Published in J Med Chem on April 08, 2010
Synergism between a serotonin 5-HT2A receptor (5-HT2AR) antagonist and 5-HT2CR agonist suggests new pharmacotherapeutics for cocaine addiction. ACS Chem Neurosci (2012) 1.06
Development and in vitro characterization of a novel bifunctional μ-agonist/δ-antagonist opioid tetrapeptide. ACS Chem Biol (2011) 1.03
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Design of novel peptide ligands which have opioid agonist activity and CCK antagonist activity for the treatment of pain. Life Sci (2003) 1.24
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. J Med Chem (2006) 1.16
Environment and mobility of a series of fluorescent reporters at the amino terminus of structurally related peptide agonists and antagonists bound to the cholecystokinin receptor. J Biol Chem (2002) 1.15
Narcotic antagonistic potency of bivalent ligands which contain beta-naltrexamine. Evidence for bridging between proximal recognition sites. J Med Chem (1982) 1.10
Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands. J Med Chem (2009) 1.06
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. J Med Chem (2007) 0.94
Cholecystokinin-B receptor antagonists attenuate morphine dependence and withdrawal in rats. Neuroreport (2000) 0.94
Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors. J Med Chem (2009) 0.93
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Antidepressant-like effects of kappa-opioid receptor antagonists in the forced swim test in rats. J Pharmacol Exp Ther (2003) 3.48
Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol Rev (2010) 3.27
Study of recurrence after surgical resection of intraductal papillary mucinous neoplasm of the pancreas. Gastroenterology (2002) 2.76
Effects of kappa-opioid receptor ligands on intracranial self-stimulation in rats. Psychopharmacology (Berl) (2004) 2.35
A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers. Proc Natl Acad Sci U S A (2005) 2.31
Opioid-induced tolerance and dependence in mice is modulated by the distance between pharmacophores in a bivalent ligand series. Proc Natl Acad Sci U S A (2005) 2.29
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Serine-arginine protein kinase 1 overexpression is associated with tumorigenic imbalance in mitogen-activated protein kinase pathways in breast, colonic, and pancreatic carcinomas. Cancer Res (2007) 1.73
Possible endogenous agonist mechanism for the activation of secretin family G protein-coupled receptors. Mol Pharmacol (2006) 1.72
A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers. J Med Chem (2004) 1.61
Transmembrane segment IV contributes a functionally important interface for oligomerization of the Class II G protein-coupled secretin receptor. J Biol Chem (2007) 1.55
Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening. Mol Pharmacol (2010) 1.49
Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations. Proc Natl Acad Sci U S A (2013) 1.46
A bivalent ligand (KDAN-18) containing delta-antagonist and kappa-agonist pharmacophores bridges delta2 and kappa1 opioid receptor phenotypes. J Med Chem (2005) 1.41
Targeting the RNA splicing machinery as a novel treatment strategy for pancreatic carcinoma. Cancer Res (2006) 1.29
Interaction of bivalent ligand KDN21 with heterodimeric delta-kappa opioid receptors in human embryonic kidney 293 cells. Mol Pharmacol (2005) 1.29
Spatial approximation between the amino terminus of a peptide agonist and the top of the sixth transmembrane segment of the secretin receptor. J Biol Chem (2003) 1.26
Constitutive formation of oligomeric complexes between family B G protein-coupled vasoactive intestinal polypeptide and secretin receptors. Mol Pharmacol (2005) 1.23
Absence of conditioned place preference or reinstatement with bivalent ligands containing mu-opioid receptor agonist and delta-opioid receptor antagonist pharmacophores. Eur J Pharmacol (2007) 1.22
Ligands that interact with putative MOR-mGluR5 heteromer in mice with inflammatory pain produce potent antinociception. Proc Natl Acad Sci U S A (2013) 1.22
Molecular approximation between a residue in the amino-terminal region of calcitonin and the third extracellular loop of the class B G protein-coupled calcitonin receptor. J Biol Chem (2004) 1.21
Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation. J Biol Chem (2011) 1.19
Heterodimerization of type A and B cholecystokinin receptors enhance signaling and promote cell growth. J Biol Chem (2003) 1.17
Molecular approximations between residues 21 and 23 of secretin and its receptor: development of a model for peptide docking with the amino terminus of the secretin receptor. Mol Pharmacol (2007) 1.16
Environment and mobility of a series of fluorescent reporters at the amino terminus of structurally related peptide agonists and antagonists bound to the cholecystokinin receptor. J Biol Chem (2002) 1.15
