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Overview of P-glycoprotein inhibitors: a rational outlook


 
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1. Title Title of document Overview of P-glycoprotein inhibitors: a rational outlook
 
2. Creator Author's name, affiliation, country Kale Mohana Raghava Srivalli; Osmania University; G. Pulla Reddy College of Pharmacy; Department of Pharmaceutics;
 
2. Creator Author's name, affiliation, country P. K. Lakshmi; Osmania University; G. Pulla Reddy College of Pharmacy; Department of Pharmaceutics;
 
3. Subject Discipline(s)
 
3. Subject Keyword(s) P-glycoprotein^i1^sinhibit;Multidrug resistence;Cluster of differentiation 243;Sphingolipids;Competitive inhibitors
 
4. Description Abstract P-glycoprotein (P-gp), a transmembrane permeability glycoprotein, is a member of ATP binding cassette (ABC) super family that functions specifically as a carrier mediated primary active efflux transporter. It is widely distributed throughout the body and has a diverse range of substrates. Several vital therapeutic agents are substrates to P-gp and their bioavailability is lowered or a resistance is induced because of the protein efflux. Hence P-gp inhibitors were explored for overcoming multidrug resistance and poor bioavailability problems of the therapeutic P-gp substrates. The sensitivity of drug moieties to P-gp and vice versa can be established by various experimental models in silico, in vitro and in vivo. Ever since the discovery of P-gp, the research plethora identified several chemical structures as P-gp inhibitors. The aim of this review was to emphasize on the discovery and development of newer, inert, non-toxic, and more efficient, specifically targeting P-gp inhibitors, like those among the natural herb extracts, pharmaceutical excipients and formulations, and other rational drug moieties. The applications of cellular and molecular biology knowledge, in silico designed structural databases, molecular modeling studies and quantitative structure-activity relationship (QSAR) analyses in the development of novel rational P-gp inhibitors have also been mentioned.
 
5. Publisher Organizing agency, location Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
 
6. Contributor Sponsor(s)
 
7. Date (YYYY-MM-DD) 2012-09-01
 
8. Type Status & genre Peer-reviewed Article
 
8. Type Type
 
9. Format File format PDF
 
10. Identifier Uniform Resource Identifier https://www.revistas.usp.br/bjps/article/view/47849
 
10. Identifier Digital Object Identifier (DOI) http://dx.doi.org/10.1590/S1984-82502012000300002
 
11. Source Title; vol., no. (year) Brazilian Journal of Pharmaceutical Sciences (Impresso); Vol 48, No 3 (2012)
 
12. Language English=en
 
13. Relation Supp. Files
 
14. Coverage Geo-spatial location, chronological period, research sample (gender, age, etc.)
 
15. Rights Copyright and permissions Copyright (c) 2017 Brazilian Journal of Pharmaceutical Sciences (Impresso)
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