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.
Export Options
About this article
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 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Classical to Current Approach for Treatment of Psoriasis: A Review
Endocrine, Metabolic & Immune Disorders - Drug Targets Asthma, Allergy and Chemokines
Current Drug Targets Role of the Non-Receptor Tyrosine Kinase Fes in Cancer
Current Medicinal Chemistry Daclizumab: A Potential Asthma Therapy?
Recent Patents on Inflammation & Allergy Drug Discovery Beneficial and Adverse Effects of Molecularly Targeted Therapies for Acute Promyelocytic Leukemia in Central Nervous System
CNS & Neurological Disorders - Drug Targets HPLC-NMR Chemical Profiling of the Australian Carnivorous Plant, Drosera erythrohiza subspecies magna
The Natural Products Journal 2-Arylbenzimidazoles as Antiviral and Antiproliferative Agents-Part 2
Medicinal Chemistry Pharmacogenetics of Phase I and Phase II Drug Metabolism
Current Pharmaceutical Design Prodrugs and Endogenous Transporters: Are They Suitable Tools for Drug Targeting into the Central Nervous System?
Current Pharmaceutical Design Targeting the Human Thioredoxin System by Diverse Strategies to Treat Cancer and Other Pathologies
Recent Patents on DNA & Gene Sequences AAV Hybrid Serotypes: Improved Vectors for Gene Delivery
Current Gene Therapy Angiogenesis and Hypoxia in Glioblastoma: A Focus on Cancer Stem Cells
CNS & Neurological Disorders - Drug Targets The Genetic Landscapes of Inflammation-Driven Gastrointestinal Tract Cancers
Current Pharmaceutical Design Cytokine/Antibody Complexes: An Emerging Class of Immunostimulants
Current Pharmaceutical Design Protein Phosphatase 2A as a Potential Target for Treatment of Adult T Cell Leukemia
Current Cancer Drug Targets Immunotherapy Resistance Mechanisms in Renal Cell Cancer
Current Signal Transduction Therapy Electrochemical Indicators for DNA Electroanalysis
Current Analytical Chemistry The Metabolomic Strategy in Tuberculosis Therapy
Combinatorial Chemistry & High Throughput Screening Stem Cells, Cancer, Liver, and Liver Cancer Stem Cells: Finding a Way Out of the Labyrinth...
Current Cancer Drug Targets Opportunities and Challenges for Host-Directed Therapies in Tuberculosis
Current Pharmaceutical Design