Standard opioid agonists activate heteromeric opioid receptors: evidence for morphine and [d-Ala(2)-MePhe(4)-Glyol(5)]enkephalin as selective μ-δ agonists. ACS Chem Neurosci (2009) 1.13
Mapping spatial approximations between the amino terminus of secretin and each of the extracellular loops of its receptor using cysteine trapping. FASEB J (2012) 1.13
Functional importance of a structurally distinct homodimeric complex of the family B G protein-coupled secretin receptor. Mol Pharmacol (2009) 1.12
Dimeric arrangement of the parathyroid hormone receptor and a structural mechanism for ligand-induced dissociation. J Biol Chem (2010) 1.10
A misspliced form of the cholecystokinin-B/gastrin receptor in pancreatic carcinoma: role of reduced sellular U2AF35 and a suboptimal 3'-splicing site leading to retention of the fourth intron. Cancer Res (2002) 1.10
Dimerization in the absence of higher-order oligomerization of the G protein-coupled secretin receptor. Biochim Biophys Acta (2008) 1.10
Kappa opioid antagonist effects of the novel kappa antagonist 5'-guanidinonaltrindole (GNTI) in an assay of schedule-controlled behavior in rhesus monkeys. Psychopharmacology (Berl) (2002) 1.09
Molecular basis of secretin docking to its intact receptor using multiple photolabile probes distributed throughout the pharmacophore. J Biol Chem (2011) 1.06
Spatial approximation between secretin residue five and the third extracellular loop of its receptor provides new insight into the molecular basis of natural agonist binding. Mol Pharmacol (2008) 1.06
Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands. J Med Chem (2009) 1.06
N-naphthoyl-beta-naltrexamine (NNTA), a highly selective and potent activator of μ/kappa-opioid heteromers. Proc Natl Acad Sci U S A (2011) 1.05
Pattern of intra-family hetero-oligomerization involving the G-protein-coupled secretin receptor. J Mol Neurosci (2008) 1.05
Secretin receptor oligomers form intracellularly during maturation through receptor core domains. Biochemistry (2006) 1.05
Differential effects of modification of membrane cholesterol and sphingolipids on the conformation, function, and trafficking of the G protein-coupled cholecystokinin receptor. J Biol Chem (2004) 1.04
Importance of the amino terminus in secretin family G protein-coupled receptors. Intrinsic photoaffinity labeling establishes initial docking constraints for the calcitonin receptor. J Biol Chem (2003) 1.04
Molecular basis of glucagon-like peptide 1 docking to its intact receptor studied with carboxyl-terminal photolabile probes. J Biol Chem (2009) 1.04
Refinement of the conformation of a critical region of charge-charge interaction between cholecystokinin and its receptor. Mol Pharmacol (2002) 1.04
Transmembrane segment peptides can disrupt cholecystokinin receptor oligomerization without affecting receptor function. Biochemistry (2006) 1.03
Silencing of secretin receptor function by dimerization with a misspliced variant secretin receptor in ductal pancreatic adenocarcinoma. Cancer Res (2002) 1.03
Spatial approximations between residues 6 and 12 in the amino-terminal region of glucagon-like peptide 1 and its receptor: a region critical for biological activity. J Biol Chem (2010) 1.02
Structure and function of Norrin in assembly and activation of a Frizzled 4-Lrp5/6 complex. Genes Dev (2013) 1.01
Secretin occupies a single protomer of the homodimeric secretin receptor complex: insights from photoaffinity labeling studies using dual sites of covalent attachment. J Biol Chem (2010) 1.01
Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation. Mol Pharmacol (2011) 1.00
Allosteric interactions between δ and κ opioid receptors in peripheral sensory neurons. Mol Pharmacol (2011) 1.00
Molecular characterization and distribution of motilin family receptors in the human gastrointestinal tract. J Gastroenterol (2006) 0.99
Therapeutic potential for novel drugs targeting the type 1 cholecystokinin receptor. Br J Pharmacol (2009) 0.99
Insights into the structural basis of endogenous agonist activation of family B G protein-coupled receptors. Mol Endocrinol (2008) 0.98
Quiescin sulfhydryl oxidase 1 promotes invasion of pancreatic tumor cells mediated by matrix metalloproteinases. Mol Cancer Res (2011) 0.98
Importance of each residue within secretin for receptor binding and biological activity. Biochemistry (2011) 0.98
Spatial approximation between a photolabile residue in position 13 of secretin and the amino terminus of the secretin receptor. Mol Pharmacol (2003) 0.97
Molecular basis of association of receptor activity-modifying protein 3 with the family B G protein-coupled secretin receptor. Biochemistry (2009) 0.97
Novel benzodiazepine photoaffinity probe stereoselectively labels a site deep within the membrane-spanning domain of the cholecystokinin receptor. J Med Chem (2006) 0.97
Paired cysteine mutagenesis to establish the pattern of disulfide bonds in the functional intact secretin receptor. J Biol Chem (2005) 0.96
