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https://www.readbyqxmd.com/read/28106377/chemical-proteomics-maps-brain-region-specific-activity-of-endocannabinoid-hydrolases
#1
Marc P Baggelaar, Annelot van Esbroeck, Eva van Rooden, Bogdan I Florea, Herman S Overkleeft, Giovanni Marsicano, Francis Chaouloff, Mario van der Stelt
The biosynthetic and catabolic enzymes of the endocannabinoids tightly regulate endocannabinoid-mediated activation of the cannabinoid CB1 receptor. Monitoring the activities of these endocannabinoid hydrolases in different brain regions is, therefore, key to gain insight in spatiotemporal control of CB1 receptor-mediated physiology. We have employed a comparative chemical proteomics approach to quantitatively map the activity profile of endocannabinoid hydrolases in various mouse brain regions at the same time...
January 20, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28069688/up-regulation-of-cb2-receptors-in-reactive-astrocytes-in-canine-degenerative-myelopathy-a-disease-model-of-amyotrophic-lateral-sclerosis
#2
María Fernández-Trapero, Francisco Espejo-Porras, Carmen Rodríguez-Cueto, Joan R Coates, Carmen Pérez-Díaz, Eva de Lago, Javier Fernández-Ruiz
Targeting the CB2 receptor afforded neuroprotection in SOD1(G93A) mutant mice, a model of amyotrophic lateral sclerosis (ALS). The neuroprotective effects of CB2 receptors were facilitated by their up-regulation in the spinal cord in SOD1(G93A) mutant mice. Herein, we have investigated whether a similar CB2 receptor up-regulation, as well as parallel changes in other endocannabinoid elements, are evident in the spinal cord of dogs with degenerative myelopathy (DM), caused from mutations in the superoxide dismutase 1 gene (SOD1)...
January 9, 2017: Disease Models & Mechanisms
https://www.readbyqxmd.com/read/27992221/triazole-ureas-act-as-diacylglycerol-lipase-inhibitors-and-prevent-fasting-induced-refeeding
#3
Hui Deng, Sander Kooijman, Adrianus M C H van den Nieuwendijk, Daisuke Ogasawara, Tom van der Wel, Floris van Dalen, Marc P Baggelaar, Freek J Janssen, Richard J B H N van den Berg, Hans den Dulk, Benjamin F Cravatt, Herman S Overkleeft, Patrick C N Rensen, Mario van der Stelt
Triazole ureas constitute a versatile class of irreversible inhibitors that target serine hydrolases in both cells and animal models. We have previously reported that triazole ureas can act as selective and CNS-active inhibitors for diacylglycerol lipases (DAGLs), enzymes responsible for the biosynthesis of 2-arachidonoylglycerol (2-AG) that activates cannabinoid CB1 receptor. Here, we report the enantio- and diastereoselective synthesis and structure-activity relationship studies. We found that 2,4-substituted triazole ureas with a biphenylmethanol group provided the most optimal scaffold...
December 19, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27893720/a-functional-atg16l1-t300a-variant-is-associated-with-necrotizing-enterocolitis-in-premature-infants
#4
Venkatesh Sampath, Vineet Bhandari, Jessica Berger, Daniel Merchant, Liyun Zhang, Mihoko Ladd, Heather Menden, Jeffery Garland, Namasivayam Ambalavanan, Neil Mulrooney, Michael Quasney, John Dagle, Pascal M Lavoie, Pippa Simpson, Mary Dahmer
BACKGROUND: The genetic basis of dysfunctional immune responses in necrotizing enterocolitis (NEC) remains unknown. We hypothesized that variants in nucleotide binding and oligomerization domain (NOD)-like receptors (NLRs) and autophagy (ATG) genes modulate vulnerability to NEC. METHODS: We genotyped a multi-center cohort of premature infants with and without NEC for NOD1, NOD2, ATG16L1, CARD8, and NLRP3 variants. Chi-square tests and logistic regression were used for statistical analysis...
January 18, 2017: Pediatric Research
https://www.readbyqxmd.com/read/27784678/oxyradical-stress-increases-the-biosynthesis-of-2-arachidonoylglycerol-involvement-of-nadph-oxidase
#5
Anberitha T Matthews, Jung Hwa Lee, Abdolsamad Borazjani, Lee C Mangum, Xiang Hou, Matthew K Ross
NADPH oxidase (Nox)-derived oxyradicals contribute to atherosclerosis by oxidizing low-density lipoproteins (LDL), leading to their phagocytosis by vascular macrophages. Endocannabinoids, such as 2-arachidonoylglycerol (2-AG), might be an important link between oxidative stress and atherosclerosis. We hypothesized that 2-AG biosynthesis in macrophages is enhanced following ligation of oxidized LDL by scavenger receptors via a signal transduction pathway involving Nox-derived ROS that activates diacylglycerol lipase-β (DAGL-β), the 2-AG biosynthetic enzyme...
