Inhibition of the reverse transcriptase from HIV by 3'-azido-3'-deoxythymidine triphosphate and its threo analogue.

Abstract:

:3'-Azido-3'-deoxythymidine triphosphate (erythro) and its threo isomer were synthesized and investigated for their inhibition of HIV reverse transcriptase from virus isolate U 937/HTLV-III. The erythro isomer was a competitive inhibitor of the reaction directed by (rA)n(dT)12-18 and the Ki value was 0.0022 microM. The threo isomer was at least 100-fold less active. The inhibition was specific for dTMP incorporation, and dGMP incorporation using (rC)n(dG)12-18 as template/primer was not affected. The Km value for dTTP varied between 0.7 microM and 1.7 microM. Reverse transcriptase from nine HIV isolates were tested for inhibition by the erythro isomer and only slight differences in sensitivity were observed.

journal_name

Antiviral Res

journal_title

Antiviral research

authors

Vrang L,Bazin H,Remaud G,Chattopadhyaya J,Oberg B

doi

10.1016/0166-3542(87)90002-7

subject

Has Abstract

pub_date

1987-03-01 00:00:00

pages

139-49

issue

3

eissn

0166-3542

issn

1872-9096

pii

0166-3542(87)90002-7

journal_volume

7

pub_type

杂志文章
  • Are in vitro hepatitis B core promoter mutations important for clinical alterations in viral load?

    abstract::In vitro studies of HBV core promoter mutations in hepatoma cell lines suggest that some mutations in core promoter transcription factor binding sites result in reduced core promoter activity and viral replication. We sought to validate this hypothesis using clinical samples with viral load differences before and afte...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2005.11.005

    authors: Cheng Y,Seet BL,Ong CS,Wasser S,Tan TM,Peter FJ,Lim SG

    更新日期:2006-03-01 00:00:00

  • Effects of apricitabine and other nucleoside reverse transcriptase inhibitors on replication of mitochondrial DNA in HepG2 cells.

    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

    authors: de Baar MP,de Rooij ER,Smolders KG,van Schijndel HB,Timmermans EC,Bethell R

    更新日期:2007-10-01 00:00:00

  • Effect of chloro-, cyano-, and amidino-substituted flavanoids on enterovirus infection in vitro.

    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

    authors: Genovese D,Conti C,Tomao P,Desideri N,Stein ML,Catone S,Fiore L

    更新日期:1995-05-01 00:00:00

  • Cathelicidin antimicrobial peptides suppress EV71 infection via regulating antiviral response and inhibiting viral binding.

    abstract::Cathelicidin antimicrobial peptides (human LL-37 and mouse CRAMP) are mainly virucidal to enveloped virus. However, the effects and relative mechanisms of LL-37 and CRAMP on non-enveloped virus are elusive. We herein found that CRAMP expression was significantly up-regulated post non-enveloped Enterovirus 71 (EV71) in...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2021.105021

    authors: Yu J,Dai Y,Fu Y,Wang K,Yang Y,Li M,Xu W,Wei L

    更新日期:2021-01-25 00:00:00

  • Antiviral action of 5-amino-2-(2-dimethyl-aminoethyl)benzo-[de]-isoquinolin-1,3-dion e.

    abstract::A newly synthesized imide derivative of 3-nitro-1,8-naphthalic acid, 5-amino-2-(2-dimethylaminoethyl)benzo-[de]-isoquinolin-1,3-dione (designated M-FA-142), was tested on chick embryo cells against herpes simplex virus type 1 (HSV-1) and vaccinia virus (VV), and on Vero cells against African swine fever virus (ASFV). ...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/0166-3542(84)90018-4

    authors: García Gancedo A,Gil-Fernández C,Vilas P,Pérez S,Rodriguez F,Paez E,Braña MF,Roldán CM

    更新日期:1984-08-01 00:00:00

  • Metal-chelating 3-hydroxypyrimidine-2,4-diones inhibit human cytomegalovirus pUL89 endonuclease activity and virus replication.

    abstract::Human cytomegalovirus terminase complex cleaves the concatemeric genomic viral DNA into unit lengths during genome packaging and particle assembly. Terminase complex ATPase and endonuclease activity is provided by the viral protein pUL89. pUL89 is an attractive drug target because its activities are required for infec...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2018.01.015

    authors: Wang Y,Tang J,Wang Z,Geraghty RJ

    更新日期:2018-04-01 00:00:00

  • Antiviral activities of lactoferrin.

