Published in J Med Chem on August 01, 2002
Both Th1 and Th17 are immunopathogenic but differ in other key biological activities. J Immunol (2008) 1.36
South African HIV-1 subtype C transmitted variants with a specific V2 motif show higher dependence on α4β7 for replication. Retrovirology (2015) 0.82
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Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A (2008) 17.41
Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature (2010) 16.12
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Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity. Proc Natl Acad Sci U S A (2012) 3.21
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design. Nat Biotechnol (2005) 2.51
ANGPTL3 stimulates endothelial cell adhesion and migration via integrin alpha vbeta 3 and induces blood vessel formation in vivo. J Biol Chem (2002) 2.02
Engineering human IgG1 affinity to human neonatal Fc receptor: impact of affinity improvement on pharmacokinetics in primates. J Immunol (2009) 1.93
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
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Global gene expression analysis of human erythroid progenitors. Blood (2011) 1.59
Comprehensive and quantitative mapping of energy landscapes for protein-protein interactions by rapid combinatorial scanning. J Biol Chem (2006) 1.59
An in vivo human-plasmablast enrichment technique allows rapid identification of therapeutic influenza A antibodies. Cell Host Microbe (2013) 1.46
Comparative structural analysis of the Erbin PDZ domain and the first PDZ domain of ZO-1. Insights into determinants of PDZ domain specificity. J Biol Chem (2006) 1.43
Pharmacokinetics of humanized monoclonal anti-tumor necrosis factor-{alpha} antibody and its neonatal Fc receptor variants in mice and cynomolgus monkeys. Drug Metab Dispos (2010) 1.38
Structures of APRIL-receptor complexes: like BCMA, TACI employs only a single cysteine-rich domain for high affinity ligand binding. J Biol Chem (2004) 1.38
Structural and functional analysis of the PDZ domains of human HtrA1 and HtrA3. Protein Sci (2007) 1.31
Vascular endothelial-junctional adhesion molecule (VE-JAM)/JAM 2 interacts with T, NK, and dendritic cells through JAM 3. J Immunol (2002) 1.26
Stability of cyclic beta-hairpins: asymmetric contributions from side chains of a hydrogen-bonded cross-strand residue pair. J Am Chem Soc (2003) 1.23
Disruption of PH-kinase domain interactions leads to oncogenic activation of AKT in human cancers. Proc Natl Acad Sci U S A (2012) 1.22
Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res (2013) 1.18
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A therapeutic anti-VEGF antibody with increased potency independent of pharmacokinetic half-life. Cancer Res (2010) 1.10
Therapeutic peptides. Trends Biotechnol (2003) 1.08
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J Med Chem (2011) 1.08
Redesigning an antibody fragment for faster association with its antigen. Biochemistry (2003) 1.04
Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition. J Med Chem (2012) 1.03
On the edge of validation--cancer protease fibroblast activation protein. Mini Rev Med Chem (2008) 1.02
Potent and highly selective benzimidazole inhibitors of PI3-kinase delta. J Med Chem (2012) 0.99
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. J Med Chem (2010) 0.99
Tumor-specific activation of an EGFR-targeting probody enhances therapeutic index. Sci Transl Med (2013) 0.98
Turn stability in beta-hairpin peptides: Investigation of peptides containing 3:5 type I G1 bulge turns. Protein Sci (2003) 0.96
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem (2012) 0.96
Comparative analysis of the alpha-like globin clusters in mouse, rat, and human chromosomes indicates a mechanism underlying breaks in conserved synteny. Genome Res (2004) 0.96
Sequence plasticity in the antigen-binding site of a therapeutic anti-HER2 antibody. J Mol Biol (2002) 0.95
Identification and characterization of native proteins of Escherichia coli BL-21 that display affinity towards Immobilized Metal Affinity Chromatography and Hydrophobic Interaction Chromatography Matrices. Protein Expr Purif (2009) 0.94
Refinement of the solution structure of the heparin-binding domain of vascular endothelial growth factor using residual dipolar couplings. J Biomol NMR (2002) 0.94
CDK2/cyclinA inhibitors: targeting the cyclinA recruitment site with small molecules derived from peptide leads. Bioorg Med Chem Lett (2005) 0.92
Genetic deletion of JAM-C reveals a role in myeloid progenitor generation. Blood (2008) 0.92
