Targeting HIV-1 Reverse Transcriptase Using a Fragment-Based Approach.
HIV-1
drug discovery
fragment-based drug design
non-nucleoside reverse transcriptase inhibitors (NNRTIs)
reverse transcriptase
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
30 Mar 2023
30 Mar 2023
Historique:
received:
28
12
2022
revised:
24
03
2023
accepted:
24
03
2023
medline:
14
4
2023
entrez:
13
4
2023
pubmed:
14
4
2023
Statut:
epublish
Résumé
Human immunodeficiency virus type I (HIV-1) is a retrovirus that infects cells of the host's immune system leading to acquired immunodeficiency syndrome and potentially death. Although treatments are available to prevent its progression, HIV-1 remains a major burden on health resources worldwide. Continued emergence of drug-resistance mutations drives the need for novel drugs that can inhibit HIV-1 replication through new pathways. The viral protein reverse transcriptase (RT) plays a fundamental role in the HIV-1 replication cycle, and multiple approved medications target this enzyme. In this study, fragment-based drug discovery was used to optimize a previously identified hit fragment (compound
Identifiants
pubmed: 37049868
pii: molecules28073103
doi: 10.3390/molecules28073103
pmc: PMC10095864
pii:
doi:
Substances chimiques
reverse transcriptase, Human immunodeficiency virus 1
EC 2.7.7.-
Reverse Transcriptase Inhibitors
0
HIV Reverse Transcriptase
EC 2.7.7.49
Anti-HIV Agents
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : NIGMS NIH HHS
ID : T32 GM135141
Pays : United States
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