Abstract:
:Combinations of anti-HIV agents including one or two reverse transcriptase inhibitors with a protease inhibitor are potent and effective. However, toxicities, costs and the emergence of drug-resistant organisms have compromised their long-term efficacy in people. A next, likely, target for anti-HIV therapy is HIV-1 integrase. Viral integration, catalyzed by integrase, is absolutely required for HIV replication. L-chicoric acid is a potent and selective inhibitor of HIV-1 integrase that also inhibits HIV-1 replication in cell culture. As a first step in understanding the potential role for integrase inhibitors in clinical medicine, the activities of L-chicoric acid alone and in combination with 2', 3'-dideoxycytidine, zidovudine, and a protease inhibitor, nelfinavir, were tested in vitro against molecular clones of HIV-1 resistant to reverse transcriptase inhibitors. L-chicoric acid was equally effective against a wild-type clone of HIV-1, HIV(NL4-3), or against HIV-1 resistant to either zidovudine or dideoxycytidine. L-chicoric acid was largely synergistic with zidovudine and synergistic with both dideoxycytidine and nelfinavir.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
Beale KK,Robinson WE Jrdoi
10.1016/s0166-3542(00)00083-8subject
Has Abstractpub_date
2000-06-01 00:00:00pages
223-32issue
3eissn
0166-3542issn
1872-9096pii
S0166354200000838journal_volume
46pub_type
杂志文章abstract::Murine cytomegalovirus (MCMV) neither induces a viral thymidine kinase (TK) nor enhances the activity of a cellular TK. Nevertheless, MCMV is highly susceptible to 9-(2-hydroxyethoxymethyl)guanine (acyclovir, ACV). The cellular TK is neither responsible for phosphorylation of ACV nor its anti-MCMV activity. This is cl...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(92)90086-k
更新日期:1992-01-01 00:00:00
abstract::DNA immunizations with the major structural protein VP1 of Coxsackie virus B3 (CVB3) have been previously found to protect BALB/c mice from lethal challenge. Here we report that the other CVB3 capsid proteins, VP2, VP3, and VP4, were less effective at preventing CVB3-caused disease. The application of pCMV/VP1 as a va...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(00)00132-7
更新日期:2001-01-01 00:00:00
abstract::Many flaviviruses, such as Zika virus (ZIKV), Dengue virus (DENV1-4) and yellow fever virus (YFV), are significant human pathogens. Infection with ZIKV, an emerging mosquito-borne flavivirus, is associated with increased risk of microcephaly in newborns and Guillain-Barré syndrome and other complications in adults. Cu...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2017.12.018
更新日期:2018-02-01 00:00:00
abstract::The effects of HIV-1 protease inhibitors on proteolytic processing and infectivity of virions produced from lymphocytes chronically infected with the virus were studied. Protease inhibition was detected by the accumulation of the polyprotein precursors Pr55gag and Pr160gag-pol and their cleavage intermediates. Immunob...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(99)00074-1
更新日期:2000-01-01 00:00:00
abstract::Synthetic flavans, isoflavans and isoflavenes substituted with chloro, cyano and amidino groups were tested for their in vitro activity against poliovirus type 2, Coxsackie virus B4, echovirus type 6 and enterovirus 71. Plaque-reduction assays showed that substituted 3-(2H)-isoflavenes, carrying a double bond in the o...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(95)00088-4
更新日期:1995-05-01 00:00:00
abstract:BACKGROUND:By modulating the antiviral immune response via vitamin D receptor, the active form of vitamin D (1,25-dihydroxyvitamin D, calcitriol) could play a central role in protection against respiratory virus infections. This in vitro study tested the hypothesis that respiratory viruses modulate vitamin D receptor e...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2016.11.004
更新日期:2017-01-01 00:00:00
abstract::Several pyrophosphate analogues have been studied for their effects on avian myeloblastosis virus reverse transcriptase and on cellular DNA polymerase alpha. Examination of structure-activity relationships for these compounds revealed that two acidic groups connected by a short bridge were necessary, but not sufficien...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(82)90028-6
更新日期:1982-05-01 00:00:00
abstract::Serious outbreaks of severe acute respiratory syndrome (SARS), caused by the newly discovered coronavirus SARS-CoV, occurred between late 2002 and early 2003 and there is an urgent need for effective antiviral agents. RNA interference in animals and post-transcriptional gene silencing plants is mediated by small doubl...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2004.09.005
