OATP1B3
Overview[edit | edit source]
OATP1B3 (Organic Anion Transporting Polypeptide 1B3) is a protein encoded by the SLCO1B3 gene in humans. It is a member of the organic anion transporting polypeptides (OATPs) family, which are responsible for the uptake of a wide range of endogenous and exogenous organic compounds, including drugs, hormones, and toxins, into cells. OATP1B3 is primarily expressed in the liver and plays a crucial role in hepatic drug uptake and metabolism.
Structure[edit | edit source]
OATP1B3 is a transmembrane protein that consists of 702 amino acids. It is characterized by 12 transmembrane domains, with both the N-terminus and C-terminus located intracellularly. The structure of OATP1B3 allows it to function as a transporter by facilitating the movement of substrates across the cell membrane.
Function[edit | edit source]
OATP1B3 is involved in the hepatic uptake of a variety of substrates, including:
- Bilirubin
- Bile acids
- Thyroid hormones
- Steroid hormones
- Various pharmaceutical drugs such as statins, anticancer drugs, and antibiotics.
The transport activity of OATP1B3 is essential for the proper metabolism and clearance of these compounds from the body. It plays a significant role in drug-drug interactions and can influence the pharmacokinetics and pharmacodynamics of medications.
Clinical Significance[edit | edit source]
Mutations or polymorphisms in the SLCO1B3 gene can affect the function of OATP1B3, leading to altered drug metabolism and disposition. This can result in variations in drug efficacy and toxicity among individuals. OATP1B3 is also implicated in certain liver diseases and conditions, such as Dubin-Johnson syndrome, where impaired transport function leads to the accumulation of bilirubin and other substrates.
Research and Applications[edit | edit source]
OATP1B3 is a subject of extensive research due to its role in drug transport and metabolism. Understanding the function and regulation of OATP1B3 can aid in the development of new therapeutic strategies and the optimization of drug dosing regimens. It is also a target for drug development, with efforts to design inhibitors or modulators that can alter its activity for therapeutic benefit.
Also see[edit | edit source]
References[edit | edit source]
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