Fluorescence resonance energy transfer analysis of secretin docking to its receptor: mapping distances between residues distributed throughout the ligand pharmacophore and distinct receptor residues. J Biol Chem (2007) 0.96
Molecular pharmacology of the secretin receptor. Receptors Channels (2002) 0.96
Use of probes with fluorescence indicator distributed throughout the pharmacophore to examine the peptide agonist-binding environment of the family B G protein-coupled secretin receptor. J Biol Chem (2005) 0.96
CCK(2) receptor splice variant with intron 4 retention in human gastrointestinal and lung tumours. J Cell Mol Med (2009) 0.95
Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor. Bioorg Med Chem Lett (2008) 0.95
A bivalent ligand (KMN-21) antagonist for mu/kappa heterodimeric opioid receptors. Bioorg Med Chem Lett (2009) 0.94
Insights into interactions between the alpha-helical region of the salmon calcitonin antagonists and the human calcitonin receptor using photoaffinity labeling. J Biol Chem (2005) 0.94
Fluorescent indicators distributed throughout the pharmacophore of cholecystokinin provide insights into distinct modes of binding and activation of type A and B cholecystokinin receptors. J Biol Chem (2006) 0.94
Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors. J Med Chem (2009) 0.93
Differential sensitivity of types 1 and 2 cholecystokinin receptors to membrane cholesterol. J Lipid Res (2011) 0.93
Role of N-linked glycosylation in biosynthesis, trafficking, and function of the human glucagon-like peptide 1 receptor. Am J Physiol Endocrinol Metab (2010) 0.92
Naloxone acts as a potent analgesic in transgenic mouse models of sickle cell anemia. Proc Natl Acad Sci U S A (2007) 0.92
Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor. J Biol Chem (2012) 0.92
Distinct molecular mechanisms for agonist peptide binding to types A and B cholecystokinin receptors demonstrated using fluorescence spectroscopy. J Biol Chem (2004) 0.92
Clinically employed opioid analgesics produce antinociception via μ-δ opioid receptor heteromers in Rhesus monkeys. ACS Chem Neurosci (2012) 0.92
Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function. J Biol Chem (2011) 0.90
The FEMA GRAS assessment of cinnamyl derivatives used as flavor ingredients. Food Chem Toxicol (2004) 0.90
Analysis of the cellular and molecular mechanisms of trophic action of a misspliced form of the type B cholecystokinin receptor present in colon and pancreatic cancer. Cancer Lett (2005) 0.90
Key differences in molecular complexes of the cholecystokinin receptor with structurally related peptide agonist, partial agonist, and antagonist. Mol Pharmacol (2004) 0.90
Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: implications for drug discovery. Mol Endocrinol (2013) 0.89
The δ opioid receptor agonist SNC80 selectively activates heteromeric μ-δ opioid receptors. ACS Chem Neurosci (2012) 0.89
Selectivity of delta- and kappa-opioid ligands depends on the route of central administration in mice. J Pharmacol Exp Ther (2007) 0.89
Homology modeling and molecular dynamics simulations of the mu opioid receptor in a membrane-aqueous system. Chembiochem (2005) 0.89
Disulfide bond structure and accessibility of cysteines in the ectodomain of the cholecystokinin receptor: specific mono-reactive receptor constructs examine charge-sensitivity of loop regions. Receptors Channels (2003) 0.89
Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery. Proc Natl Acad Sci U S A (2012) 0.89
Juxtamembranous region of the amino terminus of the family B G protein-coupled calcitonin receptor plays a critical role in small-molecule agonist action. J Biol Chem (2009) 0.88
Fluorescence resonance energy transfer analysis of the antagonist- and partial agonist-occupied states of the cholecystokinin receptor. J Biol Chem (2005) 0.88
Differential docking of high-affinity peptide ligands to type A and B cholecystokinin receptors demonstrated by photoaffinity labeling. Biochemistry (2005) 0.88
Sensitivity of cholecystokinin receptors to membrane cholesterol content. Front Endocrinol (Lausanne) (2012) 0.87
Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor. J Biol Chem (2013) 0.87
Measurement of intermolecular distances for the natural agonist Peptide docked at the cholecystokinin receptor expressed in situ using fluorescence resonance energy transfer. Mol Pharmacol (2004) 0.87
Functional and structural diversification of the Anguimorpha lizard venom system. Mol Cell Proteomics (2010) 0.87
Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function. Biochem Soc Trans (2013) 0.87
Interaction among four residues distributed through the secretin pharmacophore and a focused region of the secretin receptor amino terminus. Mol Endocrinol (2002) 0.87
Importance of lipid-exposed residues in transmembrane segment four for family B calcitonin receptor homo-dimerization. Regul Pept (2010) 0.87