Substrates and Inhibitors of SAMHD1

  title={Substrates and Inhibitors of SAMHD1},
  author={Joseph A. Hollenbaugh and J. Roger Shelton and Sijia Tao and Sheida Amiralaei and P. F. Liu and Xiao Ping Lu and Russell W. Goetze and Longhu Zhou and James H. Nettles and Raymond F Schinazi and Baek ki Kim},
  booktitle={PloS one},
SAMHD1 hydrolyzes 2'-deoxynucleoside-5'-triphosphates (dNTPs) into 2'-deoxynucleosides and inorganic triphosphate products. In this paper, we evaluated the impact of 2' sugar moiety substitution for different nucleotides on being substrates for SAMHD1 and mechanisms of actions for the results. We found that dNTPs ((2'R)-2'-H) are only permissive in the catalytic site of SAMHD1 due to L150 exclusion of (2'R)-2'-F and (2'R)-2'-OH nucleotides. However, arabinose ((2'S)-2'-OH) nucleoside-5… CONTINUE READING