Experimental and computational approaches for evaluating molecule interactions with equilibrative nucleoside transporters 1 and 2.

ABSTRACT: Equilibrative nucleoside transporters (ENTs) facilitate the equilibrative movement of nucleosides and nucleobases across cell membranes in a sodium-independent manner. ENT1 (SLC29A1) and ENT2 (SLC29A2) also transport nucleoside analogs and can affect the pharmacokinetics and pharmacodynamics of drugs used in cancer, viral infections, and inflammatory disorders. ENT1 and ENT2 may be differentiated functionally by their sensitivity to inhibition by nitrobenzylthioinosine (NBMPR), and we used this difference in NBMPR sensitivity to create a HeLa-based ENT2 inhibition assay. We then screened a library of 1600 diverse compounds composed of drugs and natural products for inhibition against ENT1 and ENT2, selecting a subset of compounds for side-by-side comparison of dose-response studies. We use

SUBMITTER: Martinez-Guerrero LJ 

PROVIDER: S-EPMC12486301 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature