What is OATP1B1 substrate?

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What is OATP1B1 substrate?

Known substrates of OATP1B1 and OATP1B3 include statins, repaglinide, olmesartan, enalapril, valsartan, several xenobiotic glucuronide metabolites, as well as a host of cytotoxic chemotherapeutic agents, including the taxanes paclitaxel and docetaxel, the platinum-based drug cisplatin, and methotrexate.

What is the function of organic anion transporter?

Organic anion transporters (OATs) are the secondary/tertiary active transporter proteins that regulate anion balance in the body. They are primarily expressed in the kidney and liver and control the excretion of common drugs, toxins, and endogenous metabolites into the urine.

What is OATP1?

OATP1 (Organic Anion Transporting Polypeptide 1) from MyBioSource.com. MyBioSource.com’s OATP1 (Organic Anion Transporting Polypeptide 1) is a Rabbit Polyclonal antibody. This antibody has been shown to work in applications such as: ELISA, Immunohistochemistry, and Western Blot.

What is the meaning of Oatp?

Organic anion transporting polypeptide (OATP) family transporters accept a number of drugs and are increasingly being recognized as important factors in governing drug and metabolite pharmacokinetics.

What is Bcrp substrate?

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).

What is the SLCO1B1 gene?

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.

Are organic anions proteins?

The following table lists some of the organic anions and their conjugate acids which are substrates of the organic acid transporter (OAT) family of transmembrane proteins….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?

Together, these data suggest that Oatp1c1 transports fenamates into, and perhaps across, brain barrier cells. The fenamate class of nonsteroidal anti-inflammatory drugs is transported by organic anion transporting polypeptides and competitively inhibits thyroxine transport in brain microvessels.

What are concomitant oat1 b1 inhibitors?

A medication used to treat gouty arthritis, tophaceous gout, and hyperuricemia. An antibiotic used to treat several types of mycobacterial infections including Mycobacterium avium complex, leprosy, and in combination with other antibacterials to treat latent or active tuberculosis.

What are BCRP inhibitors?

BCRP inhibitors include, among others, fumitremorgin C (FTC), the FTC analogue Ko143, the acridone carboxamide derivative GF120918, anti-HIV protease inhibitors nelfinavir and ritonavir, the dietary flavonoids chrysin and biochanin A, the tyrosine kinase inhibitors gefitinib and imatinib [5, 16, 36], and herb extracts …

What drugs are P gp inhibitors?

Some common pharmacological inhibitors of P-glycoprotein include: amiodarone, clarithromycin, ciclosporin, colchicine, diltiazem, erythromycin, felodipine, ketoconazole, lansoprazole, omeprazole and other proton-pump inhibitors, nifedipine, paroxetine, reserpine, saquinavir, sertraline, quinidine, tamoxifen, verapamil.

What medications are affected by SLCO1B1?

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.

Which is an organic anion transporting polypeptide 1B1?

OATP1B1 (organic anion transporting polypeptide 1B1) This is particularly important for members of the statin class of medicines, where elevated blood concentrations due to inhibition of hepatic uptake can result in myopathy and rhabdomyolysis. Complex drug interactions involving OATP1B1, other uptake and efflux transporters,…

What is the role of the OATP1B1 transporter?

OATP1B1-mediated hepatic uptake of repaglinide is important for its elimination by CYP-mediated reactions, as evidenced by the elevation of repaglinide plasma levels in subjects with the OATP1B1 521CC genotype.

How does OATP recognize and transport structurally diverse compounds?

OATP transporters recognize and transport structurally diverse compounds. It has been proposed that OATP transporters have multiple substrate binding sites as a mechanism of transport and/or inhibition.

Where is the OATP1B1 protein found in the liver?

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. For example, the OATP1B1 protein transports bilirubin, which is a yellowish substance that is produced when red blood cells are broken down.

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