Links to pubs, patents, compounds

 

Pubs

HTS Assay

M. A. Parniak, K. L. Min, S. R. Budihas, S. F. J. Le Grice, and J. A. Beutler. A fluorescence-based high-throughput screening assay for inhibitors of HIV-1 reverse transcriptase associated ribonuclease H activity. Anal.Biochem. 322 (1):33-39, 2003. PubMed link

K. C. Chan, S. R. Budihas, S. F. J. Le Grice, M. A. Parniak, R. J. Crouch, S. A. Gaidamakov, H. J. Isaaq, A. Wamiru, J. B. McMahon, and J. A. Beutler. A capillary electrophoretic assay for ribonuclease H activity. Anal.Biochem. 331 (2):296-302, 2004. PubMed link

Vinylogous urea hits

M. Wendeler, H.-F. Lee, A. Bermingham, J. T. Miller, O. Chertov, M. K. Bona, N. S. Baichoo, M. Ehteshami, J. A. Beutler, B. R. O'Keefe, M. Götte, M. Kvaratskhelia, and S. F. J. Le Grice. Vinylogous ureas as a novel class of inhibitors of reverse transcriptase-associated ribonuclease H activity.  ACS Chem.Biol. 3 (10):635-644, 2008. PubMed link

S. Chung, M. Wendeler, J. W. Rausch, G. Beilhartz, M. Gotte, B. R. O'Keefe, A. Bermingham, J. A. Beutler, S. Liu, X. Zhuang, and S. F. J. Le Grice. Structure-activity analysis of vinylogous urea inhibitors of human immunodeficiency virus-encoded ribonuclease H. Antimicrob.Agents Chemother. 54 (9):3913-3921, 2010. PubMed link

S. Chung, J. T. Miller, B. C. Johnson, S. H. Hughes, and S. F. Le Grice. Mutagenesis of human immunodeficiency virus reverse transcriptase p51 subunit defines residues contributing to vinylogous urea inhibition of ribonuclease H activity. J.Biol.Chem. 287 (6):4066-4075, 2012. PubMed link

T. Masaoka, S. Chung, P. Carboni, J. A. Wilson, J. A. Beutler, G. Tocco, and S. F. J. Le Grice. Exploiting drug-resistant enzymes as tools to identify thienopyrimidinone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H. J.Med.Chem. 56:5436-5445, 2013. PubMed link

Tropolones

S. R. Budihas, I. I. Gorshkova, S. A. Gaidamakov, A. Wamiru, M. K. Bona, M. A. Parniak, R. C. Crouch, J. B. McMahon, J. A. Beutler, and S. F. J. Le Grice. Selective inhibition of HIV-1 reverse transcriptase-associated ribonuclease H activity by hydroxylated tropolones. Nucl.Acids Res. 33 (4):1249-1256, 2005. PubMed link

G. Beilhartz, D. Eggink, S. F. J. Le Grice, J. A. Beutler, and M. Götte. Exploring the mechanism of specific inhibition of the HIV-1 RNase H domain by beta-thujaplicinol.  Cold Spring Harbor Meeting on Retroviruses, 2006. (Abstract)

S. Chung, D. M. Himmel, J. K. Jiang, K. Wojtak, J. D. Baumann, J. W. Rausch, J. A. Wilson, J. A. Beutler, C. J. Thomas, E. Arnold, and S. F. J. Le Grice. Synthesis, activity, and structural analysis of novel a -hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H. J.Med.Chem. 54 (13):4462-4473, 2011. PubMed link

G. Lu, E. Lomonosova, X. Cheng, E. A. Moran, M. J. Meyers, S. F. J. Le Grice, C. J. Thomas, J. K. Jiang, C. Meck, D. R. Hirsch, M. P. D'Erasmo, D. M. Suyabatmaz, R. P. Murelli, and J. P. Tavis. Hydroxylated tropolones inhibit hepatitis B virus replication by blocking the viral ribonuclease H activity. Antimicrob.Agents Chemother. 59 (2):1070-1079, 2015. PubMed link

J. Ma, R. S. Pawar, E. Grundel, E. P. Mazzola, C. D. Ridge, T. Masaoka, S. F. J. Le Grice, J. A. Wilson, J. A. Beutler, and A. J. Krynitsky. Sesquiterpenoid tropolone glycosides from Liriosma ovata. J.Nat.Prod. 78 (2):315-319, 2015. PubMed link

Natural Product Isolation

N. T. Dat, K. H. Bae, A. Wamiru, J. B. McMahon, S. F. J. Le Grice, M. Bona, J. A. Beutler, and Y. H. Kim. A dimeric lactone from Ardisia japonica which inhibits HIV-1 and HIV-2 ribonuclease H. J.Nat.Prod. 70 (5):839-841, 2007. PubMed link

K. Takada, A. Bermingham, B. R. O'Keefe, A. Wamiru, J. A. Beutler, S. F. J. Le Grice, J. Lloyd, K. R. Gustafson, and J. B. McMahon. A new HIV RNase H inhibitory 1,3,4,5-tetragalloylapiitol from the African plant Hylodendron gabunensis. J.Nat.Prod. 70 (10):1647-1649, 2007. PubMed link

H. R. Bokesch, A. Wamiru, S. F. J. Le Grice, J. A. Beutler, T. C. McKee, and J. B. McMahon. New HIV-1 inhibitory ribonuclease H phenolic glycosides from Eugenia hiemalis. J.Nat.Prod. 71 (9):1634-1636, 2008. PubMed link

J. A. Kim, A. Wamiru, J. B. McMahon, S. F. J. Le Grice, J. A. Beutler, and Y. H. Kim. New monoterpene glycosides and phenolic compounds from Distylium racemosum, and their inhibitory activity against ribonuclease H. Bioorg.Med.Chem.Lett. 21 (10):2840-2844, 2011. PubMed link

Integrase vs. RNAse H Overlap

C. Marchand, J. A. Beutler, A. Wamiru, S. R. Budihas, U. Mollmann, L. Heinisch, J. W. Mellors, S. F. Le Grice, and Y. Pommier. Madurahydroxylactone derivatives as dual inhibitors of HIV-1 integrase and RNase H. Antimicrob.Agents Chemother. 52 (1):361-364, 2008. PubMed link

Reviews

M. Wendeler, G. L. Beilhartz, J. A. Beutler, M. Götte, and S. F. J. Le Grice. HIV ribonuclease H: Continuing the search for small molecule antagonists. HIV Therapy 3 (1):39-53, 2009.

A. Corona, T. Masaoka, G. Tocco, E. Tramontano, and S. F. Le Grice. Active site and allosteric inhibitors of the ribonuclease H activity of HIV reverse transcriptase. Future.Med.Chem. 5 (18):2127-2139, 2013. PubMed link

 

 

 

 

 

 

 
Last updated by Beutler, John (NIH/NCI) [E] on Mar 24, 2015