Published in Bioorg Med Chem on June 12, 2003
Molecular targets for flavivirus drug discovery. Antiviral Res (2008) 2.32
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Carboxylic acid isosteres improve the activity of ring-fused 2-pyridones that inhibit pilus biogenesis in E. coli. Bioorg Med Chem Lett (2008) 0.87
Three-component synthesis of C2F5-substituted pyrazoles from C2F5CH2NH2·HCl, NaNO2 and electron-deficient alkynes. Beilstein J Org Chem (2015) 0.81
Synthesis of 2-oxoamides based on sulfonamide analogs of gamma-amino acids and their activity on phospholipase A2. J Pept Sci (2008) 0.81
The structure of an infectious P22 virion shows the signal for headful DNA packaging. Science (2006) 3.33
Induction of myeloid-derived suppressor cells by tumor exosomes. Int J Cancer (2009) 2.64
Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist. J Med Chem (2004) 1.74
Angiotensin II type 2 receptor stimulation: a novel option of therapeutic interference with the renin-angiotensin system in myocardial infarction? Circulation (2008) 1.72
Microwave-accelerated homogeneous catalysis in organic chemistry. Acc Chem Res (2002) 1.58
In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor. Antimicrob Agents Chemother (2009) 1.50
Direct angiotensin II type 2 receptor stimulation acts anti-inflammatory through epoxyeicosatrienoic acid and inhibition of nuclear factor kappaB. Hypertension (2010) 1.50
Adipose tissue exosome-like vesicles mediate activation of macrophage-induced insulin resistance. Diabetes (2009) 1.42
The functional network of the Arabidopsis plastoglobule proteome based on quantitative proteomics and genome-wide coexpression analysis. Plant Physiol (2012) 1.23
Induced-fit binding of the macrocyclic noncovalent inhibitor TMC435 to its HCV NS3/NS4A protease target. Angew Chem Int Ed Engl (2010) 1.19
Stimulation of AT2 receptor exerts beneficial effects in stroke-prone rats: focus on renal damage. J Hypertens (2009) 1.18
Structural and functional analysis of hepatitis C virus strain JFH1 polymerase. J Virol (2009) 1.17
Non-peptide AT2-receptor agonists. Curr Opin Pharmacol (2010) 1.15
The IncRNAs PCGEM1 and PRNCR1 are not implicated in castration resistant prostate cancer. Oncotarget (2014) 1.14
Plasmepsins as potential targets for new antimalarial therapy. Med Res Rev (2006) 1.11
Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350. Bioorg Med Chem Lett (2008) 1.06
Discovery and development of simeprevir (TMC435), a HCV NS3/4A protease inhibitor. J Med Chem (2014) 1.05
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. J Med Chem (2009) 1.01
A new highly asymmetric chelation-controlled heck arylation. J Am Chem Soc (2003) 0.99
Formamide as a combined ammonia synthon and carbon monoxide source in fast palladium-catalyzed aminocarbonylations of aryl halides. J Comb Chem (2003) 0.99
Cathepsin K inhibitors prevent matrix-derived growth factor degradation by human osteoclasts. Bone (2007) 0.97
Structural basis of ligand recognition in 5-HT3 receptors. EMBO Rep (2012) 0.96
Short pseudopeptides containing turn scaffolds with high AT2 receptor affinity. Bioorg Med Chem (2006) 0.95
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors. J Med Chem (2002) 0.95
Incorporation of scaffolding protein gpO in bacteriophages P2 and P4. Virology (2007) 0.94
Loss of plastoglobule kinases ABC1K1 and ABC1K3 causes conditional degreening, modified prenyl-lipids, and recruitment of the jasmonic acid pathway. Plant Cell (2013) 0.94
AT2-receptor stimulation enhances axonal plasticity after spinal cord injury by upregulating BDNF expression. Neurobiol Dis (2012) 0.93
Synthesis, biological evaluation, and modeling studies of inhibitors aimed at the malarial proteases plasmepsins I and II. Bioorg Med Chem (2005) 0.92
A selective AT2 receptor ligand with a gamma-turn-like mimetic replacing the amino acid residues 4-5 of angiotensin II. J Med Chem (2004) 0.92
Effects on protease inhibition by modifying of helicase residues in hepatitis C virus nonstructural protein 3. FEBS J (2007) 0.92
Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors. Eur J Biochem (2003) 0.91
Synthesis of a new class of druglike angiotensin II C-terminal mimics with affinity for the AT2 receptor. J Med Chem (2007) 0.91
Kinetic and thermodynamic characterization of HIV-1 protease inhibitors. J Mol Recognit (2004) 0.91
Hydrogen bonding descriptors in the prediction of human in vivo intestinal permeability. J Mol Graph Model (2003) 0.90
Dimethylformamide as a carbon monoxide source in fast palladium-catalyzed aminocarbonylations of aryl bromides. J Org Chem (2002) 0.90
Biosensor-based kinetic characterization of the interaction between HIV-1 reverse transcriptase and non-nucleoside inhibitors. J Med Chem (2006) 0.90
Identification of a novel scaffold for allosteric inhibition of wild type and drug resistant HIV-1 reverse transcriptase by fragment library screening. J Med Chem (2011) 0.89
Characterization of Ca2+ and phosphocholine interactions with C-reactive protein using a surface plasmon resonance biosensor. Anal Biochem (2009) 0.89
