CNT1 Transporter Assay (SLC28A1)

The CNT1 transporter is a nucleoside concentrative transporter that is encoded by the SLC28A1 gene. CNT1 is expressed widely throughout the body and plays an important role in nucleoside salvage pathways that lead to biosynthesis of nucleotides. CNT1 is also localized in the blood brain barrier and can be responsible for hydrophilic compounds entering the brain.

Optivia offers CNT1 substrate and inhibition assays for transport in polarized mammalian cells. We offer a wide range of studies including single concentration screens up to full kinetic studies to determine the IC50 for CNT1 inhibitors as well as Vmax and Km for CNT1 substrates.

CNT1 Transporter Assay

Relevance – nucleosides salvage, nucleoside analog drugs intracellular accumulation Single or Multi-Transporter Model – Single
Transporter Type – Uptake Cell Model – MDCK-II
Assay Type – Intracellular accumulation Exactly Matched Control Cells – yes
Species – Human, rat Probe Substrate – Uridine
Subcellular Localization in Assay Model – Apical Inhibition Positive Control – Adenosine

Clinical & Regulatory Relevance

CNT1 transporter is responsible for nucleoside salvage. Though there is no evidence that nucleoside transporters are directly involved in pathophysiologies, most tumor-derived cell lines express lower level of CNT1.  CNT1 transporter plays a critical role in the cellular delivery of nucleoside analogs, including many antiviral and anticancer drugs such as 3-azido-3-deoxythymidine (AZT) and gemcitabine.

Applications & Therapeutic Areas

Delivery of antiviral/anticancer drugs