What is Oatp in pharmacology?
Organic anion transporting polypeptides (OATPs in humans, Oatps in rodents) are multispecific transporters located in numerous epithelia throughout the body. They mediate the cellular uptake of a broad range of substrates, including bile acids, steroid conjugates and numerous xenobiotics.
Where is OATP1B1 expressed?
hepatocytes
Expression of OATP1B1 was shown in adult and fetal liver by Northern blot analysis. This expression was confirmed at the protein level and localized to the basolateral membrane of hepatocytes throughout the liver lobule.
Where are Oatp located?
OATPs are encoded by genes of the SLCO family (previously SLC21) (Hagenbuch and Meier, 2004). The genes encoding human OATP1 family members are located in the short arm of chromosome 12, whereas genes encoding other OATPs are located in chromosomes 3, 5, 8, 11, 15 and 20.
What does SLCO1B1 stand for?
SLCO1B1 (solute carrier organic anion transporter family member 1B1) is a drug transporter that helps the body get rid of certain medicines through the liver. There are many medications that may be affected by SLCO1B1. There are many variations or genetic differences in the gene for SLCO1B1.
What is OATPs?
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.
What drugs are P glycoprotein 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 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 medications are processed by SLCO1B1?
OATP1B1/SLCO1B1 Substrates
| Drug | Target |
|---|---|
| Taurocholic acid | Solute carrier organic anion transporter family member 1A2 |
| Taurocholic acid | Ileal sodium/bile acid cotransporter |
| Taurocholic acid | Canalicular multispecific organic anion transporter 1 |
| Taurocholic acid | Solute carrier organic anion transporter family member 1B1 |
What are strong OAT3 inhibitors?
Drugs which inhibit organic anion transporter 3. An isocitrate dehydrogenase-1 inhibitor used to treat acute myeloid leukemia with a susceptible mutation.
What is the function of OATP?
Organic anion transporting polypeptides (OATPs in humans, Oatps in rodents) are multispecific transporters located in numerous epithelia throughout the body. They mediate the cellular uptake of a broad range of substrates, including bile acids, steroid conjugates and numerous xenobiotics.
Is OATP expression linked to the origin of the cells?
We found a strong relationship between OATP expression and the origin of the cells, as cells from primary or metastatic SCLC and carcinoid tumors differ with respect to OATP levels.
Where is OATP2B1 expressed in the human body?
OATP2B1 protein expression was confirmed at the basolateral membrane of hepatocytes ( 29a ), at the apical membrane of enterocytes ( 30 ), at the endothelium of the blood-brain barrier ( 31 ), at the endothelial cells of the heart ( 32 ), at the myoepithelium of mammary ducts ( 33 ), and in the placenta ( 34 ).
What are the substrates of OatP4a1?
Other OATP4A1 substrates are thyroid hormones and they are known to modulate tumor progression via binding the nuclear thyroid hormone receptor [50].