Abstract
A number of studies have identified differential kavalactone activity against a variety of molecular targets, including P glycoprotein (Pgp), platelet monoamine oxidase (MAO-B), transcription factor binding domains, pregnane X (PXR) and GABA receptors, and cytochrome P450 and cyclo-oxygenase (COX) enzymes. The molecular structure of the kavalactones possesses a pharmacophore for several of these targets. In most cases, conformational stability is more significant than the substituents present. The analysis of these pharmacophores provides important insights for future medicinal chemistry-based approaches to kavalactone-type drugs.
Keywords: Kavalactone, pharmacophore, molecular targets, conformational isomerism, Piper methysticum, P-Glycoprotein (Pgp), kavain/dihydrokavain, methysticin/dihydromethysticin, desmethoxyyangonin, Cyclo-Oxygenase Enzymes, COX, NSAIDs, luciferase-based assay, Kavain, 7,8-Dihydrokavain, Methysticin, 7,8-Dihydromethysticin, Yangonin, Cytochrome P450, Pregnane X Receptor, GABA, LITAF
Mini-Reviews in Medicinal Chemistry
Title: Kavalactone Pharmacophores for Major Cellular Drug Targets
Volume: 11 Issue: 1
Author(s): A. Rowe, R. Narlawar, P. W. Groundwater and I. Ramzan
Affiliation:
Keywords: Kavalactone, pharmacophore, molecular targets, conformational isomerism, Piper methysticum, P-Glycoprotein (Pgp), kavain/dihydrokavain, methysticin/dihydromethysticin, desmethoxyyangonin, Cyclo-Oxygenase Enzymes, COX, NSAIDs, luciferase-based assay, Kavain, 7,8-Dihydrokavain, Methysticin, 7,8-Dihydromethysticin, Yangonin, Cytochrome P450, Pregnane X Receptor, GABA, LITAF
Abstract: A number of studies have identified differential kavalactone activity against a variety of molecular targets, including P glycoprotein (Pgp), platelet monoamine oxidase (MAO-B), transcription factor binding domains, pregnane X (PXR) and GABA receptors, and cytochrome P450 and cyclo-oxygenase (COX) enzymes. The molecular structure of the kavalactones possesses a pharmacophore for several of these targets. In most cases, conformational stability is more significant than the substituents present. The analysis of these pharmacophores provides important insights for future medicinal chemistry-based approaches to kavalactone-type drugs.
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Cite this article as:
Rowe A., Narlawar R., W. Groundwater P. and Ramzan I., Kavalactone Pharmacophores for Major Cellular Drug Targets, Mini-Reviews in Medicinal Chemistry 2011; 11 (1) . https://dx.doi.org/10.2174/138955711793564088
DOI https://dx.doi.org/10.2174/138955711793564088 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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