A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells.

Analysis of natural sequence variation and covariation in human immunodeficiency virus type 1 integrase. J Virol (2008) 1.27

Defining the DNA substrate binding sites on HIV-1 integrase. J Mol Biol (2008) 1.01

Raltegravir: first in class HIV integrase inhibitor. Ther Clin Risk Manag (2008) 0.87

Dihydroxythiophenes are novel potent inhibitors of human immunodeficiency virus integrase with a diketo acid-like pharmacophore. J Virol (2006) 0.84

Raltegravir in the management of HIV-infected patients. Drug Des Devel Ther (2009) 0.78

Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy. Infect Drug Resist (2010) 0.76

Replication-incompetent adenoviral vaccine vector elicits effective anti-immunodeficiency-virus immunity. Nature (2002) 12.49

Raltegravir with optimized background therapy for resistant HIV-1 infection. N Engl J Med (2008) 7.33

Genome-scale RNAi screen for host factors required for HIV replication. Cell Host Microbe (2008) 6.24

Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. N Engl J Med (2008) 5.58

Attenuation of simian immunodeficiency virus SIVmac239 infection by prophylactic immunization with dna and recombinant adenoviral vaccine vectors expressing Gag. J Virol (2005) 4.78

Host cell factors in HIV replication: meta-analysis of genome-wide studies. PLoS Pathog (2009) 4.24

Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes. Proc Natl Acad Sci U S A (2002) 3.40

Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. J Med Chem (2008) 3.09

Complete genome sequence of Yersinia pestis strain 91001, an isolate avirulent to humans. DNA Res (2004) 2.95

Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitro. J Biol Chem (2003) 2.82

A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase. Proc Natl Acad Sci U S A (2004) 2.55

Mamu-A*01 allele-mediated attenuation of disease progression in simian-human immunodeficiency virus infection. J Virol (2002) 2.44

A limited group of class I histone deacetylases acts to repress human immunodeficiency virus type 1 expression. J Virol (2009) 2.30

Expression of latent human immunodeficiency type 1 is induced by novel and selective histone deacetylase inhibitors. AIDS (2009) 2.28

Antiretroviral therapy with the integrase inhibitor raltegravir alters decay kinetics of HIV, significantly reducing the second phase. AIDS (2007) 2.27

c-Myc and Sp1 contribute to proviral latency by recruiting histone deacetylase 1 to the human immunodeficiency virus type 1 promoter. J Virol (2007) 2.24

HIV-1 antiretroviral drug therapy. Cold Spring Harb Perspect Med (2012) 2.18

Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques. Science (2004) 2.12

Genetics of metabolic variations between Yersinia pestis biovars and the proposal of a new biovar, microtus. J Bacteriol (2004) 2.04

Structure-based design of novel inhibitors of the MDM2-p53 interaction. J Med Chem (2012) 2.01

A 7-deaza-adenosine analog is a potent and selective inhibitor of hepatitis C virus replication with excellent pharmacokinetic properties. Antimicrob Agents Chemother (2004) 1.94

Isolation, structure, and absolute stereochemistry of platensimycin, a broad spectrum antibiotic discovered using an antisense differential sensitivity strategy. J Am Chem Soc (2006) 1.87

Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1). J Med Chem (2004) 1.87

MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. Antimicrob Agents Chemother (2009) 1.80

Inhibition of HIV-1 ribonuclease H by a novel diketo acid, 4-[5-(benzoylamino)thien-2-yl]-2,4-dioxobutanoic acid. J Biol Chem (2002) 1.80

PD-1 blockade in rhesus macaques: impact on chronic infection and prophylactic vaccination. J Immunol (2009) 1.77

Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. J Med Chem (2010) 1.76

A human monoclonal antibody neutralizes diverse HIV-1 isolates by binding a critical gp41 epitope. Proc Natl Acad Sci U S A (2005) 1.74

Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells. J Med Chem (2003) 1.55

DNA microarray analysis of genome dynamics in Yersinia pestis: insights into bacterial genome microevolution and niche adaptation. J Bacteriol (2004) 1.52

Vectored Gag and Env but not Tat show efficacy against simian-human immunodeficiency virus 89.6P challenge in Mamu-A*01-negative rhesus monkeys. J Virol (2005) 1.52

Cytotoxic T-lymphocyte escape does not always explain the transient control of simian immunodeficiency virus SIVmac239 viremia in adenovirus-boosted and DNA-primed Mamu-A*01-positive rhesus macaques. J Virol (2005) 1.50

MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants. Antimicrob Agents Chemother (2012) 1.48

Identification of novel mutations responsible for resistance to MK-2048, a second-generation HIV-1 integrase inhibitor. J Virol (2010) 1.46