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic. J Med Chem (2008) 0.88
Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core. Eur J Med Chem (2009) 0.86
Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes. J Med Chem (2003) 0.86
Identification of MMP-12 inhibitors by using biosensor-based screening of a fragment library. J Med Chem (2008) 0.86
Interaction kinetic characterization of HIV-1 reverse transcriptase non-nucleoside inhibitor resistance. J Med Chem (2006) 0.86
Probing conserved helical modules of portal complexes by mass spectrometry-based hydrogen/deuterium exchange. J Mol Biol (2008) 0.86
Discovery of dipeptides with high affinity to the specific binding site for substance P1-7. J Med Chem (2010) 0.86
Intramolecular Enantioselective Palladium-Catalyzed Heck Arylation of Cyclic Enamides. J Org Chem (1997) 0.85
Resistance profiling of hepatitis C virus protease inhibitors using full-length NS3. Antivir Ther (2007) 0.85
Design and synthesis of potent and selective BACE-1 inhibitors. J Med Chem (2010) 0.85
Macrocyclic inhibitors of the malarial aspartic proteases plasmepsin I, II, and IV. Bioorg Med Chem (2005) 0.85
Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues. Bioorg Med Chem (2008) 0.85
Resolving the distribution-metabolism interplay of eight OATP substrates in the standard clearance assay with suspended human cryopreserved hepatocytes. Mol Pharm (2013) 0.85
Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships. Bioorg Med Chem (2008) 0.84
Comparative functional properties of two structurally similar selective nonpeptide drug-like ligands for the angiotensin II type-2 (AT(2)) receptor. Effects on neurite outgrowth in NG108-15 cells. Eur J Pharmacol (2012) 0.84
Design and synthesis of potent inhibitors of plasmepsin I and II: X-ray crystal structure of inhibitor in complex with plasmepsin II. J Med Chem (2005) 0.84
Disulfide cyclized tripeptide analogues of angiotensin IV as potent and selective inhibitors of insulin-regulated aminopeptidase (IRAP). J Med Chem (2010) 0.84
On the active site protonation state in aspartic proteases: implications for drug design. Curr Pharm Des (2013) 0.84
Angiotensin II type 2 receptor promotes adipocyte differentiation and restores adipocyte size in high-fat/high-fructose diet-induced insulin resistance in rats. Am J Physiol Endocrinol Metab (2012) 0.83
Deconstruction of non-nucleoside reverse transcriptase inhibitors of human immunodeficiency virus type 1 for exploration of the optimization landscape of fragments. J Med Chem (2011) 0.83
Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors. Bioorg Med Chem Lett (2008) 0.83
Selective terminal heck arylation of vinyl ethers with aryl chlorides: a combined experimental-computational approach including synthesis of betaxolol. J Org Chem (2006) 0.83
Elucidation of HIV-1 protease resistance by characterization of interaction kinetics between inhibitors and enzyme variants. Antiviral Res (2003) 0.83
A new regioselective Heck vinylation with enamides. Synthesis and investigation of fluorous-tagged bidentate ligands for fast separation. J Org Chem (2003) 0.83
Effect of the protonation state of the titratable residues on the inhibitor affinity to BACE-1. Biochemistry (2010) 0.83
In silico prediction of unbound brain-to-plasma concentration ratio using machine learning algorithms. J Mol Graph Model (2011) 0.82
Quantification of interactions between drug leads and serum proteins by use of "binding efficiency". Anal Biochem (2010) 0.82
Modified Clp protease complex in the ClpP3 null mutant and consequences for chloroplast development and function in Arabidopsis. Plant Physiol (2013) 0.82
Resolution of the interaction mechanisms and characteristics of non-nucleoside inhibitors of hepatitis C virus polymerase. Antiviral Res (2013) 0.82
First reported nonpeptide AT1 receptor agonist (L-162,313) acts as an AT2 receptor agonist in vivo. J Med Chem (2004) 0.82
Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein. Biochemistry (2010) 0.82
In vitro and in vivo evaluation of a (18)F-labeled high affinity NOTA conjugated bombesin antagonist as a PET ligand for GRPR-targeted tumor imaging. PLoS One (2013) 0.82
Endomorphin-1 and endomorphin-2 differentially interact with specific binding sites for substance P (SP) aminoterminal SP1-7 in the rat spinal cord. Peptides (2005) 0.82
Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity. J Med Chem (2004) 0.82
HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells. J Med Chem (2010) 0.81
HIV-1 Vif-derived peptide inhibits drug-resistant HIV proteases. Biochem Biophys Res Commun (2002) 0.81
2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase. J Med Chem (2010) 0.81
New selective AT2 receptor ligands encompassing a gamma-turn mimetic replacing the amino acid residues 4-5 of angiotensin II act as agonists. J Med Chem (2005) 0.81
Structure-activity relationships of HCV NS3 protease inhibitors evaluated on the drug-resistant variants A156T and D168V. Antivir Ther (2010) 0.81
A new structural theme in C2-symmetric HIV-1 protease inhibitors: ortho-substituted P1/P1' side chains. Bioorg Med Chem (2006) 0.81