更新日期:2005-01-01 00:00:00
abstract::Serum from wild alligators was collected and tested for antibiotic activity against three enveloped viruses using cell-based assays. Alligator serum demonstrated antiviral activities against human immunodeficiency virus type 1 (HIV-1; IC50=0.9%), West Nile virus (WNV; IC50=4.3%), and Herpes simplex virus type 1 (HSV-1...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2004.12.007
更新日期:2005-04-01 00:00:00
abstract::The effects of caps, dinucleotides, oligonucleotides and polynucleotides on influenza virus RNA polymerase activity have been investigated. The results show that both methyl groups in a cap are necessary for optimal stimulation of polymerase activity. Both m7G(5')ppp(5')Am and ApG stimulated the influenza RNA polymera...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(81)90036-x
更新日期:1981-06-01 00:00:00
abstract::Several nucleoside reverse transcriptase inhibitors are associated with mitochondrial toxicity resulting from inhibition of DNA polymerase-gamma. This study compared the effects on mitochondrial DNA of apricitabine (previously referred to as AVX754 or SPD754), a novel cytidine analogue under development for the treatm...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2007.05.004
更新日期:2007-10-01 00:00:00
abstract::RNase L is a cellular endoribonuclease that is activated by 2',5'-linked oligoadenylates (2-5A), which are unique and specific ligands synthesized by a family of interferon-inducible, dsRNA-activated enzymes named oligoadenylate synthetases. In the typical antiviral pathway, activated RNase L degrades viral and cellul...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2014.01.021
更新日期:2014-04-01 00:00:00
abstract::Double-stranded RNAs induce interferons and cause the development of antiviral and antiproliferative activities. Antiviral activity is related to the production of interferons and other proteins that stimulate various immunologic activities, which appear to contribute to their overall antiproliferative activity. The m...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2004.08.002
更新日期:2004-12-01 00:00:00
abstract::The identification of more effective and less toxic foscarnet (PFA) analogs for antiviral therapy would be useful. We recently synthesized 1-O-octadecyl-sn-glycero-3-phosphonoformic acid (ODG-PFA) and noted a 93-fold increase in its anti-HCMV activity relative to PFA. In addition, the antiviral activity of ODG-PFA in ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(97)00039-9
更新日期:1997-09-01 00:00:00
abstract::We isolated a ganciclovir (GCV)-resistant human cytomegalovirus (HCMV) from a laboratory strain, AD169, and analysed the mutant. Attempts were also made to identify directly the mutated gene. The 50% inhibitory concentration (IC50) of GCV for the mutant strain was five times higher than that of the wild-type strain. T...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(98)00051-5
更新日期:1998-12-01 00:00:00
abstract::JNJ63623872 (formerly known as VX-787) is an inhibitor of influenza A virus polymerases through interaction with the viral PB2 subunit. This interaction blocks the cap-snatching activity of the virus that is essential for virus replication. Previously published work has documented antiviral activity of JNJ63623872 in ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2016.10.009
更新日期:2016-12-01 00:00:00
abstract::Two new influenza virus neuraminidase inhibitors (NAIs), peramivir and laninamivir, were approved in 2010 which resulted to four NAIs that were used during the 2010-2011 influenza season in Japan. This study aims to monitor the susceptibility of influenza virus isolates in 2009-2010 and 2010-2011 influenza seasons in ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2013.06.003
更新日期:2013-09-01 00:00:00
abstract::Therapeutic strategies controlling human cytomegalovirus (hCMV) infection are limited due to adverse side effects and emergence of antiviral resistance variants. A compound being evaluated for treating hCMV disease is maribavir (MBV) which disrupts replication by inhibiting the viral kinase pUL97. Previous studies hav...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2013.09.011
更新日期:2013-11-01 00:00:00
abstract::Anti-herpes simplex virus (HSV) activities of oxyresveratrol in vitro and topical administration in cutaneous HSV-1 infection in mice were examined. The inhibitory concentrations for 50% plaque formation (IC(50)) of oxyresveratrol against HSV-1 clinical isolates and HSV-2 clinical isolates were 20.9-29.5 and 22.2-27.5...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2011.05.013
