Published in J Med Chem on September 13, 2011
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Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets. Front Endocrinol (Lausanne) (2012) 1.18
Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor. Mol Pharmacol (2012) 1.00
Drug discovery opportunities and challenges at g protein coupled receptors for long chain free Fatty acids. Front Endocrinol (Lausanne) (2012) 0.98
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In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469. Naunyn Schmiedebergs Arch Pharmacol (2013) 0.77
A Novel TGR5 Activator WB403 Promotes GLP-1 Secretion and Preserves Pancreatic β-Cells in Type 2 Diabetic Mice. PLoS One (2015) 0.76
Arachidonic acid triggers [Ca2+]i increases in rat round spermatids by a likely GPR activation, ERK signalling and ER/acidic compartments Ca2+ release. PLoS One (2017) 0.75
Crystal structure of the µ-opioid receptor bound to a morphinan antagonist. Nature (2012) 6.18
T-helper-1-cell cytokines drive cancer into senescence. Nature (2013) 4.47
Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor. Nature (2010) 3.19
A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers. Proc Natl Acad Sci U S A (2005) 2.31
Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements. Nat Biotechnol (2010) 2.11
A molecular dissection of the glycoprotein hormone receptors. Trends Biochem Sci (2004) 1.89
Delay in treatment of colorectal cancer: multifactorial problem. World J Surg (2003) 1.89
Ligand-regulated oligomerization of beta(2)-adrenoceptors in a model lipid bilayer. EMBO J (2009) 1.86
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Role of radiotherapy in supratentorial primitive neuroectodermal tumor in young children: results of the German HIT-SKK87 and HIT-SKK92 trials. J Clin Oncol (2006) 1.73
Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist. Sci Signal (2013) 1.71
Long-term outcome and clinical prognostic factors in children with medulloblastoma treated in the prospective randomised multicentre trial HIT'91. Eur J Cancer (2009) 1.70
Targeting the prostaglandin D2 receptors DP and CRTH2 for treatment of inflammation. Curr Top Med Chem (2006) 1.70
Comparative analysis of magnetosome gene clusters in magnetotactic bacteria provides further evidence for horizontal gene transfer. Environ Microbiol (2009) 1.66
Diagnostic and prognostic impact of urinary catecholamines in neuroblastoma patients. Pediatr Blood Cancer (2007) 1.65
"Wait and see" strategy in localized neuroblastoma in infants: an option not only for cases detected by mass screening. Pediatr Blood Cancer (2004) 1.62
Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2. Mol Pharmacol (2005) 1.54
Rates of autoimmune diseases in Kaiser Permanente for use in vaccine adverse event safety studies. Vaccine (2009) 1.50
Activation of peroxisome-proliferator-activated receptors α and γ mediates remote ischemic preconditioning against myocardial infarction in vivo. Exp Biol Med (Maywood) (2010) 1.48
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Pharmacogenomic and structural analysis of constitutive g protein-coupled receptor activity. Annu Rev Pharmacol Toxicol (2007) 1.42
Emerging roles of DP and CRTH2 in allergic inflammation. Trends Mol Med (2006) 1.41
Treatment for soft tissue sarcoma in childhood and adolescence. Austrian results within the CWS 96 study. Wien Klin Wochenschr (2005) 1.39
GPR55 ligands promote receptor coupling to multiple signalling pathways. Br J Pharmacol (2010) 1.39
Functional analysis of the magnetosome island in Magnetospirillum gryphiswaldense: the mamAB operon is sufficient for magnetite biomineralization. PLoS One (2011) 1.38
Human papillomavirus prevalence and type distribution in invasive cervical cancer in sub-Saharan Africa. Int J Cancer (2013) 1.38
Dexamethasone induces cell death in insulin-secreting cells, an effect reversed by exendin-4. Diabetes (2006) 1.35
Glycoprotein hormone receptors: determinants in leucine-rich repeats responsible for ligand specificity. EMBO J (2003) 1.35
Diagnostic accuracy of colorectal cancer staging with whole-body PET/CT colonography. JAMA (2006) 1.29
Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-hydroxytryptamine-4 receptors. Mol Pharmacol (2009) 1.29
Applying label-free dynamic mass redistribution technology to frame signaling of G protein-coupled receptors noninvasively in living cells. Nat Protoc (2011) 1.26
Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. J Med Chem (2008) 1.25
Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors. Cell Signal (2002) 1.22
GPR55 regulates cannabinoid 2 receptor-mediated responses in human neutrophils. Cell Res (2011) 1.21
The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism. Mol Pharmacol (2013) 1.18
Prognostic relevance of clinical and biological risk factors in childhood medulloblastoma: results of patients treated in the prospective multicenter trial HIT'91. Clin Cancer Res (2007) 1.18
