Identification of the amino acid-AZT-phosphoramidase by affinity T7 phage display selection

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6379-81. doi: 10.1016/j.bmcl.2009.09.067. Epub 2009 Sep 22.

Abstract

A CEM cell cDNA T7 phage display library was prepared and used to screen for activating enzymes of phosphoramidate prodrugs of AZT monophosphate. Although, inefficient compared to ribonucleotide based phosphoramidates, hHint 1 was identified as the likely intracellular pronucleotide activating enzyme.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemistry*
  • Amino Acids / metabolism
  • Anti-HIV Agents / metabolism
  • Bacteriophage T7 / metabolism*
  • Cytarabine / pharmacology
  • Drug Delivery Systems
  • Drug Design
  • Humans
  • Peptide Library
  • Phosphoric Acids / chemistry*
  • Virus Replication
  • Zidovudine / metabolism*

Substances

  • Amides
  • Amino Acids
  • Anti-HIV Agents
  • Peptide Library
  • Phosphoric Acids
  • Cytarabine
  • Zidovudine
  • phosphoramidic acid