ACYLATION;
ANTIVIRAL ACTIVITY;
ANTIVIRAL RESISTANCE;
ARTICLE;
CHEMICAL REACTION;
CONTROLLED STUDY;
CYCLIZATION;
CYCLOADDITION;
DEPROTONATION;
DRUG CYTOTOXICITY;
DRUG DESIGN;
DRUG EFFICACY;
DRUG POTENCY;
DRUG SCREENING;
DRUG SYNTHESIS;
HUMAN;
HUMAN CELL;
HUMAN IMMUNODEFICIENCY VIRUS 1;
IC 50;
NONHUMAN;
PRIORITY JOURNAL;
PUMMERER REACTION;
VIRUS MUTANT;
WILD TYPE;
AMINO ACID SUBSTITUTION;
BICYCLO COMPOUNDS;
BINDING SITES;
CELL LINE, TUMOR;
COMPUTER SIMULATION;
DRUG RESISTANCE, VIRAL;
HIV INTEGRASE;
HIV INTEGRASE INHIBITORS;
HIV-1;
HUMANS;
IMIDES;
MUTATION;
PYRIDINES;
PYRIDONES;
PYRROLIDINONES;
Interfacial inhibition of macromolecular interactions: nature's paradigm for drug discovery
Pommier Y., Cherfils J. (2005) Interfacial inhibition of macromolecular interactions: nature's paradigm for drug discovery. Trends Pharmacol Sci;26:138-145.
Raltegravir (mk-0518): a novel integrase inhibitor for the treatment of HIV infection
Anker M., Corales R.B. (2008) Raltegravir (mk-0518): a novel integrase inhibitor for the treatment of HIV infection. Expert Opin Investig Drugs;17:97-103.
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection
Summa V., Petrocchi A., Bonelli F., Crescenzi B., Donghi M., Ferrara M., Fiore F. et al. (2008) Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. J Med Chem;51:5843-5855.
Retroviral intasome assembly and inhibition of DNA strand transfer
Hare S., Gupta S.S., Valkov E., Engelman A., Cherepanov P. (2010) Retroviral intasome assembly and inhibition of DNA strand transfer. Nature;464:232-236.
Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants
Marinello J., Marchand C., Mott B.T., Bain A., Thomas C.J., Pommier Y. (2008) Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants. Biochemistry;47:9345-9354.
Loss of raltegravir susceptibility by human immunodeficiency virus type 1 is conferred via multiple nonoverlapping genetic pathways
Fransen S., Gupta S., Danovich R., Hazuda D., Miller M., Witmer M., Petropoulos C.J., Huang W. (2009) Loss of raltegravir susceptibility by human immunodeficiency virus type 1 is conferred via multiple nonoverlapping genetic pathways. J Virol;83:11440-11446.
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors
Muraglia E., Kinzel O., Gardelli C., Crescenzi B., Donghi M., Ferrara M., Nizi E. et al. (2008) Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors. J Med Chem;51:861-874.
Elvitegravir overcomes resistance to raltegravir induced by integrase mutation Y143
Metifiot M., Vandegraaff N., Maddali K., Naumova A., Zhang X., Rhodes D., Marchand C., Pommier Y. (2011) Elvitegravir overcomes resistance to raltegravir induced by integrase mutation Y143. AIDS;25:1175-1178.
Examination of halogen substituent effects on HIV-1 integrase inhibitors derived from 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-ones and 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones
Zhao X.Z., Maddali K., Vu B.C., Marchand C., Hughes Stephen H., Pommier Y., Burke Terrence R. Jr (2009) Examination of halogen substituent effects on HIV-1 integrase inhibitors derived from 2, 3-dihydro-6, 7-dihydroxy-1H-isoindol-1-ones and 4, 5-dihydroxy-1H-isoindole-1, 3(2H)-diones. Bioorg Med Chem Lett;19:2714-2717.
Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors
Zhao X.Z., Maddali K., Metifiot M., Smith S.J., Christie Vu B., Marchand C., Hughes S.H., Pommier Y., Burke T.R. (2011) Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors. Bioorg Med Chem Lett;21:2986-2990.
Synthesis of substituted 2-pyridones via the Pummerer cyclization' deprotonation' cycloaddition cascade of imidosulfoxides
Padwa A., Heidelbaugh T.M., Kuethe J.T. (1999) Synthesis of substituted 2-pyridones via the Pummerer cyclization' deprotonation' cycloaddition cascade of imidosulfoxides. J Org Chem;64:2038-2049.
Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture
Zouhiri F., Mouscadet J.-F., Mekouar K., Desmaele D., Savourr D., Leh H., Subra F., Le Bret M., Auclair C., d'Angelo J. (2000) Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture. J Med Chem;43:1533-1540.
Using the Pummerer cyclization' deprotonation' cycloaddition cascade of imidosulfoxides for alkaloid synthesis
Padwa A., Heidelbaugh T.M., Kuethe J.T. (2000) Using the Pummerer cyclization' deprotonation' cycloaddition cascade of imidosulfoxides for alkaloid synthesis. J Org Chem;65:2368-2378.
Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance
Hare S., Vos A.M., Clayton R.F., Thuring J.W., Cummings M.D., Cherepanov P. (2010) Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci USA;107:20057-20062.
A dynamic model of HIV integrase inhibition and drug resistance
Perryman A.L., Forli S., Morris G.M., Burt C., Cheng Y., Palmer M.J., Whitby K., McCammon J.A., Phillips C., Olson A.J. (2010) A dynamic model of HIV integrase inhibition and drug resistance. J Mol Biol;397:600-615.
Mechanism by which the HIV integrase active-site mutation N155H confers resistance to raltegravir
Grobler J.A., Stillmock K.A., Miller M.D., Hazuda D.J. (2008) Mechanism by which the HIV integrase active-site mutation N155H confers resistance to raltegravir. Antivir Ther;13:A41.