更新日期:2011-08-01 00:00:00
abstract::In this study we tested whether HIV-1 replication could be inhibited by stable RNAi-mediated knockdown of cellular co-factors. Cell lines capable of expressing shRNAs against 30 candidate co-factors implicated at different steps of the viral replication cycle were generated and analyzed for effects on cell viability a...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2010.11.005
更新日期:2011-01-01 00:00:00
abstract::The ability of hypericin to protect mice from splenomegaly resulting from infection with Friend leukemia virus (FLV) was re-examined in light of recent evidence showing that light is absolutely required for this drug's antiviral activity. FLV-induced splenomegaly was not prevented or ameliorated in mice injected with ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(93)90048-n
更新日期:1993-06-01 00:00:00
abstract::Each year, up to 10,000 cases of infections with the flavivirus tick-borne encephalitis (TBE) virus that affect the central nervous system are reported in Europe and Asia. Due to the potentially severe adverse effects of post-exposure prophylaxis with TBE virus hyperimmunoglobulin, TBE can currently only be treated sy...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2011.10.023
更新日期:2012-01-01 00:00:00
abstract::Respiratory syncytial virus (RSV) is the major cause for respiratory tract disease in infants and young children. Currently, no licensed vaccine or a selective antiviral drug against RSV infections are available. Here, we describe a structure-based drug design approach that led to the synthesis of a novel series of zi...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2015.08.003
更新日期:2015-10-01 00:00:00
abstract::SAMHD1 is a triphosphohydrolase that restricts HIV-1 by limiting the intracellular dNTP pool required for reverse transcription. Although SAMHD1 is expressed and active/unphosphorylated in most cell lines, its restriction activity is thought to be relevant only in non-cycling cells. However, an in depth evaluation of ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2017.03.019
更新日期:2017-06-01 00:00:00
abstract::This study describes the extent of cross-resistance and interactions for selected inhibitors of human cytomegalovirus (HCMV) DNA synthesis and DNA processing. HCMV isolates resistant to the benzimidazole D-ribonucleoside viral DNA processing inhibitors TCRB and BDCRB were sensitive to BAY 38-4766, a non-nucleoside inh...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(02)00094-3
更新日期:2002-10-01 00:00:00
abstract::Argentine hemorrhagic fever is a systemic viral disease caused by Junin virus, with a mortality of 15-30% in untreated individuals. Current specific therapy is highly effective in reducing mortality, and consists of the early administration of immune plasma in defined doses of specific neutralizing antibodies per kg o...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(94)90030-2
更新日期:1994-01-01 00:00:00
abstract::In the present study, the protective effect of 1T1, a lambda-carrageenan extracted from the red seaweed Gigartina skottsbergii was evaluated in a murine model of herpes simplex virus type 2 (HSV-2) genital infection. Six to eight-week-old female BALB/c mice were intravaginally inoculated with a lethal dose of HSV-2 (M...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2004.07.001
更新日期:2004-11-01 00:00:00
abstract::The model of simian immunodeficiency virus (SIV) infection in rhesus macaques was used to evaluate the effects of recombinant human interferon alpha, Hu IFN-alpha 2b and Hu IFN-gamma B,D, at two doses. Administration began 1 day prior to infection and was continued for 90 days postinfection. Both interferons suppresse...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(95)00955-8
更新日期:1996-08-01 00:00:00
abstract::Prunellin, an anti-HIV active compound, was isolated from aqueous extracts of the Chinese medicinal herb, Prunella vulgaris, and purified to chromatographic homogeneity. Infrared and NMR spectroscopy identified prunellin as a polysaccharide. Elemental analyses, precipitation with calcium(II), barium(II), or 9-aminoacr...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(89)90036-3
更新日期:1989-06-01 00:00:00
abstract::Drug resistance testing has proven its use to guide treatment decisions in HIV-1 infected patients. Genotyping is the preferred technique for clinical drug resistance testing. Many factors complicate the interpretation of mutations towards therapy response, such that an interpretation system is necessary to help the c...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2006.05.003
更新日期:2006-09-01 00:00:00