SCL-mediated regulation of the cell-cycle regulator p21 is critical for murine megakaryopoiesis. Blood (2011) 0.92
Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A (2013) 0.91
Identification of a small peptide that inhibits PCSK9 protein binding to the low density lipoprotein receptor. J Biol Chem (2013) 0.90
Rapid identification of small binding motifs with high-throughput phage display: discovery of peptidic antagonists of IGF-1 function. Chem Biol (2002) 0.90
Competition between intercellular adhesion molecule-1 and a small-molecule antagonist for a common binding site on the alphal subunit of lymphocyte function-associated antigen-1. Protein Sci (2005) 0.89
A substrate-phage approach for investigating caspase specificity. Protein J (2004) 0.88
Stable "zeta" peptides that act as potent antagonists of the high-affinity IgE receptor. Proc Natl Acad Sci U S A (2002) 0.87
Discovery of pyrrolopyrimidine inhibitors of Akt. Bioorg Med Chem Lett (2010) 0.87
Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain. ChemMedChem (2013) 0.87
Convergent recognition of the IgE binding site on the high-affinity IgE receptor. Structure (2004) 0.85
Integrin alpha4beta1 function is required for cell survival in developing retina. Dev Biol (2004) 0.85
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor. Bioorg Med Chem Lett (2011) 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
Thermodynamic and kinetic characterization of hydroxyethylamine β-secretase-1 inhibitors. Biochem Biophys Res Commun (2013) 0.84
Alpha 4 integrins and vascular cell adhesion molecule-1 play a role in sympathetic innervation of the heart. J Neurosci (2002) 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
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
Calcium-independent inhibition of PCSK9 by affinity-improved variants of the LDL receptor EGF(A) domain. J Mol Biol (2012) 0.83
Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf. Bioorg Med Chem Lett (2012) 0.83
Technology comparisons for anti-therapeutic antibody and neutralizing antibody assays in the context of an anti-TNF pharmacokinetic study. J Immunol Methods (2009) 0.82
Phosphate ester serum albumin affinity tags greatly improve peptide half-life in vivo. Bioorg Med Chem Lett (2003) 0.82
Albumin affinity tags increase peptide half-life in vivo. Bioorg Med Chem Lett (2002) 0.82
Increases in free, unbound insulin-like growth factor I enhance insulin responsiveness in human hepatoma G2 cells in culture. J Biol Chem (2002) 0.81
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT). J Med Chem (2014) 0.81
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor. Bioorg Med Chem Lett (2010) 0.81
Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA. Bioorg Med Chem Lett (2011) 0.81
Complex with a phage display-derived peptide provides insight into the function of insulin-like growth factor I. Biochemistry (2003) 0.80
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region. Bioorg Med Chem Lett (2010) 0.80
Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors. Bioorg Med Chem Lett (2010) 0.80
Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity. Bioorg Med Chem Lett (2013) 0.79
N-Benzoyl amino acids as LFA-1/ICAM inhibitors 1: amino acid structure-activity relationship. Bioorg Med Chem Lett (2003) 0.79
Noncompetitive inhibition of hepatocyte growth factor-dependent Met signaling by a phage-derived peptide. J Mol Biol (2008) 0.79
Probody therapeutics for targeting antibodies to diseased tissue. Expert Opin Biol Ther (2014) 0.78
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
Discovery and SAR of spirochromane Akt inhibitors. Bioorg Med Chem Lett (2011) 0.77
N-Benzoyl amino acids as ICAM/LFA-1 inhibitors. Part 2: structure-activity relationship of the benzoyl moiety. Bioorg Med Chem Lett (2004) 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
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
Involvement of alpha4 integrins in maintenance of cardiac sympathetic axons. Auton Neurosci (2005) 0.76
Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores. Bioorg Med Chem Lett (2002) 0.76
Case studies of minimizing nonspecific inhibitors in HTS campaigns that use assay-ready plates. J Biomol Screen (2011) 0.75
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors. Bioorg Med Chem Lett (2013) 0.75
Thinking about abortion. First Things (1995) 0.75
Corrigendum: A broadly protective therapeutic antibody against influenza B virus with two mechanisms of action. Nat Commun (2017) 0.75
Lack of antenatal care in far north Queensland. Aust N Z J Obstet Gynaecol (2004) 0.75