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(-)-2'-deoxy-3'-thiacytidine is a potent, highly selective inhibitor of human immunodeficiency virus type 1 and type 2 replication in vitro

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Coates, J A, Cammack, N, Jenkinson, H J, Jowett, A J, Jowett, M I, Pearson, B A, Penn, C R, Rouse, P L, Viner, K C, Cameron, J M·1992·Antimicrobial Agents and Chemotherapy

DOI 10.1128/aac.36.4.733PMC PMC189378

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Abstract

The (-)-enantiomer of 2'-deoxy-3'-thiacytidine (3TC) was found to be a potent and selective inhibitor of human immunodeficiency virus types 1 (HIV-1) and 2 (HIV-2) in vitro. We determined its antiviral activity against a number of laboratory strains of HIV-1 and HIV-2 in a range of CD4-bearing lymphocyte cell lines (mean 50% inhibitory concentration [IC50] range, 4 nM to 0.67 microM). 3TC was also active against a range of HIV-1 strains in peripheral blood lymphocytes (mean IC50 range, 2.5 to 90 nM). The IC50 for cytotoxicity in seven lymphocyte cell cultures, including human peripheral blood lymphocytes, ranged from 0.5 to 6 mM. 3TC had no detectable antiviral activity against a range of other viruses or in cells chronically infected with HIV-1 or HIV-2. The effects of time of addition of the compound and varying the multiplicity of infection on the antiviral activity of 3TC were determined. The results showed that 3TC is a potent and selective inhibitor of HIV-1 and HIV-2 replication in vitro.

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Authors: Coates, J. A., Cammack, N., Jenkinson, H. J., Jowett, A. J., Jowett, M. I., Pearson, B. A., Penn, C. R., Rouse, P. L., Viner, K. C., & Cameron, J. M.
Affiliations: GlaxoSmithKline (United Kingdom) (GB)
Venue: Antimicrobial Agents and Chemotherapy
Publisher: American Society for Microbiology
Published: 1992-04
Volume: 36
Issue: 4
Pages: 733-739
ISSN: 0066-4804 (ISSN-L)
1098-6596
DOI: 10.1128/aac.36.4.733
PMC: PMC189378
OpenAlex: W2001967406
Cited by: 240
References: 26
Citations by year: 2026: 1 · 2025: 1 · 2024: 5 · 2022: 2 · 2020: 4 · 2018: 5 · 2017: 6 · 2016: 2 · 2015: 6 · 2014: 3 · 2013: 1 · 2012: 4
FWCI: 16.70
Type: journal article
Language: en
Open access: green
europepmc.org
Licence: journals.asm.org/non-commercial-tdm-license (tdm)
Locations: Antimicrobial Agents and Chemotherapy (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Infectious Diseases › HIV/AIDS drug development and treatment
Life Sciences › Immunology and Microbiology › Virology › HIV Research and Treatment
Health Sciences › Medicine › Infectious Diseases › Herpesvirus Infections and Treatments
Keywords: zalcitabine, HIV-1, HIV-2, antiviral activity, HIV replication inhibition, enantiomers, peripheral blood lymphocytes, cytotoxicity, drug selectivity
MeSH terms: Cells, Cultured, Humans, RNA-Directed DNA Polymerase, Tritium, Virus Replication, Zidovudine, HIV-1, HIV-2, Giant Cells, Zalcitabine, Didanosine, Cell Death, Lamivudine, HIV Reverse Transcriptase

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(-)-2'-deoxy-3'-thiacytidine is a potent, highly selective inhibitor of human immunodeficiency virus type 1 and type 2 replication in vitro

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