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N-acyl or cannabinoid or NAPE

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https://www.readbyqxmd.com/read/29656308/bacterial-lipid-modification-of-icp11-and-a-new-elisa-system-applicable-for-wssv-infection-detection
#1
Vidhyapriya Murugan, Krishnan Sankaran
In ELISA, a popular analytical diagnostic tool, the stable non-covalent immobilization (coating) of hydrophilic proteins/peptides on to hydrophobic polystyrene surface has remained a major common challenge. Recombinant bacterial lipid modification of proteins in Escherichia coli system has been shown in this study to solve this problem owing to the hydrophobic anchorage provided by three fatty acyl groups in N-acyl-S-diacylglyceryl Cys at the N-terminus. Exploiting this first post-translational protein engineering, the most abundantly expressed white spot syndrome viral protein ICP11 was lipid-modified and tested as a new target in a new ELISA method useful to shrimp farming...
April 14, 2018: Marine Biotechnology
https://www.readbyqxmd.com/read/29652995/-association-of-polymorphisms-of-nape-pld-and-faah-genes-with-schizophrenia-in-chinese-han-population
#2
Peiru Si, Shulian Liu, Dongxiao Tong, Meijin Cheng, Liwen Wang, Xiaoli Cheng
OBJECTIVE: To assess the association of polymorphisms of N-acyl-phosphatidylethanolamine-phospholipase D (DAPE-PLD) and fatty acid amide hydrolase (FAAH) genes, as well as their interaction, with schizophrenia. METHODS: Polymorphisms of NAPE-PLD rs12540583 and FAAH rs324420, rs2295633, and rs6429600 were determined with PCR - restriction fragment length polymorphism assay and Sanger sequencing. The genotypes of 345 subjects of Han Chinese origin diagnosed with schizophrenia and a 403 controls were compared...
April 10, 2018: Zhonghua Yi Xue Yi Chuan Xue za Zhi, Zhonghua Yixue Yichuanxue Zazhi, Chinese Journal of Medical Genetics
https://www.readbyqxmd.com/read/29652664/alcohol-use-in-adolescence-5-years-admissions-at-a-pediatric-emergency-department
#3
Marlene Rodrigues, Teresa Pontes, Juliana Almeida, Alexandra Estrada, Susana Carvalho
Objective To characterize the profile and pattern of alcohol consumption in adolescents, admitted with acute alcoholic intoxication (AAI) at a pediatric emergency department of North Portugal. Methods Retrospective descriptive study of adolescents aged between 10 and 17 years, admitted with AAI between 2012 and 2016. The following variables were evaluated: age, gender, drinking context, quantity and type of alcohol, Glasgow Coma Scale (GCS), previous episodes, associated injuries, transport to the emergency department, other drug consumption, blood alcohol level (BAL), blood glucose level, treatment and orientation...
April 13, 2018: International Journal of Adolescent Medicine and Health
https://www.readbyqxmd.com/read/29652258/the-crystal-structure-of-the-lipoaminopeptaibol-helioferin-an-antibiotic-peptide-from-mycogone-rosea
#4
Renate Gessmann, Hans Brückner, Albrecht Berg, Kyriacos Petratos
The crystal structure of the natural nonapeptide antibiotic helioferin has been determined and refined to 0.9 Å resolution. Helioferin consists of helioferin A and B, which contain 2-(2'-aminopropyl)aminoethanol (Apae) and 2-[(2'-aminopropyl)methylamino]ethanol (Amae) at their respective alkanolamine termini. In addition, helioferin contains the unusual amino-acid residues α-aminoisobutyric acid (Aib) and (2S,4S,6S)-2-amino-6-hydroxy-4-methyl-8-oxodecanoic acid (Ahmod). The amino-terminus is capped with 2-methyl-n-1-octanoic acid (M8a)...
