PMID: 9449274Feb 4, 1998Paper

Dicaffeoylquinic and dicaffeoyltartaric acids are selective inhibitors of human immunodeficiency virus type 1 integrase

Antimicrobial Agents and Chemotherapy
B R McDougallW Edward Robinson

Abstract

Current pharmacological agents for human immunodeficiency virus (HIV) infection include drugs targeted against HIV reverse transcriptase and HIV protease. An understudied therapeutic target is HIV integrase, an essential enzyme that mediates integration of the HIV genome into the host chromosome. The dicaffeoylquinic acids (DCQAs) and the dicaffeoyltartaric acids (DCTAs) have potent activity against HIV integrase in vitro and prevent HIV replication in tissue culture. However, their specificity against HIV integrase in cell culture has been questioned. Thus, the ability of the DCQAs and DCTAs to inhibit binding of HIV type 1 (HIV-1) gp120 to CD4 and their activities against HIV-1 reverse transcriptase and HIV RNase H were studied. The DCQAs and DCTAs inhibited HIV-1 integrase at concentrations between 150 and 840 nM. They inhibited HIV replication at concentrations between 2 and 12 microM. Their activity against reverse transcriptase ranged from 7 microM to greater than 100 microM. Concentrations that inhibited gp120 binding to CD4 exceeded 80 microM. None of the compounds blocked HIV-1 RNase H by 50% at concentrations exceeding 80 microM. Furthermore, when the effects of the DCTAs on reverse transcription in acutely infected c...Continue Reading

References

Oct 30, 1992·Biochemical and Biophysical Research Communications·R I Brinkworth, D P Fairlie
Jun 1, 1992·AIDS Research and Human Retroviruses·D D Richman
May 29, 1992·Biochemical and Biophysical Research Communications·M Cushman, P Sherman
Feb 15, 1991·Proceedings of the National Academy of Sciences of the United States of America·Z HostomskyB R Nodes
Apr 15, 1991·Biochemical and Biophysical Research Communications·R I BrinkworthD P Fairlie
Jan 24, 1985·Nature·L RatnerK Baumeister
Dec 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·B J PoieszR C Gallo
Jul 1, 1993·Proceedings of the National Academy of Sciences of the United States of America·J L MartinP A Furman
Feb 1, 1995·Antimicrobial Agents and Chemotherapy·R L LaFeminaD J Hazuda
Apr 18, 1995·Biochemical Pharmacology·A MazumderY Pommier
Aug 1, 1994·Current Opinion in Biotechnology·R Swanstrom
Mar 1, 1995·Nature Structural Biology·E T BaldwinJ W Erickson
Feb 3, 1995·Journal of Medicinal Chemistry·M CushmanW G Rice
Aug 15, 1993·Proceedings of the National Academy of Sciences of the United States of America·M J OttoY S Cheng
Sep 1, 1993·Archives of Biochemistry and Biophysics·S CarteauC Auclair
May 14, 1993·Biochemical and Biophysical Research Communications·S CarteauC Auclair
Mar 15, 1993·Proceedings of the National Academy of Sciences of the United States of America·M R FesenY Pommier
Jun 25, 1996·Proceedings of the National Academy of Sciences of the United States of America·W E RobinsonS A Chow
Sep 3, 1996·Proceedings of the National Academy of Sciences of the United States of America·C M FarnetF D Bushman
Jan 17, 1997·Journal of Medicinal Chemistry·H ZhaoT R Burke
Mar 14, 1997·Journal of Medicinal Chemistry·M C NicklausY Pommier
Mar 14, 1997·Journal of Medicinal Chemistry·H HongG W Milne
Mar 14, 1997·Journal of Medicinal Chemistry·H ZhaoT R Burke
Apr 11, 1997·Journal of Medicinal Chemistry·H ZhaoT R Burke

❮ Previous
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Citations

Aug 27, 1998·Pharmazie in unserer Zeit·R Bauer
Jun 2, 2009·Antiviral Chemistry & Chemotherapy·Hans-Jürgen Stellbrink
Jun 16, 2012·Evidence-based Complementary and Alternative Medicine : ECAM·Yi-Hang WuLan-Juan Li
Aug 17, 2016·Evidence-based Complementary and Alternative Medicine : ECAM·Nadia TabassumDarren R Williams
Mar 22, 2019·Journal of Medicinal Food·Ye PengYeonhwa Park
Oct 9, 2002·Medicinal Research Reviews·Erik De Clercq
Mar 28, 2009·TAG. Theoretical and applied genetics. Theoretische und angewandte Genetik·Alberto AcquadroEzio Portis
Apr 23, 2009·Natural Product Research·Xian-Feng ZhuRamond Lo
Apr 5, 2012·Evidence-based Complementary and Alternative Medicine : ECAM·Chengwu SongNianbai Fang
Aug 28, 2015·Plant Foods for Human Nutrition·Maryem Ben SalemKhaled Mounir Zeghal
Dec 24, 2015·Virology Journal·Paula Rodrigues ZanelloJuliano Bordignon
Mar 5, 2019·Metabolomics : Official Journal of the Metabolomic Society·Gerhard Prinsloo, Jacques Vervoort
Jan 1, 2016·Journal of Pharmaceutical Investigation·Tran Dang Xuan, Tran Dang Khanh
May 19, 2000·Antimicrobial Agents and Chemotherapy·R B TurnerJ D Gangemi
Jan 24, 2003·Expert Opinion on Therapeutic Targets·Khampoune SayasithJocelyn Yelle
Apr 7, 2006·Molecular Nutrition & Food Research·Hirotoshi TamuraW Edward Robinson
Aug 27, 2013·Applied Biochemistry and Biotechnology·Janusz MalarzWanda Kisiel
Jun 9, 2012·Organic & Biomolecular Chemistry·Rakesh JaiswalNikolai Kuhnert
Jun 18, 2017·Bioscience, Biotechnology, and Biochemistry·Takashi ShionoAruto Yoshida
Apr 2, 2005·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Bo YangGuifang Dou
Sep 19, 2018·International Journal of Molecular Medicine·Nuramina MamatHaji Akber Aisa
Feb 17, 2001·European Journal of Biochemistry·J SnáselI Pichová
Aug 14, 2012·Blood Coagulation & Fibrinolysis : an International Journal in Haemostasis and Thrombosis·Hyun-Jeong ChoHwa-Jin Park
Jul 30, 2011·TAG. Theoretical and applied genetics. Theoretische und angewandte Genetik·Gabriella SonnanteDomenico Pignone

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