1,2,4-Triazolo[1,5-
Binding Sites
Drug Design
Enzyme Activation
/ drug effects
HIV Reverse Transcriptase
/ antagonists & inhibitors
Humans
Molecular Conformation
Molecular Docking Simulation
Molecular Dynamics Simulation
Molecular Structure
Protein Binding
Pyrimidines
/ chemistry
Reverse Transcriptase Inhibitors
/ chemistry
Ribonuclease H
/ antagonists & inhibitors
Structure-Activity Relationship
1,2,4-triazolo[1,5-a]pyrimidine
AIDS
HIV-1
RNase H
RT
allosteric inhibitors
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
05 Mar 2020
05 Mar 2020
Historique:
received:
15
01
2020
revised:
25
02
2020
accepted:
03
03
2020
entrez:
11
3
2020
pubmed:
11
3
2020
medline:
15
12
2020
Statut:
epublish
Résumé
Despite great efforts have been made in the prevention and therapy of human immunodeficiency virus (HIV-1) infection, however the difficulty to eradicate latent viral reservoirs together with the emergence of multi-drug-resistant strains require the search for innovative agents, possibly exploiting novel mechanisms of action. In this context, the HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H), which is one of the few HIV-1 encoded enzymatic function still not targeted by any current drug, can be considered as an appealing target. In this work, we repurposed in-house anti-influenza derivatives based on the 1,2,4-triazolo[1,5-
Identifiants
pubmed: 32151066
pii: molecules25051183
doi: 10.3390/molecules25051183
pmc: PMC7179434
pii:
doi:
Substances chimiques
Pyrimidines
0
Reverse Transcriptase Inhibitors
0
reverse transcriptase, Human immunodeficiency virus 1
EC 2.7.7.-
HIV Reverse Transcriptase
EC 2.7.7.49
Ribonuclease H
EC 3.1.26.4
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Références
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