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  1. Proceedings of the National Academy of Sciences, India Section B: Biological Sciences
  2. Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 85
  3. Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 85, Issue 2, June 2015
  4. P-Glycoprotein: A Critical Comparison of Models Depicting Mechanism of Drug Efflux and Role of Modulators
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Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 87
Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 86
Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 85
Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 85, Issue 4, December 2015
Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 85, Issue 3, September 2015
Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 85, Issue 2, June 2015
Carbon Sequestration in Indian Soils: Present Status and the Potential
P-Glycoprotein: A Critical Comparison of Models Depicting Mechanism of Drug Efflux and Role of Modulators
CRISPR/Cas9 Systems: The Next Generation Gene Targeted Editing Tool
Diversity and Distribution of Earthworms in Different Soil Habitats of Assam, North-East India, an Indo-Burma Biodiversity Hotspot
Evaluation of Genetic Diversity and Interrelationships of Agro-Morphological Characters in Soybean (Glycine max) Genotypes
Urease Activity and Its Kinetics in Selected Benchmark Soils of Indo-Gangetic Plains, India
Effect of Fertilizer Loaded Nanoclay/Superabsorbent Polymer Composites on Nitrogen and Phosphorus Release in Soil
Statistical Modeling of Extreme Drought Occurrence in Bellary District of Eastern Karnataka
Effect of Dermal Application of Bifenthrin on Acetylcholinesterase and Oxidative Stress Indices in Rat Blood, Lung and Kidney
Phenology and Parasitization Behaviour of Telenomus cuspis (Hymenoptera: Platygastridae) an Egg Parasitoid of Helopeltis antonii (Hemiptera: Miridae) in Cashew
Effect of Environment on Fatty Acid Composition and Tocopherol Content in Soybean, Glycine max L Merrill
Pesticide: An Appraisal on Human Health Implications
Heterogeneity of Bacterial Community Compositions in Surface Sediments of Three Lake Zones in Lake Taihu
Tyrosinase Degradation in Amelanotic Melanoma Cells is Mediated by Cytoplasmic Factors in Addition to Proteasome-Mediated Mechanism
Biochemical and Physiological Stress Responses to Heat Shock and Their Recovery in Labeo rohita Fingerlings
Survival and Growth of Tiger Shrimp (Penaeus monodon) in Inland Saline Water Supplemented with Potassium
Physiological Responses of Golden Mahseer (Tor putitora) Fry to Dietary Zinc and Assessment of its Optimum Requirement
Variation in Popping Quality Related to Physical, Biochemical and Nutritional Properties of Finger Millet Genotypes
Evaluation of Mass Transfer Kinetics for Osmotic Dehydration of Oyster Mushrooms (Pleurotus sajor-caju) in Salt-sugar Solution
Physicochemical Analysis of Ethnically Fermented Soybean Products of North-East India and Molecular Characterization of Associated Lactic Acid Bacteria
Antioxidant System Against Active Oxygen Species in Cyanobacterium Aphanothece stagnina: Response to Excess Light Under Cadmium Stress
Distribution and Diversity of Lichenized Fungi Colonizing Jageshwar Group of Temples, Almora, Uttarakhand
Evaluation of Antibacterial and Antioxidant Efficacy of the Fern Azolla caroliniana Symbiotic with the Cyanobacterium Anabaena azollae
Antifungal and Antioxidant Profile of Ethnomedicinally Important Liverworts (Pellia endivaefolia and Plagiochasma appendiculatum) Used by Indigenous Tribes of District Reasi: North West Himalayas
Production and Composition of Extracellular Polysaccharide Synthesized by Rhizobium undicola Isolated from Aquatic Legume, Neptunia oleracea Lour.
Antioxidant and Anti-inflammatory Mediated Mechanism in Thermal Wound Healing by Gel Containing Flower Extract of Butea monosperma
Distribution of Andrographis species in Different Districts of Andhra Pradesh
Marker Based In-vitro Antioxidant Potential, Microscopy and Validated High Performance Thin Layer Chromatographic Method for Saffron
Abiotic Stress Tolerance of Chickpea Genotypes Depends Upon Antioxidative Potential and Nutritional Quality of Seeds
Anatomical Adaptations to Salinity in Spergularia marina (Caryophyllaceae) from Turkey
Potential Microbial Consortium for Plant Growth Promotion of Sunflower (Helianthus annuus L.)
