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NTCP - Sodium Taurocholate Cotransporting Polypeptide

In cooperation with the University Medicine of Greifswald, Department of Clinical Pharmacology, Primacyt is offering a broad range of stably transfected HEK293 cells expressing human NTCP. All cells are validated for expression rates, localization of the overexpressed transporter protein and functionality. We analyze the uptake functions using suitable substrates, inhibiting the uptake by adding the reference inhibitors.


Sodium (Na+) taurocholate cotransporting polypeptide (NTCP, gene symbol SLC10A1) belongs to the solute carrier family of transporters (SLC10A1) and expressed on the basolateral membrane of hepatocytes. It transports predominantly bile acids from the sinusoidal membrane, which occurs largely in a sodium-dependent manner. NTCP is one of the key transporters in the enterohepatic circulation of bile acids. As it is an important hepatic bile acids transporter, inhibition by drugs may be relevant to hepatotoxicity.

A cell platform using stable transfected HEK293 cells expressing human NTCP was generated and validated. We analyze the uptake functions using suitable substrates, inhibiting the uptake by adding the reference inhibitors.

NTCP - Sodium Taurocholate Cotransporting Polypeptide

Sodium (Na+) taurocholate cotransporting polypeptide (NTCP, gene symbol SLC10A1) is a sodium-dependent uptake transporter expressed on the basolateral membrane of hepatocytes. NTCP consists of seven predicted transmembrane domains and is responsible for the basolateral uptake of bile acids from the portal blood into hepatocytes. Therefore, NTCP is together with ASBT and the bile salt export pump (BSEP) one of the key transporters in the enterohepatic circulation of bile acids.
Apart from the transport of bile acids (e.g., taurocholate, cholate, glycoursodeoxycholate, and tauroursodeoxycholate), NTCP is also a transporter of bromosulfophthalein (BSP), estrone-3-sulfate or statins like pitavastatin or rosuvastatin and of thyroid hormones (for a review see Anwer et al., 2014). Interestingly, some substrate differences have been shown between rodent and human NTCP, what should be taken into account when extrapolating rodent data for human clinical relevance. Moreover, NTCP has been shown to act as a receptor and transporter for hepatitis B and hepatitis D viruses (HBV, HDV).


Literature

Anwer MS, Stieger B: Sodium-dependent bile salt transporters of the SLC10A transporter family: more than solute transporters. Pflugers Arch. 2014, 466: 77-89. doi: 10.1007/s00424-013-1367-0. Epub 2013 Oct 3.