Published in J Med Chem on October 06, 2005
Prostanoid receptor antagonists: development strategies and therapeutic applications. Br J Pharmacol (2009) 1.31
The roles of the prostaglandin D(2) receptors DP(1) and CRTH2 in promoting allergic responses. Br J Pharmacol (2007) 1.21
New drugs targeting Th2 lymphocytes in asthma. J Occup Med Toxicol (2008) 1.03
Complete genome sequence of the ammonia-oxidizing bacterium and obligate chemolithoautotroph Nitrosomonas europaea. J Bacteriol (2003) 3.72
Mitochondrial disappearance from cells: a clue to the role of autophagy in programmed cell death and disease? Biochimie (2002) 2.59
Positional cloning of a novel gene influencing asthma from chromosome 2q14. Nat Genet (2003) 2.16
A role for IL-25 and IL-33-driven type-2 innate lymphoid cells in atopic dermatitis. J Exp Med (2013) 2.11
Prostaglandin D2 causes preferential induction of proinflammatory Th2 cytokine production through an action on chemoattractant receptor-like molecule expressed on Th2 cells. J Immunol (2005) 1.47
Antibacterial activities and characterization of novel inhibitors of LpxC. Antimicrob Agents Chemother (2002) 1.41
Antibacterial alkoxybenzamide inhibitors of the essential bacterial cell division protein FtsZ. Bioorg Med Chem Lett (2008) 1.16
Fragment-based activity space: smaller is better. Curr Opin Chem Biol (2008) 0.96
Glyco- and peptidomimetics from three-component Joullié-Ugi coupling show selective antiviral activity. J Am Chem Soc (2005) 0.95
IL-33-dependent Th2 response after rhinovirus infection in asthma: more information needed. Am J Respir Crit Care Med (2015) 0.95
The effect of food on the bioavailability of panobinostat, an orally active pan-histone deacetylase inhibitor, in patients with advanced cancer. Cancer Chemother Pharmacol (2011) 0.94
Inhibition of PI3K and calcineurin suppresses chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2)-dependent responses of Th2 lymphocytes to prostaglandin D(2). Biochem Pharmacol (2006) 0.93
An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction. Bioorg Med Chem Lett (2010) 0.93
Inhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459. Eur Respir J (2012) 0.92
Use of a Design of Experiments approach for the optimisation of a microwave assisted Ugi reaction. Org Biomol Chem (2004) 0.92
Novel function of CRTH2 in preventing apoptosis of human Th2 cells through activation of the phosphatidylinositol 3-kinase pathway. J Immunol (2009) 0.92
A dominant role for chemoattractant receptor-homologous molecule expressed on T helper type 2 (Th2) cells (CRTH2) in mediating chemotaxis of CRTH2+ CD4+ Th2 lymphocytes in response to mast cell supernatants. Immunology (2006) 0.92
Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease. J Med Chem (2012) 0.87
Leukotriene E4 activates human Th2 cells for exaggerated proinflammatory cytokine production in response to prostaglandin D2. J Immunol (2011) 0.86
Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor. Bioorg Med Chem Lett (2005) 0.86
The multiple roles of computational chemistry in fragment-based drug design. J Comput Aided Mol Des (2009) 0.85
Structure--activity relationships of the peptide deformylase inhibitor BB-3497: modification of the P2' and P3' side chains. Bioorg Med Chem Lett (2003) 0.85
Peptide deformylase inhibitors with activity against respiratory tract pathogens. Bioorg Med Chem Lett (2004) 0.85
2,3-Dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid derivatives: a novel class of small molecule heparanase inhibitors. Bioorg Med Chem Lett (2004) 0.85
Disease progression in MRL/lpr lupus-prone mice is reduced by NCS 613, a specific cyclic nucleotide phosphodiesterase type 4 (PDE4) inhibitor. PLoS One (2012) 0.85
Delta12-prostaglandin D2 is a potent and selective CRTH2 receptor agonist and causes activation of human eosinophils and Th2 lymphocytes. Prostaglandins Other Lipid Mediat (2005) 0.84
A clinical investigation of inhibitory effect of panobinostat on CYP2D6 substrate in patients with advanced cancer. Cancer Chemother Pharmacol (2013) 0.84
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the metal binding group. Bioorg Med Chem Lett (2002) 0.84
