Journal
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
Volume 36, Issue 1, Pages 7-30Publisher
TAYLOR & FRANCIS INC
DOI: 10.1080/15257770.2016.1210805
Keywords
Nucleoside transport; nucleobase transport; equilibrative nucleoside transporter; membrane protein
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Funding
- Institutional Development Award (IDeA) from the National Institute of General Medical Sciences of the National Institutes of Health [P20GM103639]
- Oklahoma Center for the Advancement of Science [HR11-046]
- OUHSC College of Medicine Alumni Association
- American Heart Association [13PRE17040024]
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Equilibrative nucleoside transporters (ENTs) are polytopic integral membrane proteins that mediate the transport of nucleosides, nucleobases, and therapeutic analogs. The best-characterized ENTs are the human transporters hENT1 and hENT2. However, non-mammalian eukaryotic ENTs have also been studied (e.g., yeast, parasitic protozoa). ENTs are major pharmaceutical targets responsible for modulating the efficacy of more than 30 approved drugs. However, the molecular mechanisms and chemical determinants of ENT-mediated substrate recognition, binding, inhibition, and transport are poorly understood. This review highlights findings on the characterization of ENTs by surveying studies on genetics, permeant and inhibitor interactions, mutagenesis, and structural models of ENT function.
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