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 herpes simplex virus type-1 (HSV-1) and human immunodeficiency virus type-1 (HIV-1) infected cells was increased 40-fold relative to PFA (Hostetler et al., 1996. Antiviral Res. 31, 59). To evaluate structure-activity relationships further, we synthesized alkoxypropyl esters of foscarnet with varying alkyl chain lengths and degrees of saturation. These compounds were tested in vitro for activity and selectivity in comparison with PFA and ODG-PFA in cells infected with HCMV, HSV-1 or HIV-1. Antiviral activity was strongly dependent on chain length with alkyl ethers 14-18 carbon atoms long exhibiting the greatest antiviral activity against HCMV and HSV-1. In HIV-infected HT4-6C cells, optimal activity was observed at 18-22 carbon chain lengths. The antiviral activities of 1-octadecyloxypropane-3-PFA and 1-docosyloxypropane-3-PFA were 135- and 338-fold greater than that of PFA in HT4-6C cells infected with HIV-1. This also represents a 2.6-6-fold improvement in antiviral activity over ODG-PFA, the previously reported analog.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
Kini GD,Beadle JR,Xie H,Aldern KA,Richman DD,Hostetler KYdoi
10.1016/s0166-3542(97)00039-9subject
Has Abstractpub_date
1997-09-01 00:00:00pages
43-53issue
1eissn
0166-3542issn
1872-9096pii
S0166354297000399journal_volume
36pub_type
杂志文章abstract::Suberoylanilide hydroxamic acid (SAHA) has been assessed in clinical trials as part of a "shock and kill" strategy to cure HIV-infected patients. While it was effective at inducing expression of HIV RNA ("shock"), treatment with SAHA did not result in a reduction of reservoir size ("kill"). We therefore utilized a com...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2015.09.002
更新日期:2015-11-01 00:00:00
abstract::Although canine rabies has been eliminated from industrialized countries, infected dogs remain the primary source of human and livestock exposures in Asia, Africa and much of South America. Human deaths are the most important direct economic impact of canine rabies, followed by livestock losses and the cost of PEP, wh...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2013.03.004
更新日期:2013-05-01 00:00:00
abstract::A series of four mannose(Man)-, three N-acetylglucosamine (GlcNAc)n-, ten N-acetylgalactosamine/galactose(GalNAc/Gal)-, one 5-acetylneuraminic acid (alpha-2,3-Gal/GalNAc)- and one 5-acetylneuroaminic acid(alpha-2,6-Gal/Gal-NAc)-specific plant agglutinins were evaluated for their antiviral activity in vitro. the mannos...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(92)90038-7
更新日期:1992-06-01 00:00:00
abstract::A recombinant baculovirus (vAc-gC1) was constructed that expresses the glycoprotein C (gC) gene of herpes simplex virus type 1 (HSV-1). When Sf9 cells were infected with this recombinant, a protein that was smaller in size than authentic HSV-1 gC was detected by Western blotting using anti-gC polyclonal antibody. The ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(92)90062-a
更新日期:1992-06-01 00:00:00
abstract::We established a sensitive and accurate method for screening of anti-adenovirus agents using the 3-(4,5-dimetylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. MKN-28 cells, which are well-differentiated stomach adenocarcinoma cells, were used for adenovirus (ADV) infection and examined for the anti-ADV act...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(96)06966-5
更新日期:1996-07-01 00:00:00
abstract::Due to diverse pathogenic potentials, there is a growing need for anti-HCMV agents. In this study, we show that treatment with DAPT, a γ-secretase inhibitor (GSI), impairs HCMV replication as assessed by a progeny assay based on immunostaining. This effect is not limited to DAPT because other GSIs with different struc...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2020.104867
更新日期:2020-11-01 00:00:00
abstract::Sheeppox and goatpox, two endemic capripox infections in India, pose a significant economic threat to small ruminant productivity in the subcontinent. Vaccination of all susceptible sheep and goats is the feasible and sustainable means of control. Availability of effective live attenuated vaccines that are inherently ...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2011.06.004
更新日期:2011-09-01 00:00:00
abstract::Dengue virus (DENV) infection is the most prevalent mosquito-borne viral infection of which there is no licensed therapeutic drug available. Previous studies have shown that minocycline, an antibiotic, can inhibit DENV infection in vitro. However, the mechanism is not fully understood. It is known that macrophage migr...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2018.05.002
更新日期:2018-07-01 00:00:00
abstract::Amyotrophic lateral sclerosis (ALS) is a progressive, invariably fatal neurologic disorder resulting from upper and lower motor neuron degeneration, which typically develops during the sixth or seventh decade of life, and is diagnosed based on standard clinical criteria. Its underlying cause remains undetermined. The ...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2013.05.006
更新日期:2013-08-01 00:00:00
abstract:OBJECTIVE:We sought to investigate the differences in monocyte immune responses to the dengue virus (DENV) in those who previously had either severe disease (past SD) or non-severe dengue (past NSD) following a secondary dengue infection. METHOD:Monocytes from healthy individuals who had either past SD (n = 6) or past...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2019.104554
更新日期:2019-09-01 00:00:00
abstract::A novel substituted naphthalenone (TGG-II-23A) has been found that inhibits HIV-1 infection of CEM-SS cells at concentrations that are not cytotoxic. Time of addition experiments indicate that TGG-II-23A functions at a stage of the HIV-1 life cycle at or near reverse transcription. Cell free assays confirmed that TGG-...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(93)90091-v
更新日期:1993-10-01 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::Coxsackievirus A16 (CA16) is one of the main causative agents of hand, foot and mouth disease (HFMD), which is a common infectious disease in children. CA16 infection may lead to severe nervous system damage and even death in humans. However, study of the pathogenesis of CA16 infection and development of vaccines and ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2014.02.015
更新日期:2014-05-01 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::The viral genotype and serum viral level influence the response to interferon (IFN) treatment in patients with chronic hepatitis C virus (HCV) viremia. The aim of this study was to investigate a possible relationship between early virological response and helper T (Th) cell cytokine expansion by 4 weeks of ribavirin (...