December 1, 2016: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/27778288/competitive-abpp-of-serine-hydrolases-a-case-study-on-dagl-alpha
#6
Marc P Baggelaar, Mario Van der Stelt
Competitive activity-based protein profiling is a highly efficient chemical biology technique to determine target engagement and selectivity profiles of enzyme inhibitors in complex proteomes. Fluorophosphonate-based fluorescent inhibitors are widely used as broad-spectrum probes for serine hydrolases. However, diacylglycerol lipase-α is not labeled by fluorophosphonate-based probes. To overcome this problem, we have developed a tailor-made activity-based probe that reacts with diacylglycerol lipase-α. Here we describe a case study in which we apply competitive activity-based protein profiling using a broad-spectrum and a tailor-made activity-based probe to establish selectivity and activity profiles of inhibitors targeting diacylglycerol lipase-α in the mouse brain proteome...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27766867/therapeutic-potential-of-fatty-acid-amide-hydrolase-monoacylglycerol-lipase-and-n-acylethanolamine-acid-amidase-inhibitors
#7
Wei Tuo, Natascha Leleu-Chavain, John Spencer, Supojjanee Sansook, Regis Millet, Philippe Chavatte
Fatty acid ethanolamides (FAEs) and endocannabinoids (ECs) have been shown to alleviate pain and inflammation, regulate motility and appetite, and produce anti-cancer, anxiolytic, and neuroprotective efficacies via cannabinoid receptor type 1 (CB1) or type 2 (CB2), or via peroxisome proliferator-activated receptor α (PPAR-α) stimulation. FAEs and ECs are synthesized by a series of endogenous enzymes, including N-acylphosphatidylethanolamine-phospholipase D (NAPE-PLD), diacylglycerol lipase (DAGL), or phospholipase C (PLC), and their metabolism is mediated by several metabolic enzymes, including fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), N-acylethanolamine acid amidase (NAAA), or cyclooxygenase-2 (COX-2)...
October 21, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27552286/fabp1-a-novel-hepatic-endocannabinoid-and-cannabinoid-binding-protein
#8
Huan Huang, Avery L McIntosh, Gregory G Martin, Danilo Landrock, Sarah Chung, Kerstin K Landrock, Lawrence J Dangott, Shengrong Li, Ann B Kier, Friedhelm Schroeder
Endocannabinoids (ECs) and cannabinoids are very lipophilic molecules requiring the presence of cytosolic binding proteins that chaperone these molecules to intracellular targets. While three different fatty acid binding proteins (FABP3, -5, and -7) serve this function in brain, relatively little is known about how such hydrophobic ECs and cannabinoids are transported within the liver. The most prominent hepatic FABP, liver fatty acid binding protein (FABP1 or L-FABP), has high affinity for arachidonic acid (ARA) and ARA-CoA, suggesting that FABP1 may also bind ARA-derived ECs (AEA and 2-AG)...
September 20, 2016: Biochemistry
https://www.readbyqxmd.com/read/27516570/metabolism-of-endocannabinoids
#9
Michał Biernacki, Elżbieta Skrzydlewska
Endocannabinoids belong to a group of ester, ether and amide derivatives of fatty acids, which are endogenous ligands of receptors CB1, CB2, TRPV1 and GPR55 that are included in the endocannabinoid system of the animal organism. The best known endocannabinoids are: N-arachidonylethanolamide called anandamide (AEA) and 2-arachidonoylglycerol (2-AG). They occur in all organisms, and their highest level is observed in the brain. In this review the mechanisms of synthesis and degradation of both AEA and 2-AG are shown...
August 11, 2016: Postȩpy Higieny i Medycyny Doświadczalnej
https://www.readbyqxmd.com/read/27448020/orexins-contribute-to-restraint-stress-induced-cocaine-relapse-by-endocannabinoid-mediated-disinhibition-of-dopaminergic-neurons
#10
Li-Wei Tung, Guan-Ling Lu, Yen-Hsien Lee, Lung Yu, Hsin-Jung Lee, Emma Leishman, Heather Bradshaw, Ling-Ling Hwang, Ming-Shiu Hung, Ken Mackie, Andreas Zimmer, Lih-Chu Chiou
Orexins are associated with drug relapse in rodents. Here, we show that acute restraint stress in mice activates lateral hypothalamic (LH) orexin neurons, increases levels of orexin A and 2-arachidonoylglycerol (2-AG) in the ventral tegmental area (VTA), and reinstates extinguished cocaine-conditioned place preference (CPP). This stress-induced reinstatement of cocaine CPP depends on type 1 orexin receptors (OX1Rs), type 1 cannabinoid receptors (CB1Rs) and diacylglycerol lipase (DAGL) in the VTA. In dopaminergic neurons of VTA slices, orexin A presynaptically inhibits GABAergic transmission...
