What is a MATE1 substrate?

Substrate specificity Substrates for MATE1 and MATE2-K are typical organic cations, TEA, 1-methyl-4-phenylpyridinium (MPP), metformin, cimetidine, procainamide and so on (Table 2) (Tanihara et al., 2007).

What is an OCT inhibitor?

Organic Cation Transporters (OCTs) Cimetidine is a well-described inhibitor of OCT2 and has been associated with reduced clearance of a number of concomitantly administered medications, including metformin, pindolol, and dofetilide [44].

What is the function of organic cation transporter?

Organic cation transporters (OCTs) translocate endogenous (e.g. dopamine) and exogenous (e.g. drugs) substances of cationic nature and, therefore, play an important role in the detoxification of exogenous compounds.

What is renal organic cation transporter?

In the kidney, human organic cation transporters (OCTs) and multidrug and toxin extrusion proteins (MATEs) are the major transporters for the secretion of cationic drugs into the urine. OCTs and MATEs can transport important drugs, such as metformin and cisplatin.

What is Bcrp substrate?

Summary. ABCG2, more commonly referred to as BCRP (Breast Cancer Resistance Protein), is an efflux transporter that serves two major drug transport functions. Firstly, it restricts the distribution of its substrates into organs such as the brain, testes, placenta, and across the gastrointestinal tract (GIT).

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What happens when a drug inhibits a transporter?

Because transporter proteins have saturable binding sites, co-administered drugs may inhibit transporters and can thereby influence the uptake or efflux of another drug. This can lead to reduced excretion or metabolism of drugs and as a result increased internal exposure, which may lead to drug induced toxicity.

What is otc1?

OCT1 is primarily a hepatic uptake transporter, expressed on the sinusoidal membrane (blood side) of hepatocytes. It plays a key role in the disposition and hepatic clearance of mostly cationic drugs and endogenous compounds.

What does BCRP stand for?

BCRP

What is the full name of BCRP?

ABCG2, more commonly referred to as BCRP (Breast Cancer Resistance Protein), is an efflux transporter that serves two major drug transport functions. Firstly, it restricts the distribution of its substrates into organs such as the brain, testes, placenta, and across the gastrointestinal tract (GIT).

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Which is an important substrate for OCT2 transporters?

Important clinical substrates include metformin and cisplatin. Gene polymorphisms of OCT2 are associated with altered metformin and cisplatin pharmacokinetics and toxicity, but the role of other cation transporters, and their functional SNPs are also important.

Where is OCT2 located in the kidney membrane?

Substrate – a drug that is metabolized by a certain enzyme is a substrate of that enzyme OCT2 is a transport protein found in the kidney. It is located in the membrane of tubular epithelial cells in the proximal convoluted tubule.

What does Oct stand for in medical category?

OCT – Organic Cation Transporter Substrate – a drug that is metabolized by a certain enzyme is a substrate of that enzyme.

Can a OCT2 inhibitor block the action of OCT2?

Inhibitors – block the action of OCT2 When OCT2 inhibitors are taken with medications that are transported by OCT2, they can alter the elimination of that medication Drugs may be transported by OCT2 and also inhibit it at the same time.