April 1, 2018: Acta Crystallographica. Section D, Structural Biology
https://www.readbyqxmd.com/read/29652162/php-tethered-n-acyl-carbamate-a-photocage-for-nicotinamide
#5
Farbod Salahi, Vatsal Purohit, Guillermo Ferraudi, Cynthia Stauffacher, Olaf Wiest, Paul Helquist
The synthesis of a new photocaged nicotinamide having an N-acyl carbamate linker and a p-hydroxyphenacyl (pHP) chromophore is described. The photophysical and photochemical studies showed an absorption maximum at λ = 330 nm and a quantum yield for release of 11% that are dependent upon both pH and solvent. While the acyl carbamate releases nicotinamide efficiently, a simpler amide linker was inert to photocleavage. This photocaged nicotinamide has significant advantages with respect to quantum yield, absorbance wavelength, rate of release, and solubility that make it the first practical example of a photocaged amide...
April 13, 2018: Organic Letters
https://www.readbyqxmd.com/read/29652129/decarbonylative-cross-couplings-nickel-catalyzed-functional-group-interconversion-strategies-for-the-construction-of-complex-organic-molecules
#6
Lin Guo, Magnus Rueping
The utilization of carboxylic acid esters as electrophiles in metal-catalyzed cross-coupling reactions is increasingly popular, as environmentally friendly and readily available ester derivatives can be powerful alternatives to the commonly used organohalides. However, key challenges associated with the use of these chemicals remain to be addressed, including the stability of ester substrates and the high energy barrier associated with their oxidative addition to low-valent metal species. Due to recent developments in nickel catalysis that make it easier to perform oxidative additions, chemists have become interested in applying less reactive electrophiles as coupling counterparts in nickel-catalyzed transformations...
April 13, 2018: Accounts of Chemical Research
https://www.readbyqxmd.com/read/29651709/-cannabinoid-therapy-in-practice
#7
REVIEW
T Rasche, D Emmert, C Stieber, M Mücke, R Conrad
BACKGROUND: In recent years, the media and scientists have shown increased interest in cannabis-based drugs. OBJECTIVES: Background information about cannabis-based drugs and their mechanism of action as well as discussion of possible applications as supportive therapy or in palliative medicine, respectively, are presented. MATERIALS AND METHODS: The recent literature was examined and evaluated. RESULTS: In many medical fields, we do not have sufficient evidence for the efficacy of cannabinoids...
April 12, 2018: Der Urologe. Ausg. A
https://www.readbyqxmd.com/read/29650773/cannabinoid-type-1-receptors-are-upregulated-during-acute-activation-of-brown-adipose-tissue
#8
Minna Lahesmaa, Olof Eriksson, Thorsten Gnad, Vesa Oikonen, Marco Bucci, Jussi Hirvonen, Kalle Koskensalo, Jarmo Teuho, Tarja Niemi, Markku Taittonen, Salla Lahdenpohja, Mueez U Din, Merja Haaparanta-Solin, Alexander Pfeifer, Kirsi A Virtanen, Pirjo Nuutila
Activating brown adipose tissue (BAT) could provide a potential approach for the treatment of obesity and metabolic disease in humans. Obesity is associated with up-regulation of the endocannabinoid system, and blocking the cannabinoid type 1 receptor (CB1R) has been shown to cause weight loss and decrease cardiometabolic risk factors. These effects may partly be mediated via increased BAT metabolism, since there is evidence that CB1R antagonism activates BAT in rodents. To investigate the significance of CB1R in BAT function, we quantified the density of CB1R in human and rodent BAT using the positron emission tomography (PET) radioligand [18 F]FMPEP- d 2 , and in parallel measured BAT activation with the glucose analogue [18 F]FDG...