The Spongistatins: Architecturally Complex Natural Products-Part One: A Formal Synthesis of (+)-Spongistatin 1 by Construction of an Advanced ABCD Fragment Financial support was provided by the National Institutes of Health (National Cancer Institute) through Grant CA-70329, NIH Postdoctoral Fellowships to A.M.B. and W.H.M., a Japan Society for Promotion of Science Fellowship to N.M., and a Royal Society Fulbright Fellowship to V.A.D. We also thank the Daiichi Pharmaceutical Co., Ltd, and the Tanabe Seiyaku Co., Ltd for financial support. Finally we thank Dr. George T. Furst, Dr. Patrick J. Carroll, Dr. Rakesh Kohli, and Mr John Dykins of the University of Pennsylvania Spectroscopic Service Center for assistance in securing and interpreting high-field NMR spectra, X-ray crystal structures, and mass spectra. Angew Chem Int Ed Engl (2001) 1.42

Ruthenium-catalyzed ring-closing metathesis to form tetrasubstituted olefins. Org Lett (2007) 1.39

A new class of potent matrix metalloproteinase 13 inhibitors for potential treatment of osteoarthritis: Evidence of histologic and clinical efficacy without musculoskeletal toxicity in rat models. Arthritis Rheum (2009) 1.38

Replication fitness and NS5B drug sensitivity of diverse hepatitis C virus isolates characterized by using a transient replication assay. Antimicrob Agents Chemother (2005) 1.38

Covalent stabilization of coiled coils of the HIV gp41 N region yields extremely potent and broad inhibitors of viral infection. Proc Natl Acad Sci U S A (2005) 1.36

Probiotic/prebiotic supplementation of antiretrovirals improves gastrointestinal immunity in SIV-infected macaques. J Clin Invest (2013) 1.35

The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2 Financial support was provided by the National Institutes of Health (National Cancer Institute) through Grant CA-70329, a NIH Postdoctoral Fellowship to C.S.B., a Japan Society for Promotion of Science Fellowship to N.M., and a Royal Society Fulbright Fellowship to V.A.D. We also thank the Daiichi Pharmaceutical Co., Ltd, and the Tanabe Seiyaku Co., Ltd for financial support. Finally we thank Dr George T. Furst, Dr. Patrick J. Carroll, and Dr. Rakesh Kohli of the University of Pennsylvania Spectroscopic Service Center for assistance in securing and interpreting high-field NMR spectra, X-ray crystal structures, and mass spectra, respectively. Angew Chem Int Ed Engl (2001) 1.33

Structural basis for the inhibition of RNase H activity of HIV-1 reverse transcriptase by RNase H active site-directed inhibitors. J Virol (2010) 1.32

Altering expression levels of human immunodeficiency virus type 1 gp120-gp41 affects efficiency but not kinetics of cell-cell fusion. J Virol (2002) 1.29

Dissecting the effects of DNA polymerase and ribonuclease H inhibitor combinations on HIV-1 reverse-transcriptase activities. Biochemistry (2005) 1.25

Effects of fibrates on metabolism of statins in human hepatocytes. Drug Metab Dispos (2002) 1.24

Combined approaches for HIV cure. Curr Opin HIV AIDS (2013) 1.23

Structure, stereochemistry, and biological activity of integramycin, a novel hexacyclic natural product produced by Actinoplanes sp. that inhibits HIV-1 integrase. Org Lett (2002) 1.23

Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor. J Med Chem (2010) 1.19

Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors. J Med Chem (2003) 1.18

First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates. J Pharmacol Exp Ther (2008) 1.16

Analysis of low-frequency mutations associated with drug resistance to raltegravir before antiretroviral treatment. Antimicrob Agents Chemother (2010) 1.16

Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine. J Pharmacol Exp Ther (2007) 1.15

Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group. Bioorg Med Chem Lett (2004) 1.15

Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974). J Med Chem (2007) 1.14

Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity. ChemMedChem (2013) 1.13

In vivo beta-secretase 1 inhibition leads to brain Abeta lowering and increased alpha-secretase processing of amyloid precursor protein without effect on neuregulin-1. J Pharmacol Exp Ther (2007) 1.13

Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother (2009) 1.13

Mechanistic studies on metabolic interactions between gemfibrozil and statins. J Pharmacol Exp Ther (2002) 1.13

Early depletion of proliferating B cells of germinal center in rapidly progressive simian immunodeficiency virus infection. Virology (2007) 1.12

Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease. J Am Chem Soc (2008) 1.11

HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro. J Biol Chem (2006) 1.10

A potent and orally active HIV-1 integrase inhibitor. Bioorg Med Chem Lett (2006) 1.10