93 Human immunodeficiency virus type 1 (HIV-1) mutant strains emerging after combination of HIV-1-specific inhibitors in cell culture

1993 ◽  
Vol 20 ◽  
pp. 94
Keyword(s):  
Cell Culture ◽  
Human Immunodeficiency Virus ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Immunodeficiency Virus ◽  
Mutant Strains ◽  
Hiv 1 ◽  
Specific Inhibitors

scholarly journals Differential activities of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives against different human immunodeficiency virus type 1 mutant strains.

1995 ◽  
Vol 39 (4) ◽  
pp. 998-1002 ◽  
Author(s):  
J Balzarini ◽  
M Baba ◽  
E De Clercq
Keyword(s):  
Human Immunodeficiency Virus ◽  
Amino Acid ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Wild Type ◽  
Immunodeficiency Virus ◽  
Mutant Strains ◽  
Rt Inhibitors ◽  
Hiv 1

A series of 23 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives that were highly potent inhibitors of wild-type human immunodeficiency virus type 1 strain IIIB (HIV-1/IIIB) replication in CEM cells were evaluated against a panel of HIV-1 mutant strains containing the replacement of leucine by isoleucine at position 100 (100-Leu-->Ile), 103-Lys-->Asn, 106-Val-->Ala, 138-Glu-->Lys, 181-Tyr-->Cys, 181-Tyr-->Ile, or 188-Tyr-->His in their reverse transcriptase (RT). A different structure-antiviral activity relationship was found, depending on the nature of the mutated amino acid in the HIV-1 RT. The results show that 5-ethyl-1-ethoxymethyl-6-(3,5-dimethylbenzyl)uracil, 5-ethyl-1-ethoxymethyl-6-(3,5-dimethylphenylthio)uracil, and 5-ethyl-1-ethoxymethyl-6-(3,5-dimethylphenylthio)-2-thiouracil remain active against the majority of viruses containing single mutations which confer resistance to nonnucleoside RT inhibitors.

TSAO Derivatives: Highly Specific Inhibitors of Human Immunodeficiency Virus Type-1 (HIV-1) Replication

1995 ◽  
Vol 14 (3) ◽  
pp. 585-594 ◽  
Author(s):  
Maria Camarasa ◽  
Maria Péarez-Péarez ◽  
Sonsoles Velázquez ◽  
Ana San-Féalix ◽  
Rosa Alvarez ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Immunodeficiency Virus ◽  
Hiv 1 ◽  
Specific Inhibitors

scholarly journals Specific Inhibition of Human Immunodeficiency Virus Type 1 (HIV-1) Integration in Cell Culture: Putative Inhibitors of HIV-1 Integrase

2001 ◽  
Vol 45 (9) ◽  
pp. 2510-2516 ◽  
Author(s):  
Nick Vandegraaff ◽  
Raman Kumar ◽  
Helen Hocking ◽  
Terrence R. Burke ◽  
John Mills ◽  
...  
Keyword(s):  
Cell Culture ◽  
Human Immunodeficiency Virus ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Integrase Inhibitors ◽  
Pcr Assay ◽  
Hiv Dna ◽  
Immunodeficiency Virus ◽  
Hiv 1

ABSTRACT To study the effect of potential human immunodeficiency virus type 1 (HIV-1) integrase inhibitors during virus replication in cell culture, we used a modified nested Alu-PCR assay to quantify integrated HIV DNA in combination with the quantitative analysis of extrachromosomal HIV DNA. The two diketo acid integrase inhibitors (L-708,906 and L-731,988) blocked the accumulation of integrated HIV-1 DNA in T cells following infection but did not alter levels of newly synthesized extrachromosomal HIV DNA. In contrast, we demonstrated that L17 (a member of the bisaroyl hydrazine family of integrase inhibitors) and AR177 (an oligonucleotide inhibitor) blocked the HIV replication cycle at, or prior to, reverse transcription, although both drugs inhibited integrase activity in cell-free assays. Quercetin dihydrate (a flavone) was shown to not have any antiviral activity in our system despite reported anti-integration properties in cell-free assays. This refined Alu-PCR assay for HIV provirus is a useful tool for screening anti-integration compounds identified in biochemical assays for their ability to inhibit the accumulation of integrated HIV DNA in cell culture, and it may be useful for studying the effects of these inhibitors in clinical trials.

ChemInform Abstract: TSAO Derivatives: Highly Specific Inhibitors of Human Immunodeficiency Virus Type-1 (HIV-1) Replication

ChemInform ◽  
2010 ◽  
Vol 26 (39) ◽  
pp. no-no
Author(s):  
M. J. CAMARASA ◽  
M. J. PEREZ-PEREZ ◽  
S. VELAZQUEZ ◽  
A. SAN-FELIX ◽  
R. ALVAREZ ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Immunodeficiency Virus ◽  
Hiv 1 ◽  
Specific Inhibitors

scholarly journals Inhibition of Human Immunodeficiency Virus Type 1 Integration by Diketo Derivatives

2002 ◽  
Vol 46 (10) ◽  
pp. 3292-3297 ◽  
Author(s):  
Wim Pluymers ◽  
Godwin Pais ◽  
Bénédicte Van Maele ◽  
Christophe Pannecouque ◽  
Valery Fikkert ◽  
...  
Keyword(s):  
Cell Culture ◽  
Human Immunodeficiency Virus ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Effective Concentration ◽  
Fusion Inhibitors ◽  
Immunodeficiency Virus ◽  
Hiv Integration ◽  
Hiv 1

ABSTRACT A series of diketo derivatives was found to inhibit human immunodeficiency virus type 1 (HIV-1) integrase activity. Only L-708,906 inhibited the replication of HIV-1(IIIB) (50% effective concentration, 12 μM), HIV-1 clinical strains, HIV-1 strains resistant to reverse transcriptase or fusion inhibitors, HIV-2 (ROD strain) and simian immunodeficiency virus (MAC251). The combinations of L-708,906 with zidovudine, nevirapine, or nelfinavir proved to be subsynergistic. In cell culture, addition of L-708,906 could be postponed for 7 h after infection, a moment coinciding with HIV integration. Inhibition of integration in cell culture was confirmed by quantitative Alu-PCR.

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