April 12, 2018: Diabetes
https://www.readbyqxmd.com/read/29649720/differential-release-of-cell-signaling-metabolites-by-male-and-female-bovine-embryos-cultured-in-vitro
#9
E Gómez, S Carrocera, D Martin, P Herrero, N Canela, M Muñoz
Male and female early bovine embryos show dimorphic transcription that impacts metabolism. Individual release of metabolites was examined in a 24h single culture medium from Day-6 male and female morulae that developed to Day-7 expanded blastocysts. Embryos were produced in vitro, fertilized with a single bull and cultured in SOFaaci+6  g/L BSA. The embryonic sex was identified (amelogenin gene amplification). Embryos (N = 10 males and N = 10 females) and N = 6 blank samples (i.e. SOFaaci+6  g/L BSA incubated with no embryos) were collected from 3 replicates...
April 5, 2018: Theriogenology
https://www.readbyqxmd.com/read/29649363/a-targeted-differential-top-down-proteomic-methodology-for-comparison-of-apoa-i-proteoforms-in-individuals-with-high-and-low-hdl-efflux-capacity
#10
Henrique Dos Santos Seckler, Luca Fornelli, R Kannan Mutharasan, C Shad Thaxton, Ryan T Fellers, Martha Daviglus, Allan Sniderman, Daniel Rader, Neil L Kelleher, Donald M Lloyd-Jones, Philip D Compton, John T Wilkins
Top-down proteomics (TDP) allows precise determination/characterization of the different proteoforms derived from the expression of a single gene. In this study, we targeted apolipoprotein A-I (ApoA-I), a mediator of high-density-lipoprotein cholesterol efflux (HDL-E), which is inversely associated with coronary heart disease risk. Absolute ApoA-I concentration and allelic variation only partially explain inter-individual HDL-E variation. Therefore, we hypothesize that differences in HDL-E are associated with the abundances of different ApoA-I proteoforms...
April 12, 2018: Journal of Proteome Research
https://www.readbyqxmd.com/read/29648861/an-assessment-of-concurrent-cannabidiol-and-%C3%AE-%C3%A2-tetrahydrocannabinol-administration-in-place-aversion-and-taste-avoidance-conditioning
#11
Briana J Hempel, Matthew M Clasen, Katharine H Nelson, Claudia J Woloshchuk, Anthony L Riley
Rising interest in medical marijuana has prompted research into its phytocannabinoid constituents, particularly Δ⁹-tetrahydrocannabinol (THC) and cannabidiol (CBD). Coadministration of CBD with THC has been shown to modulate a number of THC's effects, including its negative stimulus properties (e.g., anxiety, paranoia, psychosis) in a clinical setting. The present series of experiments extended these analyses by examining the ability of CBD to impact the aversive effects of THC as assessed in a combined taste and place conditioning procedure...
April 2018: Experimental and Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29645334/breslow-intermediates-from-aromatic-n-heterocyclic-carbenes-benzimidazolin-2-ylidenes-thiazolin-2-ylidenes
#12
Albrecht Berkessel, Mathias Paul, Panyapon Sudkaow, Alina Wessels, Nils E Schlörer, Jörg M Neudörfl
We report the first generation and characterization of the elusive Breslow intermediates derived from aromatic N-heterocyclic carbenes (NHCs), namely benzimidazolin-2-ylidenes (NMR, X-ray) and thiazolin-2-ylidenes (NMR). In the former case, the diaminoenols were generated by reaction of the free N,N-bis-Dipp- and N,N-bis-Mes-benzimidazolin-2-ylidenes with aldehydes, while the dimer of 3,4,5-trimethylthiazolin-2-ylidene served as the starting material in the latter case. The unambiguous NMR-identification of the first thiazolin-2-ylidene based Breslow intermediate rests on double 13C labeling of both the NHC and the aldehyde component...
