What happens when P-glycoprotein is inhibited?

What happens when P-glycoprotein is inhibited?

Like the enzymes involved in drug metabolism, substrates of P-glycoprotein can potentially act as inhibitors or inducers of its function. Inhibition of P-glycoprotein can result in increased bioavailability of the susceptible drug. Induction of P-glycoprotein reduces the bioavailability.

What is the role of P-glycoprotein?

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 are collies sensitive to?

Some dog breeds are more sensitive to certain drugs than other breeds. Collies and related breeds, for instance, can have a genetic predisposition to adverse drug reactions involving many different drugs. These drug sensitivities result from a mutation in the multidrug resistance gene (MDR1 gene.)

Is digoxin a Pgp inhibitor?

Conclusions: Quinidine and digoxin are both substrates for P-glycoprotein, and quinidine is a potent inhibitor of digoxin transport in vitro.

What are the Inhibitors of glycoprotein IIb?

Glycoprotein IIb/IIIa Inhibitors Glycoprotein IIb/IIIa (GP IIb/IIIa) inhibitors prevent platelet aggregation by blocking glycoprotein IIb/IIIa receptors on their platelet’s plasma membrane and inhibit fibrinogen binding. The available GP IIb/IIIa inhibitors include abciximab, tirofiban, and eptifibatide. These agents, along with as …

What is the effect of ABCB1 polymorphisms on P-glycoprotein expression?

A 2015 review of polymorphisms in ABCB1 found that “the effect of ABCB1 variation on P-glycoprotein expression (messenger RNA and protein expression) and/or activity in various tissues (e.g. the liver, gut and heart) appears to be small.

How does Rab4 interact with P-glycoprotein in multidrug resistant K562 cells?

“Rab4 interacts with the human P-glycoprotein and modulates its surface expression in multidrug resistant K562 cells”. International Journal of Cancer. 128 (1): 192–205. doi: 10.1002/ijc.25310.

What is a P-gp inhibitor?

Any such substance can sometimes be called a P-gp inhibitor. P-gp was discovered in 1971 by Victor Ling . A 2015 review of polymorphisms in ABCB1 found that “the effect of ABCB1 variation on P-glycoprotein expression (messenger RNA and protein expression) and/or activity in various tissues (e.g. the liver, gut and heart) appears to be small.

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