    abstract::Lactoferrin (LF) is an iron binding glycoprotein that is present in several mucosal secretions. Many biological functions have been ascribed to LF. One of the functions of LF is the transport of metals, but LF is also an important component of the non-specific immune system, since LF has antimicrobial properties again...

    journal_title:Antiviral research

    pub_type: 杂志文章,评审

    doi:10.1016/s0166-3542(01)00195-4

    authors: van der Strate BW,Beljaars L,Molema G,Harmsen MC,Meijer DK

    更新日期:2001-12-01 00:00:00

  • A viral subunit immunogen for porcine transmissible gastroenteritis.

    abstract::An immunogenic component was isolated from both the Illinois (propagated in young swine) and the Miller (cell culture-adapted) strains of porcine transmissible gastroenteritis (TGE) virus. The viral subunit was released from the virion by sonication and was separated from intact virus and other viral components by iso...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/0166-3542(83)90027-x

    authors: Gough PM,Ellis CH,Frank CJ,Johnson CJ

    更新日期:1983-09-01 00:00:00

  • Nuclear localization of dengue virus (DENV) 1-4 non-structural protein 5; protection against all 4 DENV serotypes by the inhibitor Ivermectin.

    abstract::Infection by one of the 4 distinct serotypes of dengue virus (DENV) threatens >40% of the world's population, with no efficacious vaccine or antiviral agent currently available. DENV replication through the virus-encoded nonstructural protein (NS) 5 protein occurs in the infected cell cytoplasm, but NS5 from DENV2 has...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2013.06.002

    authors: Tay MY,Fraser JE,Chan WK,Moreland NJ,Rathore AP,Wang C,Vasudevan SG,Jans DA

    更新日期:2013-09-01 00:00:00

  • Germacrone inhibits early stages of influenza virus infection.

    abstract::Highly pathogenic influenza viruses pose a serious public health threat to humans. Although vaccines are available, antivirals are needed to efficiently control disease progression and virus transmission due to the emergence of drug-resistant viral strains. In this study, germacrone, which is a major component of the ...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2013.09.021

    authors: Liao Q,Qian Z,Liu R,An L,Chen X

    更新日期:2013-12-01 00:00:00

  • Effect of increasing thiolation of the polycytidylic acid strand of poly I:poly C on the alpha, beta and gamma interferon-inducing properties, antiviral and antiproliferative activities.

    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

    authors: Chadha KC,Dembinski WE,Dunn CB,Aradi J,Bardos TJ,Dunn JA,Ambrus JL Sr

    更新日期:2004-12-01 00:00:00

  • 6-Thioguanine inhibits rotavirus replication through suppression of Rac1 GDP/GTP cycling.

    abstract::Rotavirus infection has emerged as an important cause of complications in organ transplantation recipients and might play a role in the pathogenesis of inflammatory bowel disease (IBD). 6-Thioguanine (6-TG) has been widely used as an immunosuppressive drug for organ recipients and treatment of IBD in the clinic. This ...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2018.06.011

    authors: Yin Y,Chen S,Hakim MS,Wang W,Xu L,Dang W,Qu C,Verhaar AP,Su J,Fuhler GM,Peppelenbosch MP,Pan Q

    更新日期:2018-08-01 00:00:00

  • Global update on the susceptibilities of human influenza viruses to neuraminidase inhibitors and the cap-dependent endonuclease inhibitor baloxavir, 2017-2018.

    abstract::The global analysis of neuraminidase inhibitor (NAI) susceptibility of influenza viruses has been conducted since the 2012-13 period. In 2018 a novel cap-dependent endonuclease inhibitor, baloxavir, that targets polymerase acidic subunit (PA) was approved for the treatment of influenza virus infection in Japan and the...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2020.104718

    authors: Takashita E,Daniels RS,Fujisaki S,Gregory V,Gubareva LV,Huang W,Hurt AC,Lackenby A,Nguyen HT,Pereyaslov D,Roe M,Samaan M,Subbarao K,Tse H,Wang D,Yen HL,Zhang W,Meijer A

    更新日期:2020-03-01 00:00:00

  • Aprotinin aerosol treatment of influenza and paramyxovirus bronchopneumonia of mice.

    abstract::The therapeutic efficacy of aerosolized aprotinin, a natural proteinase inhibitor, against influenza and paramyxovirus bronchopneumonia of mice is shown. Small-particle aerosol of aprotinin solution was generated by a Collison type nebulizer and infected mice were exposed to aerosol atmosphere by four 30-40 min incuba...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/0166-3542(94)90038-8

    authors: Ovcharenko AV,Zhirnov OP

    更新日期:1994-02-01 00:00:00

  • HIV protease inhibitors block adipogenesis and increase lipolysis in vitro.

