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Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats

Proceedings of the National Academy of Sciences - PNAS, 2016-03, Vol.113 (13), p.E1796-E1805

2016

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Inhibition of acetyl-CoA carboxylase suppresses fatty acid synthesis and tumor growth of non-small-cell lung cancer in preclinical models

Nature medicine, 2016-10, Vol.22 (10), p.1108-1119

2016

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An allosteric mechanism for potent inhibition of human ATP-citrate lyase

Nature (London), 2019-04, Vol.568 (7753), p.566-570

2019

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Acetyl‐coenzyme A carboxylase inhibition reduces de novo lipogenesis in overweight male subjects: A randomized, double‐blind, crossover study

Hepatology (Baltimore, Md.), 2017-08, Vol.66 (2), p.324-334

2017

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The adipocyte as an endocrine organ in the regulation of metabolic homeostasis

Neuropharmacology, 2012-07, Vol.63 (1), p.57-75

Harwood, H. James

2012

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Acetyl-coenzyme A carboxylases: Versatile targets for drug discovery

Journal of cellular biochemistry, 2006-12, Vol.99 (6), p.1476-1488

2006

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Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals

The Journal of pharmacology and experimental therapeutics, 2008-09, Vol.326 (3), p.801-808

2008

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Nonhuman primates and other animal models in diabetes research

Journal of diabetes science and technology, 2012-05, Vol.6 (3), p.503-514

2012

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Treating the metabolic syndrome: acetyl-CoA carboxylase inhibition

Expert opinion on therapeutic targets, 2005-04, Vol.9 (2), p.267-281

Harwood Jr, H James

2005

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CP-346086: an MTP inhibitor that lowers plasma cholesterol and triglycerides in experimental animals and in humans

Journal of lipid research, 2003-10, Vol.44 (10), p.1887

2003

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class of selective antibacterials derived from a protein kinase inhibitor pharmacophore

Proceedings of the National Academy of Sciences - PNAS, 2009-02, Vol.106 (6), p.1737-1742

2009

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Isozyme-nonselective N-Substituted Bipiperidylcarboxamide Acetyl-CoA Carboxylase Inhibitors Reduce Tissue Malonyl-CoA Concentrations, Inhibit Fatty Acid Synthesis, and Increase Fatty Acid Oxidation in Cultured Cells and in Experimental Animals

The Journal of biological chemistry, 2003-09, Vol.278 (39), p.37099-37111

2003

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Discovery of small molecule isozyme non-specific inhibitors of mammalian acetyl-CoA carboxylase 1 and 2

Bioorganic & medicinal chemistry letters, 2010-04, Vol.20 (7), p.2383-2388

2010

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Aminopyrrolidineamide inhibitors of site-1 protease

Bioorganic & medicinal chemistry letters, 2007-08, Vol.17 (16), p.4411-4414

2007

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Old World nonhuman primate models of type 2 diabetes mellitus

ILAR journal, 2006, Vol.47 (3), p.259-271

2006

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A selective peroxisome proliferator-activated receptor alpha agonist, CP-900691, improves plasma lipids, lipoproteins, and glycemic control in diabetic monkeys

The Journal of pharmacology and experimental therapeutics, 2010-06, Vol.333 (3), p.844-853

2010

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A selective cannabinoid-1 receptor antagonist, PF-95453, reduces body weight and body fat to a greater extent than pair-fed controls in obese monkeys

The Journal of pharmacology and experimental therapeutics, 2010-10, Vol.335 (1), p.103-113

2010

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Short-term hyperglycemia increases arterial superoxide production and iron dysregulation in atherosclerotic monkeys

Metabolism, clinical and experimental, 2011-08, Vol.60 (8), p.1070-1080

2011

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Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors

Drug metabolism and disposition, 2007-03, Vol.35 (3), p.493-500

2007

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Dual-action hypoglycemic and hypocholesterolemic agents that inhibit glycogen phosphorylase and lanosterol demethylase