April 12, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29643404/canine-napepld-associated-models-of-human-myelin-disorders
#13
K M Minor, A Letko, D Becker, M Drögemüller, P J J Mandigers, S R Bellekom, P A J Leegwater, Q E M Stassen, K Putschbach, A Fischer, T Flegel, K Matiasek, K J Ekenstedt, E Furrow, E E Patterson, S R Platt, P A Kelly, J P Cassidy, G D Shelton, K Lucot, D L Bannasch, H Martineau, C F Muir, S L Priestnall, D Henke, A Oevermann, V Jagannathan, J R Mickelson, C Drögemüller
Canine leukoencephalomyelopathy (LEMP) is a juvenile-onset neurodegenerative disorder of the CNS white matter currently described in Rottweiler and Leonberger dogs. Genome-wide association study (GWAS) allowed us to map LEMP in a Leonberger cohort to dog chromosome 18. Subsequent whole genome re-sequencing of a Leonberger case enabled the identification of a single private homozygous non-synonymous missense variant located in the highly conserved metallo-beta-lactamase domain of the N-acyl phosphatidylethanolamine phospholipase D (NAPEPLD) gene, encoding an enzyme of the endocannabinoid system...
April 11, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29642559/1-acylamino-alkylphosphonic-acids-alkaline-deacylation
#14
Marek Cypryk, Jozef Drabowicz, Bartlomiej Gostynski, Marcin H Kudzin, Zbigniew H Kudzin, Pawel Urbaniak
The alkaline deacylation of a representative series of 1-(acylamino)alkylphosphonic acids [(AC)-AAP : (AC) = Ac, TFA, Bz; AAP = GlyP , AlaP , ValP , PglP and PheP ] in an aqueous solution of KOH (2M) was investigated. The results suggested a two-stage reaction mechanism with a quick interaction of the hydroxyl ion on the carbonyl function of the amide R-C(O)-N(H)- group in the first stage, which leads to instant formation of the intermediary acyl-hydroxyl adducts of R-C(O- )₂-N(H)-, visible in the 31 P NMR spectra...
April 9, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29627985/strategic-approaches-to-overcome-resistance-against-gram-negative-pathogens-using-%C3%AE-lactamase-inhibitors-and-%C3%AE-lactam-enhancers-the-activity-of-three-novel-diazabicyclooctanes-wck-5153-zidebactam-wck-5107-and-wck-4234
#15
Krisztina M Papp-Wallace, Nhu Q Nguyen, Michael R Jacobs, Christopher R Bethel, Melissa D Barnes, Vijay Kumar, Saralee Bajaksouzian, Susan D Rudin, Philip N Rather, Satish Bhavsar, Tadiparthi Ravikumar, Prasad K Deshpande, Vijay Patil, Ravindra Yeole, Sachin S Bhagwat, Mahesh V Patel, Focco van den Akker, Robert A Bonomo
Limited treatment options exist to combat infections caused by multidrug-resistant (MDR) Gram negative bacteria possessing broad-spectrum β-lactamases. The design of novel β-lactamase inhibitors is of paramount importance. Here, three novel diazabicyclooctanes (DBOs), WCK 5153, zidebactam (WCK 5107), and WCK 4234 (compounds 1-3) were synthesized and biochemically characterized against clinically important bacteria. Compound 3 inhibited class A, C and D β-lactamases with unprecedented k2/K values against OXA carbapenemases...
April 7, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29627825/effect-of-cb1-ligands-on-neurogenic-and-myogenic-contractile-responses-in-the-guinea-pig-ileum
#16
Josef Donnerer, Ingrid Liebmann
This study aimed at investigating whether the synthetic cannabinoid receptor agonist (+)-WIN 55212-2 has neurogenic and myogenic relaxant effects on the longitudinal muscle-myenteric plexus (LMMP) strip of the guinea-pig ileum. (+)-WIN 55212-2, 1-1,000 nmol/L, concentration-dependently inhibited both the electrical stimulation-induced cholinergic twitch responses as well as the myogenic smooth muscle contractions in the LMMP preparation. SR-141716A (rimonabant) 1-1,000 nmol/L, the cannabinoid CB1 receptor antagonist, being without effect on its own, antagonized the (+)-WIN 55212-2-induced effects...
