What is the function of organic anion transporting polypeptides?

Organic anion transporting polypeptides (OATPs) are important transporter proteins that are expressed at the plasma membrane of cells, where they mediate the influx of endogenous and exogenous substances including hormones, natural compounds and many clinically important drugs.

Where are Oatp located?

Therefore, OATPs are present in the lipid bilayer of the cell membrane, acting as the cell’s gatekeepers. OATPs belong to the Solute Carrier Family (SLC) and the major facilitator superfamily.

What are OATPs?

9.7 Organic Anion Transporting Polypeptides (OATPs) OATP refers to a member of the superfamily of the solute carrier that is localized at the basolateral membrane of hepatocytes. OATP acts by mediating the hepatic uptake of both endogenous as well as some important clinical compounds.

Are organic acids anions?

Organic anions are chemically heterogeneous substances possessing a carbon backbone and a net negative charge. Organic anions are conjugate bases of organic acids….Organic anion.

Organic Anions	Conjugate Organic Acids (acidic proton is shown in red)
dicarboxylates	alpha-ketoglutarate

Which drug is a competitive inhibitor of organic anionic transporter?

Competitive inhibition of human organic anion transporters 1 (SLC22A6), 3 (SLC22A8) and 4 (SLC22A11) by major components of the medicinal herb Salvia miltiorrhiza (Danshen) Drug Metab Pharmacokinet.

What does the SLCO1B1 gene do?

The SLCO1B1 gene provides instructions for making a protein called organic anion transporting polypeptide 1B1, or OATP1B1. This protein is found in liver cells; it transports compounds from the blood into the liver so that they can be cleared from the body.

What are examples of organic anions?

. Examples of such anions are hippurate, long chain fatty acids, bile salts, urate, prostaglandins, antibiotics, and diuretics, and examples of cations are choline, catecholamines, histamine, quinine, and cimetidine.

What is an inorganic anion?

Inorganic anions refer to the combination of: Common anions: chloride, fluoride, bromide, nitrate, nitrite, sulfate, and phosphate. Inorganic disinfection byproducts (DBPs): chlorate, chlorite, and bromate. Other anions, such as perchlorate and chromate.

What drugs are metabolized by SLCO1B1?

Pharmacogenomics in India The gene organic anion transporting polypeptide 1B1 (OATP1B1, also known as SLCO1B1) encodes the transmembrane protein OATP1B1, which transports anionic drugs such as statins, irinotecan, rifampin, repaglinide and methotrexate.

What transports P-gp?

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.

How does P-gp affect drug absorption?

In the gut, P-glycoprotein pumps drugs back into the lumen, decreasing their absorption. Drugs which induce P-glycoprotein, such as rifampicin, can reduce the bioavailability of some other drugs. Inhibitors of P-glycoprotein, such as verapamil, increase the bioavailability of susceptible drugs.

What medications are affected by SLCO1B1 decreased function?

drug/xenobiotic substrates	indication	measurement
atorvastatin (acid)		inhibition of Estradiol 17beta D-Glucuronide transport
lovastatin (acid)	HMG CoA reductase inhibitor	inhibition of Estradiol 17beta D-Glucuronide transport
lovastatin		inhibition of pravastatin transport
cerivastatin	HMG CoA reductase inhibitor	transport

What are organic anion transporting polypeptides?

The organic anion transporting polypeptides (OATPs) are a superfamily of drug transporters involved in the uptake and disposition of a wide array of structurally divergent endogenous and exogenous substrates, including steroid hormones, bile acids, and commonly used drugs, such as anti-infectives, antihypertensives, and cholesterol lowering agents.

Which anion-transporting polypeptides transport opioid peptides across the blood–brain barrier?

Organic anion-transporting polypeptides mediate transport of opioid peptides across blood–brain barrier. J Pharmacol Exp Ther 2000; 294: 73 – 79 .

Which flavonoids are involved in the function of organic anion transport?

Mandery K, Bujok K, Schmidt I, Keiser M, Siegmund W, Balk B, et al. Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1. Biochem Pharmacol. 2010;80(11):1746–1753.

Are OATP transporters expressed at the protein level in the intestine?

Among the OATP family transporters, OATP1A2 and OATP2B1 have been reported to be expressed in human intestine at the protein level, although the expression level of OATP1A2 was reported to be very low 6, 107.