Journal
CHEMBIOCHEM
Volume 12, Issue 18, Pages 2774-2778Publisher
WILEY-BLACKWELL
DOI: 10.1002/cbic.201100567
Keywords
conformation; hENTs and hCNTs; nucleosides; transport
Funding
- Canadian Institutes of Health Research
- Alberta Cancer Foundation
- Canadian Cancer Society Research Institute
- Center for Cancer Research, National Cancer Institute
Ask authors/readers for more resources
The conformational preference of human nucleoside transporters (hNTs) with respect to sugar ring was examined using conformationally fixed purine and pyrimidine nucleosides built on a bicyclo[3.1.0]hexane template. These fixed-conformation nucleosides, methanocarba-deoxyadenosine or methanocarba-deoxycytidine in North (C3'-endo, N-MCdA and N-MCdC) or South (C2'-endo, S-MCdA and S-MCdC) conformations, were used to study inhibition of equilibrative (hENT14) and concentrative (hCNT13) nucleoside transport by individual recombinant hNTs produced in Saccharomyces cerevisiae cells or Xenopus laevis oocytes. Our results indicated that nucleosides in the North conformation were potent inhibitors of transport mediated by hCNTs whereas South nucleosides were inhibitors of hENTs, thus showing differences in the interaction with the hNTs. In summary, hCNTs exhibited strong preferences for North nucleosides whereas hENTs exhibited slight preferences for South nucleosides, demonstrating for the first time different conformational preferences among members of the two families of hNTs.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available