April 6, 2018: Pharmacology
https://www.readbyqxmd.com/read/29626639/assessing-the-real-time-activation-of-the-cannabinoid-cb1-receptor-and-the-associated-structural-changes-using-a-fret-biosensor
#17
Ying Liu, Lu-Yao Chen, Hong Zeng, Richard Ward, Nan Wu, Li Ma, Xi Mu, Qiu-Lan Li, Yang Yang, Su An, Xiao-Xi Guo, Qian Hao, Tian-Rui Xu
The cannabinoid receptor 1 (CB1) is mainly expressed in the nervous system and regulates learning, memory processes, pain and energy metabolism. However, there is no way to directly measure its activation. In this study, we constructed a CB1 intramolecular fluorescence resonance energy transfer (FRET) sensor, which could measure CB1 activation by monitoring structural changes between the third intracellular loop and the C-terminal tail. CB1 agonists induced a time- and concentration-dependent increase in the FRET signal, corresponding to a reduction in the distance between the third intracellular loop and the C-terminal tail...
April 4, 2018: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/29626566/the-antidepressant-like-effects-of-a-novel-curcumin-derivative-j147-involvement-of-5-ht-1a-receptor
#18
Lejing Lian, Ying Xu, Jianbo Zhang, Yingcong Yu, Naping Zhu, Xiaofei Guan, Hui Huang, Ruijie Chen, Jie Chen, Guilan Shi, Jianchun Pan
Depression is a dysthymia disorder characterized by a pervasive or persistent mental disorder that causes mood, cognitive and memory deficits. J147, a curcumin analogue, increases brain derived neurotrophic factor (BDNF) levels and facilitates memory in animals. Because curcumin has the antidepressant-like activity, the present study investigated the potential antidepressant-like effects of J147 in the forced swimming test (FST) and tail suspension tests (TST) and the involvement of 5-HT receptors related to cAMP signaling...
April 4, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29625104/structural-requirement-of-the-hydrophobic-region-of-the-bordetella-pertussis-cyaa-hemolysin-for-functional-association-with-cyac-acyltransferase-in-toxin-acylation
#19
Veerada Raksanoh, Panchika Prangkio, Chompounoot Imtong, Niramon Thamwiriyasati, Kittipong Suvarnapunya, Lalida Shank, Chanan Angsuthanasombat
Previously, we demonstrated that the ∼130-kDa CyaA-hemolysin (CyaA-Hly, Met482 -Arg1706 ) from Bordetella pertussis was palmitoylated at Lys983 when co-expressed with CyaC-acyltransferase in Escherichia coli, and thus activated its hemolytic activity. Here, further investigation on a possible requirement of the N-terminal hydrophobic region (HP, Met482 -Leu750 ) for toxin acylation was performed. The ∼100-kDa RTX (Repeat-in-ToXin) fragment (CyaA-RTX, Ala751 -Arg1706 ) containing the K983 -acylation region (AR, Ala751 -Gln1000 ), but lacking HP, was co-produced with CyaC in E...
April 3, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29624642/cannabidiol-regulates-behavioural-alterations-and-gene-expression-changes-induced-by-spontaneous-cannabinoid-withdrawal
#20
Francisco Navarrete, Auxiliadora Aracil-Fernández, Jorge Manzanares
BACKGROUND AND PURPOSE: Cannabidiol (CBD) represents a promising therapeutic tool for treating cannabis use disorder (CUD). This study aimed to evaluate the effects of CBD on the behavioural and gene expression alterations induced by spontaneous cannabinoid withdrawal. EXPERIMENTAL APPROACH: Spontaneous cannabinoid withdrawal was evaluated 12 h after cessation of CP-55,940 treatment (0.5 mg·kg-1 /12 h; intraperitoneally (i.p.); 7 days) in C57BL/6J mice. The effects of CBD (5, 10 and 20 mg·kg-1 ; i...
April 6, 2018: British Journal of Pharmacology
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