journal_title:Antiviral research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/j.antiviral.2005.04.001
更新日期:2005-07-01 00:00:00
abstract::Although in vitro studies have been performed to dissect the mechanism of action of IFNα, detailed in vivo studies on the long-term effects of IFNα on monocytes have not been performed. Here we examined peripheral blood from 14 chronic HCV patients at baseline and 12 weeks after start of IFNα-based therapy. Monocytes ...
journal_title:Antiviral research
pub_type: 临床试验,杂志文章
doi:10.1016/j.antiviral.2014.06.020
更新日期:2014-09-01 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 1-(2-hydroxyethoxymethyl)-6-(phenylthio)thymine (HEPT)-like compounds with homocyclic moieties at the N-1 of the pyrimidinedione, including the highly potent lead compound IQP-0410, inhibit HIV-1 at sub-nanomolar concentrations primarily through a typical non-nucleoside mechanism involving allosteric inhibition at...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2013.09.005
更新日期:2013-11-01 00:00:00
abstract::Despite the high propensity of hepatitis C virus to establish chronic viral persistence, immune-mediated viral clearance occurs in some patients, fostering hopes that therapeutic induction of specific antiviral immune responses might be able to contribute to viral clearance in chronically infected patients. Indeed, re...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2009.02.203
更新日期:2009-06-01 00:00:00
abstract::This study aimed to investigate anti-HBV effect and major active compounds of Su-duxing, a medicine extracted from Chinese herbs. HBV-replicating cell lines HepG2.2.15 (wild-type) and HepG2.A64 (entecavir-resistant) were used for in vitro test. C57BL/6 mice infected by adeno-associated virus carrying 1.3 mer wild-type...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2018.04.017
更新日期:2018-07-01 00:00:00
abstract::Heparan sulfate (HS) is a ubiquitous glycosaminoglycan that serves as a cellular attachment site for a number of significant human pathogens, including respiratory syncytial virus (RSV), human parainfluenza virus 3 (hPIV3), and herpes simplex virus (HSV). Decoy receptors can target pathogens by binding to the receptor...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2015.01.008
更新日期:2015-04-01 00:00:00
abstract::Interleukin (IL)28-B polymorphism has been related to interferon response in the treatment of hepatitis C, but its role in chronic hepatitis B (CHB) therapy is still poorly understood. We aimed to investigate the effect of IL28-B polymorphisms in the treatment with pegylated-interferon (PEG-IFN) of patients with CHB. ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2013.11.014
更新日期:2014-02-01 00:00:00
abstract::High-throughput genomic methods are now being used to study a wide variety of viral diseases, in an effort to understand how host responses to infection can lead either to efficient elimination of the pathogen or the development of severe disease. This article reviews how gene expression studies are addressing importa...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2008.12.005
更新日期:2009-03-01 00:00:00
abstract::On the basis of three different models (namely: ddU, AZT and PMEA), mononucleotide phosphotriester derivatives were designed to be able to liberate the corresponding monophosphate (or phosphonate) inside the cell through a reductase-mediated activation process. It was demonstrated that the use of bis[S-(2-hydroxyethyl...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(93)90093-x
更新日期:1993-10-01 00:00:00
abstract::Human cytomegalovirus (HCMV) infections cause congenital birth defects and disease in immunosuppressed individuals. Antiviral compounds can control infection yet their use is restricted due to concerns of toxicity and the emergence of drug resistant strains. We have evaluated the impact of an RNA Polymerase I (Pol I) ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2018.02.014
更新日期:2018-05-01 00:00:00
abstract:DESIGN:The HIV latent CD4+ T cell reservoir is broadly recognized as a barrier to HIV cure. Induction of HIV expression using protein kinase C (PKC) agonists is one approach under investigation for reactivation of latently infected CD4+ T cells (Beans et al., 2013; Abreu et al., 2014; Jiang et al., 2014; Jiang and Dand...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2016.11.014
更新日期:2017-03-01 00:00:00
abstract::AIDS therapies employing HIV protease inhibitors (PIs) are associated with changes in fat metabolism. However, the cellular mechanisms affected by PIs are not clear. Thus, the affects of PIs on adipocyte differentiation were examined in vitro using C3H10T1/2 stem cells. In these cells the PIs, nelfinavir, saquinavir, ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(00)00102-9
更新日期:2000-08-01 00:00:00
abstract::The role of herpes simplex virus type 1 (HSV-1)-encoded ribonucleotide reductase (RR) has been investigated in mice and guinea pigs using a mutant from which 90% of the large subunit of the enzyme was deleted. The RR mutant was extremely impaired in its ability to induce external vaginal lesions or to cause death in m...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(92)90048-a
更新日期:1992-02-01 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::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