Literature DB >> 19939680

Small molecule inhibitors of HIV RT Ribonuclease H.

Martin Di Grandi1, Matthew Olson, Amar S Prashad, Geraldine Bebernitz, Amara Luckay, Stanley Mullen, Yongbo Hu, Girija Krishnamurthy, Keith Pitts, John O'Connell.   

Abstract

Two classes of compounds, thiocarbamates 1 and triazoles 2, have been identified as HIV RT RNase H inhibitors using a novel FRET-based HTS assay. The potent analogs in each series exhibited selectivity and were active in cell-based assays. In addition, saturable, 1:1 stoichiometric binding to target was established and time of addition studies were consistent with inhibition of RT-mediated HIV replication. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID： 19939680     DOI： 10.1016/j.bmcl.2009.10.043

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

1.  Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H.

Authors:  Suhman Chung; Daniel M Himmel; Jian-Kang Jiang; Krzysztof Wojtak; Joseph D Bauman; Jason W Rausch; Jennifer A Wilson; John A Beutler; Craig J Thomas; Eddy Arnold; Stuart F J Le Grice
Journal:  J Med Chem       Date:  2011-06-02       Impact factor: 7.446

2.  Identification of alternative binding sites for inhibitors of HIV-1 ribonuclease H through comparative analysis of virtual enrichment studies.

Authors:  Anthony K Felts; Krystal Labarge; Joseph D Bauman; Dishaben V Patel; Daniel M Himmel; Eddy Arnold; Michael A Parniak; Ronald M Levy
Journal:  J Chem Inf Model       Date:  2011-07-26       Impact factor: 4.956

3.  Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by Diketo acid derivatives.

Authors:  Angela Corona; Francesco Saverio Di Leva; Sylvain Thierry; Luca Pescatori; Giuliana Cuzzucoli Crucitti; Frederic Subra; Olivier Delelis; Francesca Esposito; Giuseppe Rigogliuso; Roberta Costi; Sandro Cosconati; Ettore Novellino; Roberto Di Santo; Enzo Tramontano
Journal:  Antimicrob Agents Chemother       Date:  2014-08-04       Impact factor: 5.191

Review 4.  Active site and allosteric inhibitors of the ribonuclease H activity of HIV reverse transcriptase.

Authors:  Angela Corona; Takashi Masaoka; Graziella Tocco; Enzo Tramontano; Stuart F J Le Grice
Journal:  Future Med Chem       Date:  2013-12       Impact factor: 3.808

5.  Structure-guided approach identifies a novel class of HIV-1 ribonuclease H inhibitors: binding mode insights through magnesium complexation and site-directed mutagenesis studies.

Authors:  Vasanthanathan Poongavanam; Angela Corona; Casper Steinmann; Luigi Scipione; Nicole Grandi; Fabiana Pandolfi; Roberto Di Santo; Roberta Costi; Francesca Esposito; Enzo Tramontano; Jacob Kongsted
Journal:  Medchemcomm       Date:  2018-02-01       Impact factor: 3.597

6.  A screening platform to monitor RNA processing and protein-RNA interactions in ribonuclease P uncovers a small molecule inhibitor.

Authors:  Ezequiel-Alejandro Madrigal-Carrillo; Carlos-Alejandro Díaz-Tufinio; Hugo-Aníbal Santamaría-Suárez; Marcelino Arciniega; Alfredo Torres-Larios
Journal:  Nucleic Acids Res       Date:  2019-07-09       Impact factor: 16.971

7.  Inhibitors of HIV-1 Reverse Transcriptase-Associated Ribonuclease H Activity.

Authors:  Tatiana Ilina; Krystal Labarge; Stefan G Sarafianos; Rieko Ishima; Michael A Parniak
Journal:  Biology (Basel)       Date:  2012-10-19

8.  The hepatitis B virus ribonuclease H is sensitive to inhibitors of the human immunodeficiency virus ribonuclease H and integrase enzymes.

Authors:  John E Tavis; Xiaohong Cheng; Yuan Hu; Michael Totten; Feng Cao; Eleftherios Michailidis; Rajeev Aurora; Marvin J Meyers; E Jon Jacobsen; Michael A Parniak; Stefan G Sarafianos
Journal:  PLoS Pathog       Date:  2013-01-22       Impact factor: 6.823

9.  Virtual screening models for prediction of HIV-1 RT associated RNase H inhibition.

Authors:  Vasanthanathan Poongavanam; Jacob Kongsted
Journal:  PLoS One       Date:  2013-09-16       Impact factor: 3.240
  9 in total

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