Fenamates as TRP channel blockers: mefenamic acid selectively blocks TRPM3. Br J Pharmacol (2011) 1.18
Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity. FASEB J (2008) 1.17
Discovery of a potent and selective GPR120 agonist. J Med Chem (2012) 1.16
Charge-transfer-induced structural rearrangements at both sides of organic/metal interfaces. Nat Chem (2010) 1.16
Intracellular multiplication of Legionella pneumophila depends on host cell amino acid transporter SLC1A5. Mol Microbiol (2005) 1.16
Antagonism of the prostaglandin D2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation. Respir Res (2007) 1.15
Interactions between intracellular domains as key determinants of the quaternary structure and function of receptor heteromers. J Biol Chem (2010) 1.15
Effects of human urotensin II in isolated vessels of various species; comparison with other vasoactive agents. Naunyn Schmiedebergs Arch Pharmacol (2001) 1.14
Ser and Thr residues modulate the conformation of pro-kinked transmembrane alpha-helices. Biophys J (2004) 1.14
A structural insight into the reorientation of transmembrane domains 3 and 5 during family A G protein-coupled receptor activation. Mol Pharmacol (2010) 1.14
Linking agonist binding to histamine H1 receptor activation. Nat Chem Biol (2005) 1.14
Hemophagocytic lymphohistiocytosis as severe adverse event of antineoplastic treatment in children. Haematologica (2008) 1.13
Activation of CCR5 by chemokines involves an aromatic cluster between transmembrane helices 2 and 3. J Biol Chem (2002) 1.13
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem (2005) 1.12
Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. ACS Med Chem Lett (2010) 1.12
cAMP-activated protein kinase-independent potentiation of insulin secretion by cAMP is impaired in SUR1 null islets. Diabetes (2002) 1.12
Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3. J Biol Chem (2011) 1.09
1,2-Di-hydro-spiro-[carbazole-3(4H),2'-[1,3]dioxolane]. Acta Crystallogr Sect E Struct Rep Online (2009) 1.08
An activation switch in the rhodopsin family of G protein-coupled receptors: the thyrotropin receptor. J Biol Chem (2005) 1.08
Overexpression of kinase-negative protein kinase Cdelta in pancreatic beta-cells protects mice from diet-induced glucose intolerance and beta-cell dysfunction. Diabetes (2009) 1.07
Rational design of dualsteric GPCR ligands: quests and promise. Br J Pharmacol (2010) 1.07
A physicogenetic method to assign ligand-binding relationships between 7TM receptors. Bioorg Med Chem Lett (2005) 1.06
The novel cellular mechanism of human 5-HT6 receptor through an interaction with Fyn. J Biol Chem (2006) 1.06
Molecular basis of ligand dissociation in β-adrenergic receptors. PLoS One (2011) 1.06
Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. J Med Chem (2012) 1.06
The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling. Nat Commun (2012) 1.05
Transplantation of CD3/CD19 depleted allografts from haploidentical family donors in paediatric leukaemia. Br J Haematol (2014) 1.05
Enhanced insulin sensitivity of gene-targeted mice lacking functional KCNQ1. Am J Physiol Regul Integr Comp Physiol (2009) 1.04
The C-terminal tail of CRTH2 is a key molecular determinant that constrains Galphai and downstream signaling cascade activation. J Biol Chem (2008) 1.01
Influence of the environment in the conformation of alpha-helices studied by protein database search and molecular dynamics simulations. Biophys J (2002) 1.01
Impact of helix irregularities on sequence alignment and homology modeling of G protein-coupled receptors. Chembiochem (2012) 1.00
Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3. J Biol Chem (2012) 1.00
Hetero-oligomerization of the P2Y11 receptor with the P2Y1 receptor controls the internalization and ligand selectivity of the P2Y11 receptor. Biochem J (2008) 1.00
Preradiation chemotherapy for pediatric patients with high-grade glioma. Cancer (2002) 1.00
Stimulation of osteoclast activity by low B-vitamin concentrations. Bone (2007) 0.99
Positive versus negative modulation of different endogenous chemokines for CC-chemokine receptor 1 by small molecule agonists through allosteric versus orthosteric binding. J Biol Chem (2008) 0.99
Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator. Mol Pharmacol (2011) 0.99
Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling. J Med Chem (2009) 0.98
The role of the prostaglandin D2 receptor, DP, in eosinophil trafficking. J Immunol (2007) 0.98
Survival and late effects in children with stage 4 neuroblastoma. Pediatr Blood Cancer (2011) 0.97
Fusarium verticillioides abscess of the nasal septum in an immunosuppressed child: case report and identification of the morphologically atypical fungal strain. J Clin Microbiol (2005) 0.97
Purinergic receptors influence the differentiation of human mesenchymal stem cells. Stem Cells Dev (2011) 0.97