Affordable Access

Substituted naphthalenones as a new structural class of HIV-1 reverse transcriptase inhibitors.

Authors
  • Alam, M
  • Bechtold, C M
  • Patick, A K
  • Skoog, M T
  • Gant, T G
  • Colonno, R J
  • Meyers, A I
  • Li, H
  • Trimble, J
  • Lin, P F
Type
Published Article
Journal
Antiviral Research
Publisher
Elsevier
Publication Date
Oct 01, 1993
Volume
22
Issue
2-3
Pages
131–141
Identifiers
PMID: 7506510
Source
Medline
License
Unknown

Abstract

A novel substituted naphthalenone (TGG-II-23A) has been found that inhibits HIV-1 infection of CEM-SS cells at concentrations that are not cytotoxic. Time of addition experiments indicate that TGG-II-23A functions at a stage of the HIV-1 life cycle at or near reverse transcription. Cell free assays confirmed that TGG-II-23A inhibits HIV-1 reverse transcriptase. Similar to other non-nucleoside inhibitors, TGG-II-23A was specific for HIV-1 and failed to inhibit the replication of HIV-2. The binding site of TGG-II-23A appears to be in close proximity to that of the TIBO-like inhibitors, since a TIBO-resistant HIV-1 was also resistant to TGG-II-23A treatment. TGG-II-23A is a mixed non-competitive inhibitor that exhibits the same template:primer selectivity as other non-nucleoside inhibitors. TGG-II-23A therefore represents a new structural entry into the TIBO/Nevirapine class of inhibitors of HIV-1 reverse transcriptase.

Report this publication

Statistics

Seen <100 times