Search Results - "Reyes, Allan R."
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Probing the enzyme kinetics, allosteric modulation and activation of α1- and α2-subunit-containing AMP-activated protein kinase (AMPK) heterotrimeric complexes by pharmacological and physiological activators
Published in Biochemical journal (01-03-2016)“…AMP-activated protein kinase (AMPK) is a serine/threonine protein kinase that serves as a pleotropic regulator of whole body energy homoeostasis. AMPK exists…”
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2
Crystal structure of human lysosomal acid lipase and its implications in cholesteryl ester storage disease[S]
Published in Journal of lipid research (01-08-2020)“…Lysosomal acid lipase (LAL) is a serine hydrolase that hydrolyzes cholesteryl ester (CE) and TGs delivered to the lysosomes into free cholesterol and fatty…”
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3
Expression and functional characterization of human lysosomal acid lipase gene (LIPA) mutation responsible for cholesteryl ester storage disease (CESD) phenotype
Published in Protein expression and purification (01-06-2015)“…•Mutations in lysosomal acid lipase are associated with Wolman disease and CESD.•Patients homozygous for His295Tyr (H295Y) mutation have <5% of normal LAL…”
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4
Genetic manipulation of lysine catabolism in maize kernels
Published in Plant molecular biology (01-01-2009)“…In plants, lysine catabolism is thought to be controlled by a bifunctional enzyme, lysine ketoglutarate reductase/saccharopine dehydrogenase (LKR/SDH). Lysine…”
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5
Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice
Published in Cell metabolism (02-05-2017)“…The AMP-activated protein kinase (AMPK) is a potential therapeutic target for metabolic diseases based on its reported actions in the liver and skeletal…”
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Discovery and Preclinical Characterization of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy
Published in Journal of medicinal chemistry (08-09-2016)“…Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human…”
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7
Structural studies identify angiotensin II receptor blocker-like compounds as branched-chain ketoacid dehydrogenase kinase inhibitors
Published in The Journal of biological chemistry (01-03-2023)“…The mammalian mitochondrial branched-chain ketoacid dehydrogenase (BCKD) complex is a multienzyme complex involved in the catabolism of branched-chain amino…”
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Discovery of First Branched-Chain Ketoacid Dehydrogenase Kinase (BDK) Inhibitor Clinical Candidate PF-07328948
Published in Journal of medicinal chemistry (19-11-2024)“…Inhibition of branched-chain ketoacid dehydrogenase kinase (BDK or BCKDK), a negative regulator of branched-chain amino acid (BCAA) metabolism, is hypothesized…”
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Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels
Published in Nature communications (09-08-2023)“…Branched chain amino acid (BCAA) catabolic impairments have been implicated in several diseases. Branched chain ketoacid dehydrogenase (BCKDH) controls the…”
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Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK)
Published in Journal of medicinal chemistry (23-08-2018)“…Studies on indole-3-carboxylic acid derivatives as direct activators of human adenosine monophosphate-activated protein kinase (AMPK) α1β1γ1 isoform have…”
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11
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK)
Published in Journal of medicinal chemistry (22-03-2018)“…Optimization of the pharmacokinetic (PK) properties of a series of activators of adenosine monophosphate-activated protein kinase (AMPK) is described…”
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12
Biophysical Interactions of Direct AMPK Activators
Published in Methods in molecular biology (Clifton, N.J.) (01-01-2018)“…Protein-ligand interactions can be evaluated by a number of different biophysical methods. Here we describe some of the experimental methods that we have used…”
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13
Development of a selective activity-based probe for glycosylated LIPA
Published in Bioorganic & medicinal chemistry letters (15-04-2016)“…[Display omitted] Loss of LIPA activity leads to diseases such as Wolman’s Disease and Cholesterol Ester Storage Disease. While it is possible to measure…”
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14
Structure-guided Inhibitor Design for Human Acetyl-coenzyme A Carboxylase by Interspecies Active Site Conversion
Published in The Journal of biological chemistry (02-12-2011)“…Inhibition of acetyl-CoA carboxylases (ACCs), a crucial enzyme for fatty acid metabolism, has been shown to promote fatty acid oxidation and reduce body fat in…”
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15
Structural Basis for AMPK Activation: Natural and Synthetic Ligands Regulate Kinase Activity from Opposite Poles by Different Molecular Mechanisms
Published in Structure (London) (05-08-2014)“…AMP-activated protein kinase (AMPK) is a principal metabolic regulator affecting growth and response to cellular stress. Comprised of catalytic and regulatory…”
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16
Acyl Glucuronide Metabolites of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK)
Published in Journal of medicinal chemistry (23-08-2018)“…Studies on indole-3-carboxylic acid derivatives as direct activators of human adenosine monophosphate-activated protein kinase (AMPK) α1β1γ1 isoform have…”
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Journal Article -
17
Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H -indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy
Published in Journal of medicinal chemistry (08-09-2016)Get full text
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18
Escherichia coli expression, purification and characterization of functional full-length recombinant α2β2γ3 heterotrimeric complex of human AMP-activated protein kinase
Published in Protein expression and purification (01-10-2010)“…AMP-activated protein kinase (AMPK) is an energy-sensing serine/threonine protein kinase that plays a central role in whole-body energy homeostasis. AMPK is a…”
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19
Escherichia coli expression, purification and characterization of functional full-length recombinant a2b2g3 heterotrimeric complex of human AMP-activated protein kinase
Published in Protein expression and purification (01-10-2010)“…AMP-activated protein kinase (AMPK) is an energy-sensing serine/threonine protein kinase that plays a central role in whole-body energy homeostasis. AMPK is a…”
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20
Escherichia coli expression, purification and characterization of functional full-length recombinant alpha2beta2gamma3 heterotrimeric complex of human AMP-activated protein kinase
Published in Protein expression and purification (01-10-2010)“…AMP-activated protein kinase (AMPK) is an energy-sensing serine/threonine protein kinase that plays a central role in whole-body energy homeostasis. AMPK is a…”
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