Search Results - "Erion, Mark D"
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Targeting a ceramide double bond improves insulin resistance and hepatic steatosis
Published in Science (American Association for the Advancement of Science) (26-07-2019)“…Ceramides contribute to the lipotoxicity that underlies diabetes, hepatic steatosis, and heart disease. By genetically engineering mice, we deleted the enzyme…”
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2
Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy
Published in Science (American Association for the Advancement of Science) (04-08-2017)“…5′-Adenosine monophosphate–activated protein kinase (AMPK) is a master regulator of energy homeostasis in eukaryotes. Despite three decades of investigation,…”
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Functionally selective signaling and broad metabolic benefits by novel insulin receptor partial agonists
Published in Nature communications (17-02-2022)“…Insulin analogs have been developed to treat diabetes with focus primarily on improving the time action profile without affecting ligand-receptor interaction…”
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Author Correction: Functionally selective signaling and broad metabolic benefits by novel insulin receptor partial agonists
Published in Nature communications (23-01-2024)Get full text
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5
Glucagon receptor antagonism induces increased cholesterol absorption[S]
Published in Journal of lipid research (01-11-2015)“…Glucagon and insulin have opposing action in governing glucose homeostasis. In type 2 diabetes mellitus (T2DM), plasma glucagon is characteristically elevated,…”
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Free energy calculations to estimate ligand-binding affinities in structure-based drug design
Published in Current pharmaceutical design (01-01-2014)“…Post-genomic era has led to the discovery of several new targets posing challenges for structure-based drug design efforts to identify lead compounds. Multiple…”
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7
Pharmacological AMPK activation induces transcriptional responses congruent to exercise in skeletal and cardiac muscle, adipose tissues and liver
Published in PloS one (27-02-2019)“…Physical activity promotes metabolic and cardiovascular health benefits that derive in part from the transcriptional responses to exercise that occur within…”
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Targeting thyroid hormone receptor-β agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index
Published in Proceedings of the National Academy of Sciences - PNAS (25-09-2007)“…Despite efforts spanning four decades, the therapeutic potential of thyroid hormone receptor (TR) agonists as lipid-lowering and anti-obesity agents remains…”
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Advances in binding free energies calculations: QM/MM-based free energy perturbation method for drug design
Published in Current pharmaceutical design (2013)“…Multiple approaches have been devised and evaluated to computationally estimate binding free energies. Results using a recently developed Quantum Mechanics…”
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Discovery of Potent and Specific Fructose-1,6-Bisphosphatase Inhibitors and a Series of Orally-Bioavailable Phosphoramidase-Sensitive Prodrugs for the Treatment of Type 2 Diabetes
Published in Journal of the American Chemical Society (19-12-2007)“…Excessive glucose production by the liver coupled with decreased glucose uptake and metabolism by muscle, fat, and liver results in chronically elevated blood…”
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MB06322 (CS-917): A Potent and Selective Inhibitor of Fructose 1,6-Bisphosphatase for Controlling Gluconeogenesis in Type 2 Diabetes
Published in Proceedings of the National Academy of Sciences - PNAS (31-05-2005)“…In type 2 diabetes, the liver produces excessive amounts of glucose through the gluconeogenesis (GNG) pathway and consequently is partly responsible for the…”
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Prodrugs of Phosphates and Phosphonates
Published in Journal of medicinal chemistry (24-04-2008)Get full text
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Inhibition of Fructose 1,6-Bisphosphatase Reduces Excessive Endogenous Glucose Production and Attenuates Hyperglycemia in Zucker Diabetic Fatty Rats
Published in Diabetes (New York, N.Y.) (01-06-2006)“…Inhibition of Fructose 1,6-Bisphosphatase Reduces Excessive Endogenous Glucose Production and Attenuates Hyperglycemia in Zucker Diabetic Fatty Rats Paul D…”
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Liver-targeted drug delivery using HepDirect prodrugs
Published in The Journal of pharmacology and experimental therapeutics (01-02-2005)“…Targeting drugs to specific organs, tissues, or cells is an attractive strategy for enhancing drug efficacy and reducing side effects. Drug carriers such as…”
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Antiviral Efficacy upon Administration of a HepDirect Prodrug of 2′-C-Methylcytidine to Hepatitis C Virus-Infected Chimpanzees
Published in Antimicrobial Agents and Chemotherapy (01-08-2011)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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A Long-Acting PYY 3-36 Analog Mediates Robust Anorectic Efficacy with Minimal Emesis in Nonhuman Primates
Published in Cell metabolism (02-04-2019)“…The gut hormone PYY reduces food intake in humans and exhibits at least additive efficacy in combination with GLP-1. However, the utility of PYY analogs as…”
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A Long-Acting PYY3–36 Analog Mediates Robust Anorectic Efficacy with Minimal Emesis in Nonhuman Primates
Published in Cell metabolism (02-04-2019)“…The gut hormone PYY3–36 reduces food intake in humans and exhibits at least additive efficacy in combination with GLP-1. However, the utility of PYY analogs as…”
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Preclinical Pharmacokinetics of a HepDirect Prodrug of a Novel Phosphonate-Containing Thyroid Hormone Receptor Agonist
Published in Drug metabolism and disposition (01-11-2008)“…The prodrug [(2 R ,4 S )-4-(3-chlorophenyl)-2-[(3,5-dimethyl-4-(4â²-hydroxy-3â²-isopropylbenzyl)phenoxy)methyl]-2-oxido-[1,3,2]-dioxaphosphonane (MB07811)]…”
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Discovery of a Series of Phosphonic Acid-Containing Thiazoles and Orally Bioavailable Diamide Prodrugs That Lower Glucose in Diabetic Animals Through Inhibition of Fructose-1,6-Bisphosphatase
Published in Journal of medicinal chemistry (13-01-2011)“…Oral delivery of previously disclosed purine and benzimidazole fructose-1,6-bisphosphatase (FBPase) inhibitors via prodrugs failed, which was likely due to…”
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Discovery of Insulin Receptor Partial Agonists MK-5160 and MK-1092 as Novel Basal Insulins with Potential to Improve Therapeutic Index
Published in Journal of medicinal chemistry (14-04-2022)“…We have identified a series of novel insulin receptor partial agonists (IRPAs) with a potential to mitigate the risk of hypoglycemia associated with the use of…”
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