Journal of lipid research, 2005-03, Vol.46 (3), p.547-563

2005

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Acetyl-CoA carboxylase inhibition for the treatment of metabolic syndrome

Current opinion in investigational drugs (London, England : 2000), 2004-03, Vol.5 (3), p.283

Harwood, Jr, H James

2004

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Structure-guided Inhibitor Design for Human Acetyl-coenzyme A Carboxylase by Interspecies Active Site Conversion

The Journal of biological chemistry, 2011-12, Vol.286 (48), p.41510-41519

2011

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Partial blockage of sterol biosynthesis with a squalene synthase inhibitor in early postnatal Niemann-Pick type C npcnih null mice brains reduces neuronal cholesterol accumulation, abrogates astrogliosis, but may inhibit myelin maturation

Journal of neuroscience methods, 2008-02, Vol.168 (1), p.15-25

2008

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Inhibition of Mammalian Squalene Synthetase Activity by Zaragozic Acid A Is a Result of Competitive Inhibition Followed by Mechanism-based Irreversible Inactivation

The Journal of biological chemistry, 1995-04, Vol.270 (16), p.9083-9096

1995

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Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats

Inhibition of acetyl-CoA carboxylase suppresses fatty acid synthesis and tumor growth of non-small-cell lung cancer in preclinical models

An allosteric mechanism for potent inhibition of human ATP-citrate lyase

Acetyl‐coenzyme A carboxylase inhibition reduces de novo lipogenesis in overweight male subjects: A randomized, double‐blind, crossover study

The adipocyte as an endocrine organ in the regulation of metabolic homeostasis

Acetyl-coenzyme A carboxylases: Versatile targets for drug discovery

Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals

Nonhuman primates and other animal models in diabetes research

Treating the metabolic syndrome: acetyl-CoA carboxylase inhibition

CP-346086: an MTP inhibitor that lowers plasma cholesterol and triglycerides in experimental animals and in humans

class of selective antibacterials derived from a protein kinase inhibitor pharmacophore

Isozyme-nonselective N-Substituted Bipiperidylcarboxamide Acetyl-CoA Carboxylase Inhibitors Reduce Tissue Malonyl-CoA Concentrations, Inhibit Fatty Acid Synthesis, and Increase Fatty Acid Oxidation in Cultured Cells and in Experimental Animals

Discovery of small molecule isozyme non-specific inhibitors of mammalian acetyl-CoA carboxylase 1 and 2

Inhibition of Acetyl-CoA Carboxylase by Phosphorylation or the Inhibitor ND-654 Suppresses Lipogenesis and Hepatocellular Carcinoma

Aminopyrrolidineamide inhibitors of site-1 protease

Old World nonhuman primate models of type 2 diabetes mellitus

A selective peroxisome proliferator-activated receptor alpha agonist, CP-900691, improves plasma lipids, lipoproteins, and glycemic control in diabetic monkeys

A selective cannabinoid-1 receptor antagonist, PF-95453, reduces body weight and body fat to a greater extent than pair-fed controls in obese monkeys

Short-term hyperglycemia increases arterial superoxide production and iron dysregulation in atherosclerotic monkeys

Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors

Dual-action hypoglycemic and hypocholesterolemic agents that inhibit glycogen phosphorylase and lanosterol demethylase

Acetyl-CoA carboxylase inhibition for the treatment of metabolic syndrome

Structure-guided Inhibitor Design for Human Acetyl-coenzyme A Carboxylase by Interspecies Active Site Conversion

Partial blockage of sterol biosynthesis with a squalene synthase inhibitor in early postnatal Niemann-Pick type C npcnih null mice brains reduces neuronal cholesterol accumulation, abrogates astrogliosis, but may inhibit myelin maturation

Inhibition of Mammalian Squalene Synthetase Activity by Zaragozic Acid A Is a Result of Competitive Inhibition Followed by Mechanism-based Irreversible Inactivation

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