What are OATP1B1 inhibitors?
Novel OATP Inhibitors Identified
| compound | new inhibitor of | previously known OATP interaction |
|---|---|---|
| erlotinib | OATP2B1 | |
| fluo-3 | OATP2B1 | OATP1B3 substrate |
| flutamide | OATP2B1 | |
| genistein | OATP2B1 | OATP1B1 inhibitor |
Where is OATP1B1 located?
hepatocytes
OATP1B1 is located to the sinusoidal (basolateral) membrane of hepatocytes, and is expressed uniformly throughout the lobules. Despite its name, OATP1B1 has broad substrate selectivity that includes anionic, zwitterionic, and neutral lipophilic drugs.
What drugs 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.
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.
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.
What is BSEP transporter?
The bile salt export pump (BSEP) is the major transporter for the secretion of bile acids from hepatocytes into bile in humans.
What does OATP1B1 stand for?
OATP1B1
| Acronym | Definition |
|---|---|
| OATP1B1 | Organic Anion Transport Proteins 1b1 (transporter) |
What are the symptoms of statin myopathy?
Symptoms of statin induced myopathy include fatigue, muscle pain, muscle tenderness, muscle weakness, nocturnal cramping, and tendon pain. The muscle symptoms tend to be proximal, generalised, and worse with exercise.
What is SLCO1B1 decreased function?
The SLCO1B1*5 genotype causes a loss of statin transporter function into the liver, thereby increasing the risk of muscle symptoms by exposing muscle to increased circulating levels of statins.
What does SLCO1B1 decreased function mean?
The SLCO1B1*5 genotype causes a loss of statin transporter function into the liver, thereby increasing the risk of muscle symptoms by exposing muscle to increased circulating levels of statins. 25.
What does BSEP stand for?
BSEP
| Acronym | Definition |
|---|---|
| BSEP | Bachelor of Science in Engineering Physics (various schools) |
| BSEP | Black Sea Environmental Program |
| BSEP | Basic Skills Education Program |
| BSEP | Bicycle Safety Education Program |
What is BSEP deficiency?
BSEP deficiency causes severe intrahepatic cholestasis and liver failure. Progressive familial intrahepatic cholestasis (PFIC) is one of the cholestatic diseases in children, and PFIC type 2 (PFIC2) is a form of infantile cholestatic disorder that occurs despite normal serum levels of gamma glutamyl transferase (GGT)2.
Which is a substrate of the OATP1B1 transporter?
It is responsible for the hepatic uptake of drugs and endogenous compounds from the blood. OATP1B1 substrates often, but by no means always, contain a carboxylic acid moiety. Some important therapeutic drugs, most notably HMG-CoA inhibitors also known as statins, are substrates and/or inhibitors of OATP1B1.
How are OATP transporters used in the liver?
For example, in the liver, an uptake transporter such as organic anion transporting polypeptide 1B1 (OATP1B1) may extract its drug substrates from the portal blood into hepatocytes.
Which is the uptake transporter of polypeptide 1B1?
OATP1B1 (organic anion transporting polypeptide 1B1) OATP1B1 is an uptake transporter exclusively expressed on the sinusoidal side of hepatocytes. It is responsible for the hepatic uptake of drugs and endogenous compounds from the blood.
Where are OATP1B1 and oat1b3 expressed in the hepatocytes?
OATP1B1 and OATP1B3 are transporters that are expressed on the sinusoidal membrane of hepatocytes; they accept a number of therapeutic reagents as their substrates. In vitro and in vivo studies have shown that some drugs inhibit these transporters and cause clinically relevant drug-drug interactions (DDIs).
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