What type of transport is P-glycoprotein?

What type of transport is P-glycoprotein?

Human P-glycoprotein (ABCB1) is a primary multidrug transporter located in plasma membranes, that, utilizes the energy of ATP hydrolysis to pump toxic xenobiotics out of cells. P-glycoprotein employs a most unusual molecular mechanism to perform this drug transport function.

Is P-glycoprotein an active transporter?

P-glycoprotein (P-gp) is an ATP-binding cassette (ABC) transporter responsible for the multidrug resistance (MDR) phenotype when overproduced in the plasma membrane of tumor cells (1). P-gp exhibits an ATP hydrolysis activity, coupled to the efflux of a variety of hydrophobic molecules (2, 3).

What is P-gp transporter?

Pgp (P-glycoprotein) (ABCB1) is an ATP-powered efflux pump which can transport hundreds of structurally unrelated hydrophobic amphipathic compounds, including therapeutic drugs, peptides and lipid-like compounds. It forms a major component of the blood-brain barrier and restricts the uptake of drugs from the intestine.

What is P-glycoprotein function?

P-glycoprotein, the most extensively studied ATP-binding cassette (ABC) transporter, functions as a biological barrier by extruding toxins and xenobiotics out of cells. In vitro and in vivo studies have demonstrated that P-glycoprotein plays a significant role in drug absorption and disposition.

What is the role of P-glycoprotein on pharmacokinetic aspects?

Is azithromycin a P-gp inhibitor?

Macrolides: Erythromycin, Azithromycin, and Clarithromycin The FDA approved macrolide antibiotics (erythromycin, azithromycin, and clarithromycin) were all reported as p-gp inhibitors.

Which is the best transporter for P-glycoprotein?

Solute carrier transporters comprise facilitated and ion-coupled transporters, whereas ATP-binding cassette transporters rely on ATP to actively pump substrates across cell membranes. The best characterized transporter is permeability glycoprotein (P-gp; also known as ATP-binding cassette, subfamily B, member 1 or multidrug resistance-1 [MDR1]).

Where is the permeability glycoprotein transport system located?

State-of-the-Art Paper. The P-Glycoprotein Transport System and Cardiovascular Drugs. Permeability glycoprotein (P-gp) mediates the export of drugs from cells located in the small intestine, blood-brain barrier, hepatocytes, and kidney proximal tubule, serving a protective function for the body against foreign substances.

How does digoxin affect the P-glycoprotein transport system?

The interaction of digoxin, a substrate of both intestinal and renal P-gp, with drugs that inhibit P-gp can lead to toxic accumulations of this cardiac glycoside, whereas P-gp inducers lower plasma digoxin concentration (11) ( Table 2 ).

How is P-glycoprotein used in the central nervous system?

Permeability glycoprotein (P-gp) is an efflux transporter at the luminal membranes of the BBB and the BCSFB that removes drugs from brain interstitial fluid back to blood or into the CSF, thus preventing the drug from producing central nervous system effects.