G-protein coupled receptors (GPCRs) make up 10% of the human genome
Non-peptide natural compounds able to target G protein-coupled receptors (GPCRs) structurally belong to either the alkaloid, terpenoid or flavonoid chemical types, which can be found in organisms of any of the Five
Apart from alkaloids and terpenoids, found in coffee, theophylline, mainly found in tea (Camellia sinensis), and theobromine, flavonoids are able to interact with GPCRs
Summary
Genes for G-protein coupled receptors (GPCRs) make up 10% of the human genome. When the Nobel prize in Chemistry was awarded to Lefkowitz and Kobilka in 2012, the Nobel Foundation posted: “Smart receptors on cell surfaces . Scientists knew that hormones such as adrenalin had powerful effects: increasing blood pressure and making the heart beat faster. They suspected that cell surfaces contained some kind of recipient for hormones. What these receptors consisted of and how they worked remained obscured. GPCRs. The percentage of approved drugs (in human therapy) targeting GPCRs is estimated to be. There are hopes that the remaining 90% of GPCRs can become a target of future drugs, especially for diseases for which there is no efficacious medication; two examples are Alzheimer’s disease [2] and atrial fibrillation [3,4,5]
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