Novel variants provide differential stabilisation of human equilibrative nucleoside transporter 1 states.

ABSTRACT: Human equilibrative nucleoside transporters represent a major pharmaceutical target for cardiac, cancer and viral therapies. Understanding the molecular basis for transport is crucial for the development of improved therapeutics through structure-based drug design. ENTs have been proposed to utilise an alternating access mechanism of action, similar to that of the major facilitator superfamily. However, ENTs lack functionally-essential features of that superfamily, suggesting that they may use a different transport mechanism. Understanding the molecular basis of their transport requires insight into diverse conformational states. Differences between intermediate states may be discrete and mediated by subtle gating interactions, such as salt bridges. We identified four variants of human equ

SUBMITTER: Boakes JC 

PROVIDER: S-EPMC9678926 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature