2. Academic Validation
  3. Bifunctional inhibition of HIV-1 reverse transcriptase: a first step in designing a bifunctional triphosphate

Bifunctional inhibition of HIV-1 reverse transcriptase: a first step in designing a bifunctional triphosphate

  • Bioorg Med Chem Lett. 2013 Mar 1;23(5):1511-8. doi: 10.1016/j.bmcl.2012.12.015.
Dongyuan Piao 1,  Aravind Basavapathruni,  Pinar Iyidogan,  Guangxiu Dai,  Wolfgang Hinz,  Adrian S Ray,  Eisuke Murakami,  Joy Y Feng,  Fei You,  Ginger E Dutschman,  David J Austin,  Kathlyn A Parker,  Karen S Anderson
Affiliations

Affiliation

  • 1 Brown University, Department of Chemistry, Providence, RI 02912, United States.
PMID: 23380374 DOI: 10.1016/j.bmcl.2012.12.015
Abstract

The onset of resistance to approved anti-AIDS drugs by HIV necessitates the search for novel inhibitors of HIV-1 Reverse Transcriptase (RT). Developing single molecular agents concurrently occupying the nucleoside and nonnucleoside binding sites in RT is an intriguing idea but the proof of concept has so far been elusive. As a first step, we describe molecular modeling to guide focused chemical syntheses of conjugates having nucleoside (d4T) and nonnucleoside (TIBO) moieties tethered by a flexible polyethylene glycol (PEG) linker. A triphosphate of d4T-6PEG-TIBO conjugate was successfully synthesized that is recognized as a substrate by HIV-1 RT and incorporated into a double-stranded DNA.

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