Published in Biochem Biophys Res Commun on September 23, 2013
High-resolution mapping of epitopes on the C2 domain of factor VIII by analysis of point mutants using surface plasmon resonance. Blood (2014) 1.46
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Oral effectiveness of PMIC4, a novel hydroxyethylpiperazine analogue, in Leishmania amazonensis. Int J Parasitol Drugs Drug Resist (2014) 0.75
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A (2008) 17.41
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Phosphorylation of Ser-129 is the dominant pathological modification of alpha-synuclein in familial and sporadic Lewy body disease. J Biol Chem (2006) 4.06
Epitope and isotype specificities of antibodies to beta -amyloid peptide for protection against Alzheimer's disease-like neuropathology. Proc Natl Acad Sci U S A (2003) 2.58
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design. Nat Biotechnol (2005) 2.51
Passive immunization reduces behavioral and neuropathological deficits in an alpha-synuclein transgenic model of Lewy body disease. PLoS One (2011) 2.19
Beta-amyloid immunotherapy prevents synaptic degeneration in a mouse model of Alzheimer's disease. J Neurosci (2005) 1.85
Structural basis for the activity of drugs that inhibit phosphodiesterases. Structure (2004) 1.84
Crystal structures of proto-oncogene kinase Pim1: a target of aberrant somatic hypermutations in diffuse large cell lymphoma. J Mol Biol (2005) 1.79
Immunotherapy reduces vascular amyloid-beta in PDAPP mice. J Neurosci (2008) 1.70
Comprehensive and quantitative mapping of energy landscapes for protein-protein interactions by rapid combinatorial scanning. J Biol Chem (2006) 1.59
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases. J Med Chem (2005) 1.33
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett (2007) 1.30
Discovery of novel selective inhibitors of human intestinal carboxylesterase for the amelioration of irinotecan-induced diarrhea: synthesis, quantitative structure-activity relationship analysis, and biological activity. Mol Pharmacol (2004) 1.18
Crystal structure of complete rhinovirus RNA polymerase suggests front loading of protein primer. J Virol (2005) 1.17
Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase. Bioorg Med Chem Lett (2006) 1.12
Morphological characterization of Thioflavin-S-positive amyloid plaques in transgenic Alzheimer mice and effect of passive Abeta immunotherapy on their clearance. Am J Pathol (2004) 1.11
Parallel synthesis of 5-cyano-6-aryl-2-thiouracil derivatives as inhibitors for hepatitis C viral NS5B RNA-dependent RNA polymerase. Bioorg Chem (2005) 1.10
Laminin-411 is a vascular ligand for MCAM and facilitates TH17 cell entry into the CNS. PLoS One (2012) 1.07
Antibody capture of soluble Abeta does not reduce cortical Abeta amyloidosis in the PDAPP mouse. Neurodegener Dis (2008) 1.03
Active beta-amyloid immunization restores spatial learning in PDAPP mice displaying very low levels of beta-amyloid. J Neurosci (2007) 1.02
Antagonistic effects of beta-site amyloid precursor protein-cleaving enzymes 1 and 2 on beta-amyloid peptide production in cells. J Biol Chem (2003) 1.01
Replicon cell culture system as a valuable tool in antiviral drug discovery against hepatitis C virus. Antivir Chem Chemother (2005) 0.99
Synthesis of thiazolone-based sulfonamides as inhibitors of HCV NS5B polymerase. Bioorg Med Chem Lett (2006) 0.97
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The role and significance of unconventional hydrogen bonds in small molecule recognition by biological receptors of pharmaceutical relevance. Curr Pharm Des (2007) 0.96
AL amyloid imaging and therapy with a monoclonal antibody to a cryptic epitope on amyloid fibrils. PLoS One (2012) 0.96
Structural correlates of antibodies associated with acute reversal of amyloid beta-related behavioral deficits in a mouse model of Alzheimer disease. J Biol Chem (2009) 0.94
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Axonopathy in an α-synuclein transgenic model of Lewy body disease is associated with extensive accumulation of C-terminal-truncated α-synuclein. Am J Pathol (2013) 0.92
Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors. Bioorg Med Chem Lett (2009) 0.91
Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease. Alzheimers Res Ther (2010) 0.91
Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A (2013) 0.91
Increased T cell recruitment to the CNS after amyloid beta 1-42 immunization in Alzheimer's mice overproducing transforming growth factor-beta 1. J Neurosci (2006) 0.89
A novel shape-feature based approach to virtual library screening. J Chem Inf Comput Sci (2002) 0.88
Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain. ChemMedChem (2013) 0.87
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor. Bioorg Med Chem Lett (2011) 0.85
Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents. Bioorg Med Chem Lett (2009) 0.85
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo. J Biol Chem (2005) 0.85
Shapes of things: computer modeling of molecular shape in drug discovery. Curr Top Med Chem (2007) 0.84
Promising candidates for the treatment of chronic hepatitis C. Expert Opin Investig Drugs (2003) 0.84
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration. Bioorg Med Chem Lett (2010) 0.83
Discovery and structure-activity relationships of modified salicylanilides as cell permeable inhibitors of poly(ADP-ribose) glycohydrolase (PARG). J Med Chem (2011) 0.83
Including explicit water molecules as part of the protein structure in MM/PBSA calculations. J Chem Inf Model (2014) 0.83
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK. Bioorg Med Chem Lett (2010) 0.83
Structure-based design of a novel thiazolone scaffold as HCV NS5B polymerase allosteric inhibitors. Bioorg Med Chem Lett (2006) 0.82
Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents. J Med Chem (2002) 0.81
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model. Bioorg Med Chem Lett (2010) 0.81
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region. Bioorg Med Chem Lett (2010) 0.80
Novel cyclooxygenase-1 inhibitors discovered using affinity fingerprints. J Med Chem (2004) 0.80
Improved ligand binding energies derived from molecular dynamics: replicate sampling enhances the search of conformational space. J Chem Inf Model (2013) 0.80
Thiazolone-acylsulfonamides as novel HCV NS5B polymerase allosteric inhibitors: convergence of structure-based drug design and X-ray crystallographic study. Bioorg Med Chem Lett (2007) 0.79
Structure of human uridine-cytidine kinase 2 determined by SIRAS using a rotating-anode X-ray generator and a single samarium derivative. Acta Crystallogr D Biol Crystallogr (2005) 0.79
Potent 7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-based macrocyclic inhibitors of hepatitis C virus NS3 protease. J Med Chem (2006) 0.78
Isothiazoles as active-site inhibitors of HCV NS5B polymerase. Bioorg Med Chem Lett (2006) 0.78
Quantifying amyloid beta (Aβ)-mediated changes in neuronal morphology in primary cultures: implications for phenotypic screening. J Biomol Screen (2012) 0.78
A label-free approach to identify inhibitors of alpha4beta7-mediated cell adhesion to MadCAM. J Biomol Screen (2011) 0.77
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration. Bioorg Med Chem Lett (2011) 0.77
Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors. Bioorg Med Chem Lett (2013) 0.77
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents. Bioorg Med Chem Lett (2010) 0.77
Development of a novel β-secretase binding assay using the AlphaScreen platform. J Biomol Screen (2013) 0.77
Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates. Bioorg Med Chem Lett (2013) 0.76
Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors. Bioorg Med Chem Lett (2013) 0.76
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors. Bioorg Med Chem Lett (2010) 0.76
Generation and characterization of anti-AA amyloid-specific monoclonal antibodies. Front Immunol (2011) 0.76
Label free fragment screening using surface plasmon resonance as a tool for fragment finding - analyzing parkin, a difficult CNS target. PLoS One (2013) 0.76
Parkin depletion delays motor decline dose-dependently without overtly affecting neuropathology in α-synuclein transgenic mice. BMC Neurosci (2013) 0.76
Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958. J Pharmacol Exp Ther (2007) 0.76
N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase. Bioorg Med Chem Lett (2009) 0.76
Design, synthesis, and biological activity of m-tyrosine-based 16- and 17-membered macrocyclic inhibitors of hepatitis C virus NS3 serine protease. J Med Chem (2005) 0.75