    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

    authors: Lenhard JM,Furfine ES,Jain RG,Ittoop O,Orband-Miller LA,Blanchard SG,Paulik MA,Weiel JE

    更新日期:2000-08-01 00:00:00

  • Susceptibilities of enterovirus D68, enterovirus 71, and rhinovirus 87 strains to various antiviral compounds.

    abstract::Compounds were evaluated for antiviral activity in rhabdomyosarcoma (RD) cells against a recent 2014 clinical isolate of enterovirus D68 (EV-D68), a 1962 strain of EV-68D, rhinovirus 87 (RV-87, serologically the same as EV-D68), and enterovirus 71 (EV-71). Test substances included known-active antipicornavirus agents ...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2016.04.003

    authors: Smee DF,Evans WJ,Nicolaou KC,Tarbet EB,Day CW

    更新日期:2016-07-01 00:00:00

  • Pharmacokinetics of zidovudine and didanosine during combination therapy.

    abstract::While the combination of zidovudine and didanosine is used in HIV-infected patients with more advanced disease, the possibility of a pharmacokinetic interaction between these two drugs remains controversial. Zidovudine doses of 50, 100, and 200 mg, combined with 67, 167, and 250 mg of didanosine were evaluated in 11 a...

    journal_title:Antiviral research

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1016/0166-3542(95)00032-h

    authors: Morse GD,Shelton MJ,Ho M,Bartos L,DeRemer M,Ragni M

    更新日期:1995-08-01 00:00:00

  • Altered monocyte response to the dengue virus in those with varying severity of past dengue infection.

    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

    authors: Kamaladasa A,Gomes L,Wijesinghe A,Jeewandara C,Toh YX,Jayathilaka D,Ogg GS,Fink K,Malavige GN

    更新日期:2019-09-01 00:00:00

  • The mannose-specific plant lectins from Cymbidium hybrid and Epipactis helleborine and the (N-acetylglucosamine)n-specific plant lectin from Urtica dioica are potent and selective inhibitors of human immunodeficiency virus and cytomegalovirus replication

    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

    authors: Balzarini J,Neyts J,Schols D,Hosoya M,Van Damme E,Peumans W,De Clercq E

    更新日期:1992-06-01 00:00:00

  • Comparative therapeutic effect of aerosolized and oral rimantadine HCl in experimental human influenza A virus infection.

    abstract::Thirty-six adult volunteers were inoculated intranasally with 7.2 log10 egg infectious doses 50% of an attenuated A/Khabarovsk/77/H1N1 virus. Twenty-four hours later volunteers were begun on both aerosol treatments (rimantadine HCl 25 mg in saline or saline, 10 min exposure twice daily) and oral medications (rimantadi...

    journal_title:Antiviral research

    pub_type: 临床试验,杂志文章

    doi:10.1016/0166-3542(82)90016-x

    authors: Hayden FG,Zylidnikov DM,Iljenko VI,Padolka YV

    更新日期:1982-08-01 00:00:00

  • Effect of imexon treatment on Friend virus complex infection using genetically defined mice as a model for HIV-1 infection.

    abstract::Imexon (4-imino-1,4-diazobicyclo-3.1.0-hexan-2-one) was moderately effective in the treatment of a retroviral infection in a genetically defined murine model. The animal model consisted of a Friend virus complex (FV) infection in a hybrid mouse strain, (B10.A x A/WySn)F1, which has similarities with acquired immune de...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/0166-3542(91)90040-x

    authors: Morrey JD,Warren RP,Okleberry KM,Burger RA,Chirigos MA,Sidwell RW

    更新日期:1991-01-01 00:00:00

  • Inhibition of cytomegalovirus immediate early gene expression: a therapeutic option?

    abstract::The replication cycle of the human cytomegalovirus (HCMV) is characterized by the expression of immediate early (IE), early (E), and late (L) gene regions. Current antiviral strategies are directed against the viral DNA polymerase expressed during the early phase of infection. The regulation of the IE-1 and IE-2 gene ...

    journal_title:Antiviral research

    pub_type: 杂志文章,评审

    doi:10.1016/s0166-3542(01)00126-7

    authors: Scholz M,Doerr HW,Cinatl J

    更新日期:2001-03-01 00:00:00

  • In silico study supports the efficacy of a reduced dose regimen for stavudine.

