Evidence map›Paper›PMID 9517921›Full record

ArticleAntimicrobial agents and chemotherapy1998

Inhibition of acute-, latent-, and chronic-phase human immunodeficiency virus type 1 (HIV-1) replication by a bistriazoloacridone analog that selectively inhibits HIV-1 transcription.

J A Turpin, R W Buckheit, D Derse, M Hollingshead, K Williamson, C Palamone, M C Osterling, S A Hill, L Graham, C A Schaeffer and 5 more

Open access · bronzeAbstract read
In one paragraph

Article in Antimicrobial agents and chemotherapy, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
0.8field-weighted citation impact, top 30% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

14 citing papers in PubMed, 51 citations in OpenAlex.

  1. Acridones as promising drug candidates against Oropouche virus.Current research in microbial sciences · 2024
    Article
  2. Review
  3. Review
  4. Article
  5. Targeting HIV transcription: the quest for a functional cure.Current topics in microbiology and immunology · 2015
    Review
  6. Article
  7. Article
  8. Review
  9. Article
  10. Article
  11. Article
  12. Article
  13. Article
  14. Strategies in the design of antiviral drugs.Nature reviews. Drug discovery · 2002
    Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

15 authors at 4 institutions in 1 country.

J A TurpinLaboratory of Antiviral Drug Mechanisms, Developmental Therapeutics Program, SAIC Frederick, Maryland 21702-1201, USA.
R W Buckheit
D Derse
M Hollingshead
K Williamson
C Palamone
M C Osterling
S A Hill
L Graham
C A Schaeffer
M Bu
M Huang
W M Cholody
C J Michejda
W G Rice
Science Applications International Corporation (United States) · USFrederick National Laboratory for Cancer Research · USSouthern Research Institute · USChildren's Diagnostic & Treatment Center · US

Funding

PHS HHS N01-C0-46000PHS HHS N01-C0-56000
6 · The paper itself

Abstract

Nanomolar concentrations of temacrazine (1,4-bis[3-(6-oxo-6H-v-triazolo[4,5,1-de]acridin-5-yl)amino-propyl ]piperazine) were discovered to inhibit acute human immunodeficiency virus type 1 (HIV-1) infections and suppress the production of virus from chronically and latently infected cells containing integrated proviral DNA. This bistriazoloacridone derivative exerted its mechanism of antiviral action through selective inhibition of HIV-1 transcription during the postintegrative phase of virus replication. Mechanistic studies revealed that temacrazine blocked HIV-1 RNA formation without interference with the transcription of cellular genes or with events associated with the HIV-1 Tat and Rev regulatory proteins. Although temacrazine inhibited the in vitro 3' processing and strand transfer activities of HIV-1 integrase, with a 50% inhibitory concentration of approximately 50 nM, no evidence of an inhibitory effect on the intracellular integration of proviral DNA into the cellular genome during the early phase of infection could be detected. Furthermore, temacrazine did not interfere with virus attachment or fusion to host cells or the enzymatic activities of HIV-1 reverse transcriptase or protease, and the compound was not directly virucidal. Demonstration of in vivo anti-HIV-1 activity by temacrazine identifies bistriazoloacridones as a new class of pharmaceuticals that selectively blocks HIV-1 transcription.

Indexed as

AcridinesAcute-Phase ReactionAnti-HIV AgentsCells, CulturedGene Products, revGene Products, tatHIV-1HumansPiperazinesrev Gene Products, Human Immunodeficiency Virustat Gene Products, Human Immunodeficiency VirusTranscription, GeneticVirus ReplicationAcridinesAnti-HIV AgentsGene Products, revGene Products, tatPiperazinesrev Gene Products, Human Immunodeficiency Virustat Gene Products, Human Immunodeficiency Virustemacrazine

Identifiers

PMID9517921
PMCPMC105487
OpenAlexW2154441401

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.