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Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
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Local anesthetics (LAs) are drugs that induce a temporary loss of sensation in a limited body area, preventing pain. Cocaine was the first local anesthetic discovered in the late 19th century. Cocaine is a benzoic acid ester obtained from the leaves of coca shrubs and was often used for its psychotropic effects. Cocaine was first isolated in 1860 by Albert Niemann. Sigmund Freud studied the physiological actions of cocaine. Carl Koller later introduced it into clinical practice in 1884 as a...
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Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic...
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Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

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Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
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Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

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Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
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Flavonoids differentially modulate liver X receptors activity-Structure-function relationship analysis.

Allan Fouache1, Nada Zabaiou2, Cyrille De Joussineau1

  • 1Université Clermont Auvergne, GReD, CNRS UMR 6293, INSERM U1103, 28, place Henri Dunant, BP38, F63001, Clermont-Ferrand, France; Centre de Recherche en Nutrition Humaine d'Auvergne, 58 Boulevard Montalembert, F-63009, Clermont-Ferrand, France.

The Journal of Steroid Biochemistry and Molecular Biology
|April 9, 2019
PubMed
Summary

This study investigates flavonoids as potential modulators of Liver X Receptors (LXRs). Researchers found specific flavonoids can influence LXR activity, aiding in the development of targeted therapies.

Keywords:
ApigeninFlavonoidGalanginLXRNaringeninQuercetin

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Liver X Receptors (LXRs) α (NR1H3) and β (NR1H2) are crucial nuclear receptors regulating cholesterol homeostasis, cell death, and proliferation.
  • LXRs are significant therapeutic targets for conditions like dyslipidemia, atherosclerosis, diabetes, and cancer.
  • Developing selective LXR ligands is challenging due to isoform specificity requirements.

Purpose of the Study:

  • To investigate the potential of selected flavonoids (galangin, quercetin, apigenin, naringenin) to modulate LXR activity.
  • To understand the interaction of flavonoids with LXR binding pockets.
  • To identify potential selective LXR ligands from natural products.

Main Methods:

  • Utilized cell culture experiments with double-hybrid assays to assess LXR modulation.
  • Employed in silico molecular docking to predict ligand-binding patterns.
  • Screened four specific flavonoids for their effects on LXR activity.

Main Results:

  • Demonstrated that specific flavonoids can modulate LXR activity in cell culture.
  • Molecular docking provided insights into agonistic and antagonistic binding patterns.
  • Identified galangin, quercetin, apigenin, and naringenin as compounds influencing LXR.

Conclusions:

  • Flavonoids can modulate Liver X Receptor activity, offering a new avenue for therapeutic development.
  • The study enhances understanding of the LXR ligand-binding pocket and flavonoid mechanisms of action.
  • Results facilitate the selection and design of more selective LXR ligands for various diseases.