Basic Quinolinonyl Diketo Acid Derivatives as Inhibitors of HIV Integrase and their Activity against RNase H Function of Reverse Transcriptase
暂无分享,去创建一个
Y. Pommier | E. Novellino | S. L. Le Grice | R. Di Santo | R. Costi | M. Métifiot | L. Marinelli | F. S. Di Leva | S. Cosconati | C. Marchand | L. Scipione | S. Tortorella | A. Corona | Suhman Chung | V. N. Madia | A. Messore | L. Pescatori | Kasthuraiah Maddali | Giovanni Pupo | Giuliana Cuzzucoli Crucitti
[1] Olan Dolezal,et al. Parallel Screening of Low Molecular Weight Fragment Libraries , 2013, Journal of biomolecular screening.
[2] Y. Pommier,et al. Activities, crystal structures, and molecular dynamics of dihydro-1H-isoindole derivatives, inhibitors of HIV-1 integrase. , 2013, ACS chemical biology.
[3] Wei Yang,et al. Complexes of HIV-1 RT, NNRTI and RNA/DNA hybrid reveal a structure compatible with RNA degradation , 2013, Nature Structural &Molecular Biology.
[4] Thomas S. Peat,et al. Small Molecule Inhibitors of the LEDGF Site of Human Immunodeficiency Virus Integrase Identified by Fragment Screening and Structure Based Design , 2012, PloS one.
[5] J. Newman,et al. Crystal Structures of Novel Allosteric Peptide Inhibitors of HIV Integrase Identify New Interactions at the LEDGF Binding Site , 2011, Chembiochem : a European journal of chemical biology.
[6] Yves Pommier,et al. Structural and Functional Analyses of the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir (S/GSK1349572) , 2011, Molecular Pharmacology.
[7] S. Piscitelli,et al. Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of dolutegravir as 10-day monotherapy in HIV-1-infected adults , 2011, AIDS.
[8] R. D. Santo. Diketo Acids Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and the Reverse Transcriptase RNase H Domain , 2011 .
[9] E. Arnold,et al. Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H. , 2011, Journal of medicinal chemistry.
[10] Xiaohong Liu,et al. Structural and Binding Analysis of Pyrimidinol Carboxylic Acid and N-Hydroxy Quinazolinedione HIV-1 RNase H Inhibitors , 2011, Antimicrobial Agents and Chemotherapy.
[11] J. Newman,et al. Structural Basis for a New Mechanism of Inhibition of H I V-1 Integrase Identified by Fragment Screening and Structure-Based Design , 2011, Antiviral chemistry & chemotherapy.
[12] F. Bailly,et al. Magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function. , 2011, Journal of medicinal chemistry.
[13] M. Parker,et al. Fragment‐Based Design of Ligands Targeting a Novel Site on the Integrase Enzyme of Human Immunodeficiency Virus 1 , 2011, ChemMedChem.
[14] Maxwell D. Cummings,et al. Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance , 2010, Proceedings of the National Academy of Sciences.
[15] Goedele N. Maertens,et al. The mechanism of retroviral integration through X-ray structures of its key intermediates , 2010, Nature.
[16] X. Zhuang,et al. Structure-Activity Analysis of Vinylogous Urea Inhibitors of Human Immunodeficiency Virus-Encoded Ribonuclease H , 2010, Antimicrobial Agents and Chemotherapy.
[17] Y. Pommier,et al. Scaffold rearrangement of dihydroxypyrimidine inhibitors of HIV integrase: Docking model revisited. , 2010, Bioorganic & medicinal chemistry letters.
[18] A. Marchand,et al. Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication. , 2010, Nature chemical biology.
[19] Christopher L. Daniels,et al. Structural Basis for the Inhibition of RNase H Activity of HIV-1 Reverse Transcriptase by RNase H Active Site-Directed Inhibitors , 2010, Journal of Virology.
[20] M. Parker,et al. Crystal structure of the HIV‐1 integrase core domain in complex with sucrose reveals details of an allosteric inhibitory binding site , 2010, FEBS letters.
[21] A. Engelman,et al. Retroviral intasome assembly and inhibition of DNA strand transfer , 2010, Nature.
[22] A. D. Clark,et al. Structure of HIV-1 reverse transcriptase with the inhibitor beta-Thujaplicinol bound at the RNase H active site. , 2009, Structure.
