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https://www.readbyqxmd.com/read/28731719/discovery-structure-activity-relationship-and-binding-mode-of-imidazo-1-2-a-pyridine-series-of-autotaxin-inhibitors
#1
Agnès Joncour, Nicolas Desroy, Christopher Housseman, Xavier Bock, Natacha Bienvenu, Laëtitia Cherel, Virginie Labeguere, Christophe Peixoto, Denis Annoot, Luce Lepissier, Jörg Heiermann, Willem Jan Hengeveld, Gregor Pilzak, Alain Monjardet, Emanuelle Wakselman, Veronique Roncoroni, Sandrine Le Tallec, René Galien, Christelle David, Nele Vandervoort, Thierry Christophe, Katja Conrath, Mia Jans, Alexandre Wohlkonig, Robert Touitou, Damien Fleury, Lionel Vercheval, Patrick Mollat, Nicolas Triballeau, Ellen Van der Aar, Reginald Brys, Bertrand Heckmann
Autotaxin (ATX) is a secreted enzyme playing a major role in the production of lysophosphatidic acid (LPA) in blood through hydrolysis of lysophosphatidyl choline (LPC). The ATX-LPA signaling axis arouses a high interest in the drug discovery industry as it has been implicated in several diseases including cancer, fibrotic diseases and inflammation among others. An imidazo[1,2-a]pyridine series of ATX inhibitors was identified out of a high throughput screening (HTS). A co-crystal structure with one of these compounds and ATX revealed a novel binding mode with occupancy of the hydrophobic pocket and channel of ATX but no interaction with zinc ions of the catalytic site...
July 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28716732/lysophosphatidic-acid-signaling-regulates-the-klf9-ppar%C3%AE-axis-in-human-induced-pluripotent-stem-cell-derived-neurons
#2
Tamotsu Tsukahara, Shuhei Yamagishi, Yoshikazu Matsuda, Hisao Haniu
Lysophosphatidic acid (LPA) is a lipid signaling molecule that plays several significant roles in the nervous system during development and injury. In this study, we differentiated human induced pluripotent stem cells (iPSCs) into neurons as an in vitro model to examine the specific effects of LPA. We demonstrated that LPA activates peroxisome proliferator-activated receptor gamma (PPARγ), a ligand-activated nuclear receptor, as well as its cognate receptor LPA1 on human iPSC-derived neurons to enhance proliferation and neurite outgrowth...
July 14, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28716620/distinct-physical-function-profiles-in-older-adults-receiving-cancer-chemotherapy
#3
Christine Miaskowski, Melisa L Wong, Bruce A Cooper, Judy Mastick, Steven M Paul, Katherine Possin, Michael Steinman, Janine Cataldo, Laura B Dunn, Christine Ritchie
CONTEXT: While physical function is an important patient outcome, little is known about changes in physical function in older adults receiving chemotherapy (CTX). OBJECTIVES: Identify subgroups of older patients based on changes in their level of physical function; determine which demographic and clinical characteristics were associated with subgroup membership; and determine if these subgroups differed on quality of life (QOL) outcomes. METHODS: Latent profile analysis (LPA) was used to identify groups of older oncology patients (n=363) with distinct physical function profiles...
July 14, 2017: Journal of Pain and Symptom Management
https://www.readbyqxmd.com/read/28714905/effects-of-eicosapentaenoic-acid-epa-and-docosahexaenoic-acid-dha-on-fetal-pulmonary-circulation-an-experimental-study-in-fetal-lambs
#4
Dyuti Sharma, Estelle Aubry, Thavarak Ouk, Ali Houeijeh, Véronique Houfflin-Debarge, Rémi Besson, Philippe Deruelle, Laurent Storme
Background: Persistent pulmonary hypertension of the newborn (PPHN) causes significant morbidity and mortality in neonates. n-3 Poly-unsaturated fatty acids have vasodilatory properties in the perinatal lung. We studied the circulatory effects of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in fetal sheep and in fetal pulmonary arterial rings. Methods: At 128 days of gestation, catheters were placed surgically in fetal systemic and pulmonary circulation, and a Doppler probe around the left pulmonary artery (LPA)...
July 16, 2017: Nutrients
https://www.readbyqxmd.com/read/28709689/psychiatric-reactions-to-continuous-traumatic-stress-a-latent-profile-analysis-of-two-israeli-samples
#5
Liat Itzhaky, Mark Gelkopf, Yafit Levin, Jacob Y Stein, Zahava Solomon
Many individuals worldwide are exposed to continuous traumatic stress (CTS). However, the psychiatric sequela of CTS and the relevance of posttraumatic stress disorder (PTSD) diagnostic criteria in this situation have yet to be determined. Filling this gap, the present study assessed psychiatric reactions to CTS and the relationship between such reactions and functional impairment among two representative samples of adults exposed to ongoing shelling over 6 (n=387) and 9 years (n=468). Assessment included PTSD symptomatology (i...
June 29, 2017: Journal of Anxiety Disorders
https://www.readbyqxmd.com/read/28709491/band-pattern-analysis-of-mutations-in-rifampicin-resistance-strain-of-mycobacterium-tuberculosis-by-line-probe-assay-in-patients-from-delhi-india
#6
Himanshu Vashistha, M Hanif, K K Chopra, Ashwani Khanna, Divya Shrivastava
BACKGROUND: The GenoType MTBDRplus, a commercial Line Probe Assay (LPA) kit from Hain Lifescience, Germany, is endorsed by India's RNTCP Program for diagnosis of DRTB cases among smear-positive sputum samples. Although the LPA has been studied in several laboratories, there is a wide variation in existing M. tuberculosis strains across the globe, and false results can occur due to the presence of unique genetic mutations in different settings. AIM AND OBJECTIVE: An attempt was made to carry out band pattern analysis using LPA and also to observe uncommon mutations in MDR strains...
