Search Results - "Smiley, David L."
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A rationally designed monomeric peptide triagonist corrects obesity and diabetes in rodents
Published in Nature medicine (01-01-2015)“…A rationally designed peptide agonist that targets three key hormone receptors reduces obesity and its complications in a manner superior to other agonists. We…”
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2
Both acyl and des-acyl ghrelin regulate adiposity and glucose metabolism via central nervous system ghrelin receptors
Published in Diabetes (New York, N.Y.) (01-01-2014)“…Growth hormone secretagogue receptors (GHSRs) in the central nervous system (CNS) mediate hyperphagia and adiposity induced by acyl ghrelin (AG). Evidence…”
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3
Ghrelin‐induced adiposity is independent of orexigenic effects
Published in The FASEB journal (01-08-2011)“…ABSTRACT Ghrelin is a hormone produced predominantly by the stomach that targets a number of specific areas in the central nervous system to promote a positive…”
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4
A Novel Human-Based Receptor Antagonist of Sustained Action Reveals Body Weight Control by Endogenous GLP-1
Published in ACS chemical biology (18-02-2011)“…Ex-4 (9-39)a is a well characterized GLP-1 receptor antagonist that suffers from two notable limitations, its nonhuman amino acid sequence and its relatively…”
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5
Acylation Type Determines Ghrelin's Effects on Energy Homeostasis in Rodents
Published in Endocrinology (Philadelphia) (01-10-2012)“…Ghrelin is a gastrointestinal polypeptide that acts through the ghrelin receptor (GHSR) to promote food intake and increase adiposity. Activation of GHSR…”
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6
Unimolecular dual incretins maximize metabolic benefits in rodents, monkeys, and humans
Published in Science translational medicine (30-10-2013)“…We report the discovery and translational therapeutic efficacy of a peptide with potent, balanced co-agonism at both of the receptors for the incretin hormones…”
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7
Glucagon-like peptide-1 receptor-mediated endosomal cAMP generation promotes glucose-stimulated insulin secretion in pancreatic β-cells
Published in American journal of physiology: endocrinology and metabolism (15-07-2013)“…Glucagon-like peptide-1 receptor (GLP-1R) plays a major role in promoting glucose-stimulated insulin secretion in pancreatic β-cells. In the present study, we…”
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8
Ghrelin induces adiposity in rodents
Published in Nature (London) (19-10-2000)“…The discovery of the peptide hormone ghrelin, an endogenous ligand for the growth hormone secretagogue (GHS) receptor, yielded the surprising result that the…”
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9
Design and synthesis of statine-containing BACE inhibitors
Published in Bioorganic & medicinal chemistry letters (15-12-2003)“…Utilizing structure-based techniques and solid-phase synthesis, statine-based tetrapeptide BACE inhibitors were designed and synthesized using a heptapeptide…”
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10
A new quorum‐sensing system (TprA/PhrA) for Streptococcus pneumoniae D39 that regulates a lantibiotic biosynthesis gene cluster
Published in Molecular microbiology (01-07-2015)“…Summary The Phr peptides of the Bacillus species mediate quorum sensing, but their identification and function in other species of bacteria have not been…”
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11
Neuropeptide Y-Y2 receptors mediate anxiety in the amygdala
Published in Pharmacology, biochemistry and behavior (01-03-2002)“…The behavioral effects of direct injection of the neuropeptide Y (NPY) Y2 receptor agonist C2-NPY into the basolateral nucleus of the amygdala (BLA) was…”
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12
A Novel and Selective β-Melanocyte-Stimulating Hormone-Derived Peptide Agonist for Melanocortin 4 Receptor Potently Decreased Food Intake and Body Weight Gain in Diet-Induced Obese Rats
Published in Endocrinology (Philadelphia) (01-12-2005)“…αMSH has generally been accepted as the endogenous ligand for melanocortin 4 receptor (MC4R), which plays a major role in energy homeostasis. Targeting MC4R to…”
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13
Discovery of a β-MSH-Derived MC-4R Selective Agonist
Published in Journal of medicinal chemistry (05-05-2005)“…A series of novel, disulfide-constrained human β-melanocyte stimulating hormone (β-MSH)-derived peptides were optimized for in vitro melanocortin-4 receptor…”
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14
Europium-labeled melanin-concentrating hormone analogues: ligands for measuring binding to melanin-concentrating hormone receptors 1 and 2
Published in Analytical biochemistry (15-05-2004)“…We investigated the use of Eu 3+ chelate-labeled analogues of melanin-concentrating hormone (MCH) as ligands for both human MCH receptors (MCHR1 and MCHR2)…”
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15
Potent peptide agonists for human melanocortin 3 and 4 receptors derived from enzymatic cleavages of human β-MSH(5–22) by dipeptidyl peptidase I and dipeptidyl peptidase IV
Published in Peptides (New York, N.Y. : 1980) (01-10-2005)“…Human β-MSH(1–22) was first isolated from human pituitary as a 22-amino acid (aa) peptide derived from a precursor protein, pro-opiomelanocortin (POMC)…”
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16
Potent and selective MC-4 receptor agonists based on a novel disulfide scaffold
Published in Bioorganic & medicinal chemistry letters (15-10-2005)“…Extensive structure–activity relationship studies utilizing a β-MSH-derived cyclic nonapeptide, Ac-Tyr-Arg-[Cys-Glu-His- d-Phe-Arg-Trp-Cys]-NH 2 ( 3), led to…”
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17
The neuropeptide Y Y1 antagonist, 1229U91, a potent agonist for the human pancreatic polypeptide-preferring (NPY Y4) receptor
Published in Peptides (New York, N.Y. : 1980) (1998)“…Recently, a novel high-affinity peptide antagonist, 1229U91, was published as a selective neuropeptide Y Y1 antagonist. The selectivity of 1229U91 was…”
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18
Crystal structure of human parathyroid hormone 1-34 at 0.9-A resolution
Published in The Journal of biological chemistry (01-09-2000)“…The N-terminal fragment 1-34 of parathyroid hormone (PTH), administered intermittently, results in increased bone formation in patients with osteoporosis. PTH…”
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19
A new quorum‐sensing system ( TprA / PhrA ) for S treptococcus pneumoniae D 39 that regulates a lantibiotic biosynthesis gene cluster
Published in Molecular microbiology (01-07-2015)“…Summary The Phr peptides of the B acillus species mediate quorum sensing, but their identification and function in other species of bacteria have not been…”
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Journal Article -
20
Neuropeptide Y-Y 2 receptors mediate anxiety in the amygdala
Published in Pharmacology, biochemistry and behavior (01-03-2002)“…The behavioral effects of direct injection of the neuropeptide Y (NPY) Y 2 receptor agonist C2-NPY into the basolateral nucleus of the amygdala (BLA) was…”
Get full text
Journal Article