P-glycoprotein - Wikipedia
Substrates of P-glycoprotein are susceptible to changes in pharmacokinetics due to drug interactions with P-gp inhibitors or inducers. Some of these substrates include colchicine , ciclosporin , dabigatran , [ 33 ] digoxin , diltiazem , [ 38 ] fexofenadine , …
P-glycoprotein: new insights into structure, physiological ...
The most well-known multidrug transporter is the P-glycoprotein transporter. The binding sites within P-glycoprotein can accommodate a variety of compounds with diverse structures. Hence, numerous drugs are P-glycoprotein substrates, with new ones being identified every day.
P-Glycoprotein: One Mechanism, Many Tasks and the ...
In the following we discuss how and where Pgp captures and releases its substrates, recapitulate the consequences of Pgp inhibition in absorption and excretion, and give some insight into the role of Pgp in immunosurveillance and metabolism of cancers.
P-glycoprotein and its role in drug-drug interactions
2014年8月4日 · Important substrates of P-glycoprotein include calcium channel blockers, cyclosporin, dabigatran etexilate, digoxin, erythromycin, loperamide, protease inhibitors and tacrolimus. Predicting clinically important interactions is difficult because of interindividual differences in drug transport.
Structural insight into substrate and inhibitor ... - Science
2019年2月15日 · ABCB1, also known as P-glycoprotein, actively extrudes xenobiotic compounds across the plasma membrane of diverse cells, which contributes to cellular drug resistance and interferes with therapeutic drug delivery.
ABC Transporters: P-Glycoprotein | SpringerLink
2022年1月1日 · PGP is a membrane-bound glycoprotein that can bind substrate molecules and transport them in a unidirectional manner across a phospholipid bilayer. In humans, PGP is primarily localized to a cell’s external membrane where it exports molecules from a cell to the extracellular fluid.
P-glycoprotein Substrates - Examine
P-glycoprotein substrates are compounds, including medications, that can be transported out of cells by p-glycoprotein. In the presence of intestinal p-glycoprotein inhibitors or inducers, the bioavailability of p-glycoprotein substrates may be increased or decreased, respectively.
P-glycoprotein: Tissue Distribution, Substrates, and ...
2010年10月26日 · The heart glycoside digoxin is widely accepted as typical P-glycoprotein substrate. The study in 2000 revealed a strong impact of 3435C>T on digoxin plasma distribution with elevated levels among 3435TT carriers after intake of …
2021年10月30日 · Hence, numerous drugs are P-glycoprotein substrates, with new ones being identified every day. For many years, the mechanisms of action of P-glycoprotein have been shrouded in mystery, and scientists have only recently been able to elucidate certain structural and functional aspects of this protein.
Multiclass Classifier for P-Glycoprotein Substrates ... - MDPI
In this study, an in silico multiclass classification model capable of predicting the probability of a compound to interact with P-gp was developed using a counter-propagation artificial neural network (CP ANN) based on a set of 2D molecular descriptors, as well as an extensive dataset of 2512 compounds (1178 P-gp inhibitors, 477 P-gp ...