Potent agonists of the Hedgehog signaling pathway. Bioorg Med Chem Lett (2009) 0.83
Novel 6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohepta[f]indene analogues as potent and selective 5-HT(2C) agonists for the treatment of metabolic disorders. Bioorg Med Chem Lett (2010) 0.83
Prediction of cyclin-dependent kinase 2 inhibitor potency using the fragment molecular orbital method. J Cheminform (2011) 0.83
Development of a series of aryl pyrimidine kynurenine monooxygenase inhibitors as potential therapeutic agents for the treatment of Huntington's disease. J Med Chem (2015) 0.83
A paracrine role for chemoattractant receptor-homologous molecule expressed on T helper type 2 cells (CRTH2) in mediating chemotactic activation of CRTH2+ CD4+ T helper type 2 lymphocytes. Immunology (2007) 0.83
Discovery of a novel Hsp90 inhibitor by fragment linking. ChemMedChem (2010) 0.82
Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase. J Med Chem (2010) 0.82
Fragment-based identification of Hsp90 inhibitors. ChemMedChem (2009) 0.82
Cross-linking of protein crystals as an aid in the generation of binary protein-ligand crystal complexes, exemplified by the human PDE10a-papaverine structure. Acta Crystallogr D Biol Crystallogr (2009) 0.82
Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. J Pharmacol Exp Ther (2011) 0.81
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis. J Med Chem (2012) 0.81
Membrane tetraheme cytochrome c(m552) of the ammonia-oxidizing nitrosomonas europaea: a ubiquinone reductase. Biochemistry (2008) 0.81
Fragment screening by biochemical assay. Expert Opin Drug Discov (2006) 0.80
Apoptosis-specific protein (ASP 45 kDa) is distinct from human Apg5, the homologue of the yeast autophagic gene apg5. FEBS Lett (2002) 0.80
Potent inhibitors of the hedgehog signaling pathway. J Med Chem (2008) 0.79
Exploiting differences in caspase-2 and -3 S₂ subsites for selectivity: structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors. Bioorg Med Chem (2011) 0.79
PGH1, the precursor for the anti-inflammatory prostaglandins of the 1-series, is a potent activator of the pro-inflammatory receptor CRTH2/DP2. PLoS One (2012) 0.78
An in silico method for predicting Ames activities of primary aromatic amines by calculating the stabilities of nitrenium ions. J Chem Inf Model (2010) 0.78
Fighting obesity with a sugar-based library: discovery of novel MCH-1R antagonists by a new computational-VAST approach for exploration of GPCR binding sites. J Chem Inf Model (2013) 0.78
TBAF-catalysed silver oxide-mediated cross-coupling of functional trimethysilylpyridines: access to arylpyridines and bihetaryl compounds. Org Biomol Chem (2011) 0.77
High-resolution crystal structure of human Mapkap kinase 3 in complex with a high affinity ligand. Protein Sci (2010) 0.77
Identification of G-protein-coupled receptors involved in inflammatory disease by genetic association studies. Curr Opin Pharmacol (2005) 0.77
Picking up the pieces with FBDD or FADD: invest early for future success. Drug Discov Today (2009) 0.77
Salbutamol inhibits trypsin-mediated production of CXCL8 by keratinocytes. Cytokine (2006) 0.77
An audit of pneumococcal and hepatitis vaccination in an outpatient HIV clinic. Sex Health (2012) 0.77
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the methylene spacer and the P1' side chain. Bioorg Med Chem Lett (2003) 0.77
The selection and design of GPCR ligands: from concept to the clinic. Comb Chem High Throughput Screen (2004) 0.76
Novel MK2 inhibitors by fragment screening. Comb Chem High Throughput Screen (2009) 0.76
Minimisation of palladium content in Suzuki cross-coupling reactions. Comb Chem High Throughput Screen (2006) 0.75
A soluble-polymer system for the asymmetric transfer hydrogenation of ketones. J Org Chem (2004) 0.75
Tetrahydrofuran-based amino acids as library scaffolds. J Comb Chem (2004) 0.75
Development of self-indicating resin. Comb Chem High Throughput Screen (2007) 0.75
Steve Carney talks to Mark Ashton and Mark Whittaker about Evotec and their approach to fragment-based drug discovery. Drug Discov Today (2007) 0.75