2016: Nature Communications
https://www.readbyqxmd.com/read/27394666/inhibitors-of-diacylglycerol-lipases-in-neurodegenerative-and-metabolic-disorders
#11
REVIEW
Freek J Janssen, Mario van der Stelt
2-Arachidonoylglycerol (2-AG) is an endocannabinoid that activates the cannabinoid receptors type 1 and 2. It also serves as an important lipid precursor for the eicosanoid signaling pathway. Consequently, 2-AG is involved in many physiological functions, including anxiety, food intake, inflammation, memory, pain sensation and neurotransmission. Diacylglycerol lipases (DAGLs) are the main biosynthetic enzymes for 2-AG and their role in several pathophysiological conditions is currently under investigation. In this Digest we review all DAGL inhibitors reported to date and their effects in preclinical models of neurodegeneration and metabolic disorders...
August 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27355428/age-related-changes-in-retinoic-docosahexaenoic-and-arachidonic-acid-modulation-in-nuclear-lipid-metabolism
#12
Virginia L Gaveglio, Ana C Pascual, Norma M Giusto, Susana J Pasquaré
The aim of this work was to study how age-related changes could modify several enzymatic activities that regulate lipid mediator levels in nuclei from rat cerebellum and how these changes are modulated by all-trans retinoic acid (RA), docosahexaenoic acid (DHA) and arachidonic acid (AA). The higher phosphatidate phosphohydrolase activity and lower diacylglycerol lipase (DAGL) activity observed in aged animals compared with adults could augment diacylglycerol (DAG) availability in the former. Additionally, monoacylglycerol (MAG) availability could be high due to an increase in lysophosphatidate phosphohydrolase (LPAPase) activity and a decrease in monocylglycerol lipase activity...
August 15, 2016: Archives of Biochemistry and Biophysics
https://www.readbyqxmd.com/read/27344223/genetic-modifiers-of-patent-ductus-arteriosus-in-term-infants
#13
Priti M Patel, Allison M Momany, Kendra L Schaa, Paul A Romitti, Charlotte Druschel, Margaret E Cooper, Mary L Marazita, Jeffrey C Murray, John M Dagle
OBJECTIVE: To identify single-nucleotide polymorphisms (SNPs) in specific candidate genes associated with patent ductus arteriosus in term infants. STUDY DESIGN: We conducted an initial family-based, candidate gene study to analyze genotype data from DNA samples obtained from 171 term infants and their parents enrolled in the National Birth Defects Prevention Study (NBDPS). We performed transmission disequilibrium testing (TDT) using a panel of 55 SNPs in 17 genes...
September 2016: Journal of Pediatrics
https://www.readbyqxmd.com/read/27327781/the-endocannabinoid-system-in-the-baboon-papio-spp-as-a-complex-framework-for-developmental-pharmacology
#14
Iram P Rodriguez-Sanchez, Josee Guindon, Marco Ruiz, M Elizabeth Tejero, Gene Hubbard, Laura E Martinez-de-Villarreal, Hugo A Barrera-Saldaña, Edward J Dick, Anthony G Comuzzie, Natalia E Schlabritz-Loutsevitch
INTRODUCTION: The consumption of marijuana (exogenous cannabinoid) almost doubled in adults during last decade. Consumption of exogenous cannabinoids interferes with the endogenous cannabinoid (or "endocannabinoid" (eCB)) system (ECS), which comprises N-arachidonylethanolamide (anandamide, AEA), 2-arachidonoyl glycerol (2-AG), endocannabinoid receptors (cannabinoid receptors 1 and 2 (CB1R and CB2R), encoded by CNR1 and CNR2, respectively), and synthesizing/degrading enzymes (FAAH, fatty-acid amide hydrolase; MAGL, monoacylglycerol lipase; DAGL-α, diacylglycerol lipase-alpha)...
November 2016: Neurotoxicology and Teratology
https://www.readbyqxmd.com/read/27245901/assay-of-dagl%C3%AE-%C3%AE-activity
#15
Tiziana Bisogno
The endocannabinoid 2-arachidonoylglycerol (2-AG) exerts its physiological action by binding to and functionally activating type-1 (CB1) and type-2 (CB2) cannabinoid receptors. It is thought to be produced through the action of sn-1 selective diacylglycerol lipase (DAGL) that catalyzes 2-AG biosynthesis from sn-2-arachidonate-containing diacylglycerols. Since 2-AG biosynthetic enzymes have been identified only recently, little information on methodological approaches for measuring DAGL activity is as yet available...
