Literature DB >> 19791799

RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information.

Thorsten A Kirschberg1, Mini Balakrishnan, Neil H Squires, Tiffany Barnes, Katherine M Brendza, Xiaowu Chen, Eugene J Eisenberg, Weili Jin, Nilima Kutty, Stephanie Leavitt, Albert Liclican, Qi Liu, Xiaohong Liu, John Mak, Jason K Perry, Michael Wang, William J Watkins, Eric B Lansdon.   

Abstract

Pyrimidinol carboxylic acids were designed as inhibitors of HIV-1 RNase H function. These molecules can coordinate to two divalent metal ions in the RNase H active site. Inhibition of enzymatic activity was measured in a biochemical assay, but no antiviral effect was observed. Binding was demonstrated via a solid state structure of the isolated p15-Ec domain of HIV-1 RT showing inhibitor and two Mn(II) ions bound to the RNase H active site.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19791799     DOI： 10.1021/jm900597q

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  46 in total

1.  Expression of an Mg2+-dependent HIV-1 RNase H construct for drug screening.

Authors:  Richard V Farias; Deborah A Vargas; Andres E Castillo; Beatriz Valenzuela; Marie L Coté; Monica J Roth; Oscar Leon
Journal:  Antimicrob Agents Chemother       Date:  2011-07-18       Impact factor: 5.191

2.  Inhibitors of nucleotidyltransferase superfamily enzymes suppress herpes simplex virus replication.

Authors:  John E Tavis; Hong Wang; Ann E Tollefson; Baoling Ying; Maria Korom; Xiaohong Cheng; Feng Cao; Katie L Davis; William S M Wold; Lynda A Morrison
Journal:  Antimicrob Agents Chemother       Date:  2014-09-29       Impact factor: 5.191

Review 3.  HIV-1 Reverse Transcriptase: A Metamorphic Protein with Three Stable States.

Authors:  Robert E London
Journal:  Structure       Date:  2019-01-10       Impact factor: 5.006

Review 4.  Targeting Metalloenzymes for Therapeutic Intervention.

Authors:  Allie Y Chen; Rebecca N Adamek; Benjamin L Dick; Cy V Credille; Christine N Morrison; Seth M Cohen
Journal:  Chem Rev       Date:  2018-09-07       Impact factor: 60.622

5.  Structure of a dihydroxycoumarin active-site inhibitor in complex with the RNase H domain of HIV-1 reverse transcriptase and structure-activity analysis of inhibitor analogs.

Authors:  Daniel M Himmel; Nataliya S Myshakina; Tatiana Ilina; Alexander Van Ry; William C Ho; Michael A Parniak; Eddy Arnold
Journal:  J Mol Biol       Date:  2014-05-17       Impact factor: 5.469

6.  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

7.  6-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.

Authors:  Lei Wang; Jing Tang; Andrew D Huber; Mary C Casey; Karen A Kirby; Daniel J Wilson; Jayakanth Kankanala; Jiashu Xie; Michael A Parniak; Stefan G Sarafianos; Zhengqiang Wang
Journal:  Eur J Med Chem       Date:  2018-07-17       Impact factor: 6.514

8.  6-Biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibited HIV reverse transcriptase-associated RNase H.

Authors:  Lei Wang; Jing Tang; Andrew D Huber; Mary C Casey; Karen A Kirby; Daniel J Wilson; Jayakanth Kankanala; Michael A Parniak; Stefan G Sarafianos; Zhengqiang Wang
Journal:  Eur J Med Chem       Date:  2018-07-17       Impact factor: 6.514

9.  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

10.  Structural basis of the allosteric inhibitor interaction on the HIV-1 reverse transcriptase RNase H domain.

Authors:  Martin T Christen; Lakshmi Menon; Nataliya S Myshakina; Jinwoo Ahn; Michael A Parniak; Rieko Ishima
Journal:  Chem Biol Drug Des       Date:  2012-08-31       Impact factor: 2.817
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.