[23] C. Van Lint,et al. Structural and theoretical studies of [6-bromo-1-(4-fluorophenylmethyl)-4(1H)-quinolinon-3-yl)]-4-hydroxy-2-oxo-3-butenoïc acid as HIV-1 integrase inhibitor. , 2009, Bioorganic & medicinal chemistry letters.
[24] Yves Pommier,et al. Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants. , 2008, Biochemistry.
[25] Y. Pommier,et al. Novel Quinolinonyl Diketo Acid Derivatives as HIV-1 Integrase Inhibitors: Design, Synthesis, and Biological Activities , 2008, Journal of medicinal chemistry.
[26] Zhengqiang Wang,et al. Design and synthesis of dual inhibitors of HIV reverse transcriptase and integrase: introducing a diketoacid functionality into delavirdine. , 2008, Bioorganic & medicinal chemistry.
[27] Zhengqiang Wang,et al. Synthesis of pyrimidine and quinolone conjugates as a scaffold for dual inhibitors of HIV reverse transcriptase and integrase. , 2008, Bioorganic & medicinal chemistry letters.
[28] Nouri Neamati,et al. HIV‐1 integrase inhibitors: 2005–2006 update , 2008, Medicinal research reviews.
[29] Y. Pommier,et al. Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H , 2007, Antimicrobial Agents and Chemotherapy.
[30] P. Bellecave,et al. Cellular uptake of ODNs in HIV-1 human-infected cells: a role for viral particles in DNA delivery? , 2007, Oligonucleotides.
[31] C. Salomon,et al. Rationally designed dual inhibitors of HIV reverse transcriptase and integrase. , 2007, Journal of medicinal chemistry.
[32] B. Conway,et al. The Role of Adherence to Antiretroviral Therapy in the Management of HIV Infection , 2007, Journal of acquired immune deficiency syndromes.
[33] C. Katlama,et al. Safety and efficacy of the HIV-1 integrase inhibitor raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: a phase II randomised controlled trial , 2007, The Lancet.
[34] C. Kovacs,et al. Antiretroviral Activity, Pharmacokinetics, and Tolerability of MK-0518, a Novel Inhibitor of HIV-1 Integrase, Dosed As Monotherapy for 10 Days in Treatment-Naive HIV-1-Infected Individuals , 2006, Journal of acquired immune deficiency syndromes.
[35] B. Clotet,et al. Benefits and concerns of simplification strategies in HIV-infected patients. , 2006, The Journal of antimicrobial chemotherapy.
[36] Mahindra T. Makhija. Designing HIV integrase inhibitors--shooting the last arrow. , 2006, Current medicinal chemistry.
[37] M. Kozal,et al. The hunt for HIV-1 integrase inhibitors. , 2006, AIDS patient care and STDs.
[38] R. Dayam,et al. HIV‐1 integrase inhibitors: 2003–2004 update , 2006 .
[39] Y. Pommier,et al. Preferential Inhibition of the Magnesium-Dependent Strand Transfer Reaction of HIV-1 Integrase by α-Hydroxytropolones , 2006, Molecular Pharmacology.
[40] Y. Pommier,et al. Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities, and mechanism of action. , 2006, Journal of medicinal chemistry.
[41] C. Isel,et al. Inhibition of Human Immunodeficiency Virus Type 1 Reverse Transcriptase, RNase H, and Integrase Activities by Hydroxytropolones , 2005, Antimicrobial Agents and Chemotherapy.
[42] A. Engelman,et al. Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p75. , 2005, Proceedings of the National Academy of Sciences of the United States of America.
[43] Wei Yang,et al. Crystal Structures of RNase H Bound to an RNA/DNA Hybrid: Substrate Specificity and Metal-Dependent Catalysis , 2005, Cell.
[44] Y. Pommier,et al. Integrase inhibitors to treat HIV/Aids , 2005, Nature Reviews Drug Discovery.
[45] S. L. Le Grice,et al. Selective inhibition of HIV-1 reverse transcriptase-associated ribonuclease H activity by hydroxylated tropolones , 2005, Nucleic acids research.
[46] R. Di Santo,et al. 6-[1-(4-Fluorophenyl)methyl-1H-pyrrol-2-yl)]-2,4-dioxo-5-hexenoic acid ethyl ester a novel diketo acid derivative which selectively inhibits the HIV-1 viral replication in cell culture and the ribonuclease H activity in vitro. , 2005, Antiviral research.
[47] Conrad C. Huang,et al. UCSF Chimera—A visualization system for exploratory research and analysis , 2004, J. Comput. Chem..