    abstract::Stavudine (d4T) is used extensively as part of HAART in resource poor settings, despite its toxicities. The revised WHO guidelines specify replacement of d4T with less toxic but more expensive drugs when feasible, and that d4T doses be standardized to 30 mg twice daily (bid) (irrespective of body-weight), from the app...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2011.08.004

    authors: Hurwitz SJ,Schinazi RF

    更新日期:2011-11-01 00:00:00

  • BX795 demonstrates potent antiviral benefits against herpes simplex Virus-1 infection of human cell lines.

    abstract::Herpes simplex virus-1 (HSV-1) infection is known to cause skin blisters, keratitis as well as deadly cases of encephalitis in some situations. Only a few therapeutic modalities are available for this globally prevalent infection. Very recently, a small molecule BX795 was identified as an inhibitor of HSV-1 protein sy...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2020.104814

    authors: Iqbal A,Suryawanshi R,Yadavalli T,Volety I,Shukla D

    更新日期:2020-08-01 00:00:00

  • Use of preconditioned human phagocytes for extracorporeal adsorption of viruses.

    abstract::Conventional treatment of severe viral disease is limited by the narrow choice as well as the often-significant side effects or lack of clear efficacy of antiviral chemotherapy. At the same time, however, it is known that a reduction in viral load leads to significant clinical improvement in a number of important vira...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2010.05.007

    authors: Oberender F,Oberender H,Altrichter J,Reisinger EC,Mitzner SR

    更新日期:2010-08-01 00:00:00

  • An attenuated EIAV vaccine strain induces significantly different immune responses from its pathogenic parental strain although with similar in vivo replication pattern.

    abstract::The EIAV (equine infectious anemia virus) multi-species attenuated vaccine EIAV(DLV121) successfully prevented the spread of equine infectious anemia (EIA) in China in the 1970s and provided an excellent model for the study of protective immunity to lentiviruses. In this study, we compared immune responses induced by ...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2011.08.016

    authors: Lin YZ,Shen RX,Zhu ZY,Deng XL,Cao XZ,Wang XF,Ma J,Jiang CG,Zhao LP,Lv XL,Shao YM,Zhou JH

    更新日期:2011-11-01 00:00:00

  • Inhibition of adenovirus serotype 14 infection by octadecyloxyethyl esters of (S)-[(3-hydroxy-2-phosphonomethoxy)propyl]- nucleosides in vitro.

    abstract::On September 22, 2008, a physician on Prince of Wales Island, Alaska, notified the Alaska Department of Health and Social Services (ADHSS) of an unusually high number of adult patients with recently diagnosed pneumonia (n = 10), including three persons who required hospitalization and one who died. ADHSS and CDC condu...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/j.antiviral.2018.08.004

    authors: Kumaki Y,Woolcott JD,Roth JP,Mclean TZ,Smee DF,Barnard DL,Valiaeva N,Beadle JR,Hostetler KY

    更新日期:2018-10-01 00:00:00

  • Heparin octasaccharide decoy liposomes inhibit replication of multiple viruses.

    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

    authors: Hendricks GL,Velazquez L,Pham S,Qaisar N,Delaney JC,Viswanathan K,Albers L,Comolli JC,Shriver Z,Knipe DM,Kurt-Jones EA,Fygenson DK,Trevejo JM,Wang JP,Finberg RW

    更新日期:2015-04-01 00:00:00

  • The combination of interferon alpha-2b and n-butyl deoxynojirimycin has a greater than additive antiviral effect upon production of infectious bovine viral diarrhea virus (BVDV) in vitro: implications for hepatitis C virus (HCV) therapy.

    abstract::Interferon alpha-2b (IFN) alone or in combination with Ribavirin is approved in the United States for the treatment of chronic hepatitis C virus (HCV) infection. We have previously reported that the glucosidase inhibitor, n-butyl deoxynojirimycin (nB-DNJ) inhibits the production of infectious bovine diarrhea virus (BV...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/s0166-3542(02)00075-x

    authors: Ouzounov S,Mehta A,Dwek RA,Block TM,Jordan R

    更新日期:2002-09-01 00:00:00

  • The relationship between the antiviral activity of 5'-amino-5'-deoxythymidine and its incorporation into herpes simplex virus type 1 DNA.

    abstract::As part of our studies on the molecular basis for the antiherpes activity of 5'-AdThd (5'-amino-5'-deoxythymidine), a study of the HSV-1 DNA synthesized in infected Vero cells exposed to 5'-AdThd was undertaken. Unlike many other antiviral nucleoside analogs, 5'-AdThd did not inhibit HSV-1 DNA synthesis. Analysis of t...

    journal_title:Antiviral research

    pub_type: 杂志文章

    doi:10.1016/0166-3542(84)90032-9

    authors: Otto MJ,Prusoff WH

    更新日期:1984-10-01 00:00:00