Improved Seedling Growth and Seed Germination in Legume Crop Vigna mungo (L.) Hepper Utilizing Marine Macro Algal Extracts
Association Analysis for Vegetative Propagation Traits in Eucalyptus tereticornis and Eucalyptus camaldulensis Using Simple Sequence Repeat Markers
Determination of Thermal Constant and Development Threshold of Pink Borer, Sesamia inferens Walker
Biomarker System for Genetic Analysis of Stored Grain Pests Callosobruchus maculatus and Callosobruchus chinensis
Immunohistochemical and Molecular Approaches for the Diagnosis of Campylobacter fetus subsp. venerealis in Natural Cases of Bovine Abortion
Evaluation of Biochemical Parameters in Buffalo Calves Exposed to Subacute Fenvalerate Toxicosis
Development of the Novel Loop Mediated Isothermal Amplification (LAMP) of IS711 Sequence for Rapid Detection of Brucella Species
A Review of the Epidemiology and Control of Gastrointestinal Nematode Infections of Small Ruminants
In-vitro Anthelmintic Efficacy of Aqueous Extract of Scindapsus officinalis (Roxb.) Schott Fruits Against Haemonchus contortus of Small Ruminants
Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 85, Issue 1, March 2015
Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 84
Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 83
Proceedings of the National Academy of Sciences, India Section B: Biological Sciences : Volume 82

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P-Glycoprotein: A Critical Comparison of Models Depicting Mechanism of Drug Efflux and Role of Modulators

Content Provider SpringerLink
Author Tripathi, Anushree Kesharwani, Rajesh Kumar Misra, Krishna Singh, Durg Vijay
Copyright Year 2014
Abstract Permeability or P-glycoprotein (P-gp), present in both prokaryotes and eukaryotes is an essential protein belonging to the adenosine triphosphate (ATP) binding cassette transporter family. It functions as a protective barrier by extrusion of wide range of substrates including toxins, xenobiotic compounds and drugs from the cell. These are ubiquitous integral membrane proteins that have ATPase activity for substrate transport across the lipid membrane. The potential role of P-gp in efflux mechanism is to avoid drug accumulation and to provide intrinsic resistance to a broad range of anticancer compounds against sarcoma, breast cancer and certain types of leukemia. This review recapitulates the structural and functional aspects of core domains of P-gp. Furthermore, various proposed mechanisms of translocation of substrates across the membrane which explain the conformational changes in different domains upon ATP binding and hydrolysis. Another critical aspect focuses on different modulators and their mode of binding on P-gp which facilitates the inhibition of efflux mechanism. Ten models of drug efflux mechanism have been illustrated and a comparative account of their applicability and limitations given, paving way for further improvements. In the present study it has been observed that contrary to the earlier reported models where transmembrane domain is the preferred binding site of ligands resulting in their efflux through ATP hydrolysis at nucleotide binding domain (NBD) site. The more hydrophilic NBD appears to be the appropriate binding site for majority of the hydrophobic third and fourth generation modulators thus inhibiting the binding and hydrolysis of ATP resulting in inhibition of efflux.
Starting Page 359
Ending Page 375
Page Count 17
File Format PDF
ISSN 03698211
Journal Proceedings of the National Academy of Sciences, India Section B: Biological Sciences
Volume Number 85
Issue Number 2
e-ISSN 22501746
Language English
Publisher Springer India
Publisher Date 2014-08-13
Publisher Place New Delhi
Access Restriction One Nation One Subscription (ONOS)
Subject Keyword Life Sciences Plant Biochemistry P-gp Nucleic Acid Chemistry ATPase activity Behavioral Sciences Transmembrane domain Efflux mechanism Nucleotide binding domain Modulators
Content Type Text
Resource Type Article
Subject Environmental Science Agricultural and Biological Sciences
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