[48] F. Bailly,et al. Spectroscopic studies of diketoacids-metal interactions. A probing tool for the pharmacophoric intermetallic distance in the HIV-1 integrase active site. , 2004, Journal of medicinal chemistry.
[49] Y. Pommier,et al. HIV-1 integrase inhibitors: a decade of research and two drugs in clinical trial. , 2004, Current topics in medicinal chemistry.
[50] F. Bailly,et al. Structure-activity relationships of HIV-1 integrase inhibitors--enzyme-ligand interactions. , 2003, Current medicinal chemistry.
[51] M. Chesney,et al. Adherence to HAART regimens. , 2003, AIDS patient care and STDs.
[52] D. Hazuda,et al. Inhibition of HIV-1 Ribonuclease H by a Novel Diketo Acid, 4-[5-(Benzoylamino)thien-2-yl]-2,4-dioxobutanoic Acid* , 2003, The Journal of Biological Chemistry.
[53] R. Altmeyer,et al. DNA aptamers derived from HIV-1 RNase H inhibitors are strong anti-integrase agents. , 2002, Journal of molecular biology.
[54] J. Gallant,et al. Simplification of antiretroviral treatment--how to sustain success, reduce toxicity and ensure adherence avoiding PI use. , 2002, AIDS reviews.
[55] Wei Yang,et al. Structure of a two‐domain fragment of HIV‐1 integrase: implications for domain organization in the intact protein , 2001, The EMBO journal.
[56] F. Bushman,et al. Identification of a small-molecule binding site at the dimer interface of the HIV integrase catalytic domain. , 2001, Acta crystallographica. Section D, Biological crystallography.
[57] R M Stroud,et al. Crystal structure of the HIV-1 integrase catalytic core and C-terminal domains: a model for viral DNA binding. , 2000, Proceedings of the National Academy of Sciences of the United States of America.
[58] G. Cohen,et al. Structure of the HIV-1 integrase catalytic domain complexed with an inhibitor: a platform for antiviral drug design. , 1999, Proceedings of the National Academy of Sciences of the United States of America.
[59] T. Chun,et al. Latent reservoirs of HIV: obstacles to the eradication of virus. , 1999, Proceedings of the National Academy of Sciences of the United States of America.
[60] F. Bushman,et al. The mobility of an HIV-1 integrase active site loop is correlated with catalytic activity. , 1999, Biochemistry.
[61] G L Verdine,et al. Structure of a covalently trapped catalytic complex of HIV-1 reverse transcriptase: implications for drug resistance. , 1998, Science.
[62] V. Mikol,et al. Crystal structures of the catalytic domain of HIV-1 integrase free and complexed with its metal cofactor: high level of similarity of the active site with other viral integrases. , 1998, Journal of molecular biology.
[63] D. Davies,et al. Three new structures of the core domain of HIV-1 integrase: an active site that binds magnesium. , 1998, Proceedings of the National Academy of Sciences of the United States of America.
[64] W. L. Jorgensen,et al. Development and Testing of the OPLS All-Atom Force Field on Conformational Energetics and Properties of Organic Liquids , 1996 .
[65] S. Sarafianos,et al. Biochemical analysis of catalytically crucial aspartate mutants of human immunodeficiency virus type 1 reverse transcriptase. , 1996, Biochemistry.
[66] A. D. Clark,et al. Insights into DNA polymerization mechanisms from structure and function analysis of HIV-1 reverse transcriptase. , 1995, Biochemistry.
[67] A. Engelman,et al. Crystal structure of the catalytic domain of HIV-1 integrase: similarity to other polynucleotidyl transferases. , 1994, Science.
[68] A. D. Clark,et al. Crystal structure of human immunodeficiency virus type 1 reverse transcriptase complexed with double-stranded DNA at 3.0 A resolution shows bent DNA. , 1993, Proceedings of the National Academy of Sciences of the United States of America.
[69] Y. Pommier,et al. Structural and Functional Analyses of the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir (S/GSK1349572) , 2011, Molecular Pharmacology.
[70] R. Di Santo. Diketo acids derivatives as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain. , 2011, Current medicinal chemistry.
[71] Yves Pommier,et al. Structural and Functional Analyses of the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir , 2011 .
[72] P. Yeni. Update on HAART in HIV. , 2006, Journal of hepatology.
[73] Philippe Cotelle,et al. Patented HIV-1 integrase inhibitors (1998-2005). , 2006, Recent patents on anti-infective drug discovery.
[74] A. Engelman,et al. Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p 75 , 2005 .