2016: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27167970/fabp-1-gene-ablation-impacts-brain-endocannabinoid-system-in-male-mice
#16
Gregory G Martin, Sarah Chung, Danilo Landrock, Kerstin K Landrock, Huan Huang, Lawrence J Dangott, Xiaoxue Peng, Martin Kaczocha, Drew R Seeger, Eric J Murphy, Mikhail Y Golovko, Ann B Kier, Friedhelm Schroeder
Liver fatty acid-binding protein (FABP1, L-FABP) has high affinity for and enhances uptake of arachidonic acid (ARA, C20:4, n-6) which, when esterified to phospholipids, is the requisite precursor for synthesis of endocannabinoids (EC) such as arachidonoylethanolamide (AEA) and 2-arachidonoylglycerol (2-AG). The brain derives most of its ARA from plasma, taking up ARA and transporting it intracellularly via cytosolic fatty acid-binding proteins (FABPs 3,5, and 7) localized within the brain. In contrast, the much more prevalent cytosolic FABP1 is not detectable in the brain but is instead highly expressed in the liver...
August 2016: Journal of Neurochemistry
https://www.readbyqxmd.com/read/27130217/quality-of-ehr-data-extractions-for-studies-of-preterm-birth-in-a-tertiary-care-center-guidelines-for-obtaining-reliable-data
#17
Lindsey A Knake, Monika Ahuja, Erin L McDonald, Kelli K Ryckman, Nancy Weathers, Todd Burstain, John M Dagle, Jeffrey C Murray, Prakash Nadkarni
BACKGROUND: The use of Electronic Health Records (EHR) has increased significantly in the past 15 years. This study compares electronic vs. manual data abstractions from an EHR for accuracy. While the dataset is limited to preterm birth data, our work is generally applicable. We enumerate challenges to reliable extraction, and state guidelines to maximize reliability. METHODS: An Epic™ EHR data extraction of structured data values from 1,772 neonatal records born between the years 2001-2011 was performed...
2016: BMC Pediatrics
https://www.readbyqxmd.com/read/27115711/assay-and-inhibition-of-the-purified-catalytic-domain-of-diacylglycerol-lipase-beta
#18
Praveen K Singh, Rachel Markwick, Leanne Lu, Fiona V Howell, Gareth Williams, Patrick Doherty
The diacylglycerol lipases (DAGLα and DAGLβ) hydrolyze DAG to generate 2-arachidonoylglycerol (2-AG), the principal endocannabinoid and main precursor of arachidonic acid (AA). The DAGLs make distinct tissue specific contributions toward 2-AG and AA levels, and therefore, selective modulators for these enzymes could play crucial roles toward harnessing their therapeutic potential. Relatively high-throughput assays have recently been reported for DAGLα and have proven useful toward the characterization of inhibitors of this enzyme...
May 17, 2016: Biochemistry
https://www.readbyqxmd.com/read/27114924/prolonged-activation-of-human-islet-cannabinoid-receptors-in-vitro-induces-adaptation-but-not-dysfunction
#19
Alonso Vilches-Flores, Zara Franklin, Astrid C Hauge-Evans, Bo Liu, Guo C Huang, Pratik Choudhary, Peter M Jones, Shanta J Persaud
BACKGROUND: Although in vivo studies have implicated endocannabinoids in metabolic dysfunction, little is known about direct, chronic activation of the endocannabinoid system (ECS) in human islets. Therefore, this study investigated the effects of prolonged exposure to cannabinoid agonists on human islet gene expression and function. METHODS: Human islets were maintained for 2 and 5 days in the absence or presence of CB1r (ACEA) or CB2r (JWH015) agonists. Gene expression was quantified by RT-PCR, hormone levels by radioimmunoassay and apoptosis by caspase activities...
June 2016: BBA Clinical
https://www.readbyqxmd.com/read/27057735/peripherally-inserted-central-catheters-optimize-nutrient-intake-in-moderately-preterm-infants
#20
Anne L Smazal, Anne B Kavars, Susan J Carlson, Tarah T Colaizy, John M Dagle
BACKGROUND: While very preterm (<32 wk gestation) infants are routinely provided intensive nutritional support via central line, clinical practice varies for nutrient delivery in infants born moderately preterm (32-34 wk gestation). We sought to define the impact of nutritional support via peripherally inserted central catheter (PICC) on nutrient delivery in the first 2 wk of life and growth by discharge. METHODS: Data were extracted from the records of 187 infants born between 32 and 34 6/7 wk gestation and admitted to the University of Iowa Children's Hospital between April 2012 and December 2013...
2016: Pediatric Research
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