July 2017: Indian Journal of Tuberculosis
https://www.readbyqxmd.com/read/28709486/diagnosis-of-tuberculous-meningitis-current-scenario-from-a-tertiary-neurocare-centre-in-india
#7
Jyothi Embekkat Kaviyil, Raju Ravikumar
BACKGROUND: Tuberculous meningitis (TBM) is a condition that is caused by Mycobacterium tuberculosis complex and is difficult to diagnose due to the nonspecificity of the presentations. The study analyzed the different modes of diagnosis available in a developing country set up over a period of five years to understand the diagnostic values of the current conventional and automated methods of diagnosis of TBM among the patients suspected with chronic meningitis. METHODS: A total of 10,281 cerebrospinal fluid samples (CSF) were collected from suspected chronic meningitis patients, of which 790 samples were from individuals who had clinically suspected TBM...
July 2017: Indian Journal of Tuberculosis
https://www.readbyqxmd.com/read/28708504/study-of-lysophosphatidic-acid-receptors-lpars-in-buffalo-uterus-demonstrated-upregulation-of-lpar1-and-lpar6-in-early-pregnancy
#8
Abdul Sadam, Subhashree Parida, Amol R Padol, Ankita D Verma, Naseer Ahmad Baba, Wanta M Khuman, Vivek Srivastava, Manjit Panigrahi, Thakur Uttam Singh, Souvendra Nath Sarkar
Lysophosphatidic acid (LPA) is an important factor involved in embryo implantation and pregnancy establishment in humans and domestic livestock. LPA exerts its action through six G-protein-coupled receptors (LPA1-LPA6). We investigated the types of LPA receptors expressed in buffalo uterus and also their differential expression in the nonpregnant, and early-pregnant endometrium. The nonpregnant, and early-pregnant (<42 days) uteri were collected from the local slaughterhouse. RT-PCR experiments detected mRNAs of all the six LPA receptors (LPAR1-LPAR6) in both nonpregnant, and early-pregnant endometrial tissues...
May 27, 2017: Theriogenology
https://www.readbyqxmd.com/read/28705936/cd14-is-a-key-mediator-of-both-lysophosphatidic-acid-and-lipopolysaccharide-induction-of-foam-cell-formation
#9
Dong An, Feng Hao, Fuqiang Zhang, Wei Kong, Jerold Chun, Xuemin Xu, Mei-Zhen Cui
Macrophage uptake of oxidized lowdensity lipoprotein (oxLDL) plays an important role in foam cell formation and the pathogenesis of atherosclerosis. We report here that lysophosphatidic acid (LPA) enhances lipopolysaccharide (LPS)-induced oxLDL uptake in macrophages. Our data revealed that both LPA and LPS highly induce the CD14 expression at messenger RNA and protein levels in macrophages. The role of CD14, one component of the LPS receptor cluster, in LPA-induced biological functions has been unknown. We took several steps to examine the role of CD14 in LPA signaling pathways...
July 13, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28705542/effect-of-coronary-artery-disease-risk-snps-on-serum-cytokine-levels-and-cytokine-imbalance-in-premature-coronary-artery-disease
#10
Wafa M Ansari, Steve E Humphries, Abdul K Naveed, Omer J Khan, Dilshad A Khan, Ejaz Hassan Khattak
BACKGROUND: Premature Coronary Artery Disease (PCAD) occurs almost a decade earlier in the South Asian population as compared to the West. Inclusion of genetic information can prove to be a robust measure to improve early risk prediction of PCAD. Aim was to estimate the genotypic distribution and risk allele frequencies of 13 Coronary Artery Disease (CAD) risk Single Nucleotide Polymorphisms in loci identified by the CARDIoGRAMplusC4D consortium namely MIA3 rs17465637; 9p21 rs10757274; CXCL12 rs1746048; APOA5 rs662799; APOB rs1042031; LPA rs3798220; LPA 10455872; MRAS rs9818870; LPL rs328; SORT1 rs646776; PCSK9 rs11591147; APOE rs429358; APOE rs7412 in Pakistani PCAD patients and controls...
July 10, 2017: Cytokine
https://www.readbyqxmd.com/read/28703125/flat-clathrin-lattices-are-dynamic-actin-controlled-hubs-for-clathrin-mediated-endocytosis-and-signalling-of-specific-receptors
#11
Daniela Leyton-Puig, Tadamoto Isogai, Elisabetta Argenzio, Bram van den Broek, Jeffrey Klarenbeek, Hans Janssen, Kees Jalink, Metello Innocenti
Clathrin lattices at the plasma membrane coat both invaginated and flat regions forming clathrin-coated pits and clathrin plaques, respectively. The function and regulation of clathrin-coated pits in endocytosis are well understood but clathrin plaques remain enigmatic nanodomains. Here we use super-resolution microscopy, molecular genetics and cell biology to show that clathrin plaques contain the machinery for clathrin-mediated endocytosis and cell adhesion, and associate with both clathrin-coated pits and filamentous actin...
July 13, 2017: Nature Communications
https://www.readbyqxmd.com/read/28701605/role-of-transesophageal-echocardiography-in-surgical-retrieval-of-embolized-amplatzer-device-and-closure-of-coronary-cameral-fistula
#12
Bhupesh Kumar, Alok Kumar, Ganesh Kumar, Harkant Singh
Congenital coronary artery fistula is an uncommon anomaly. Transcatheter coil embolization or Amplatzer vascular plug device closure of fistula is often done in symptomatic patients with safe accessibility to the feeding coronary artery. Embolization of Amplatzer vascular plug device is rare. We report an 11-year-old male child who presented to us with increasing shortness of breath for 7 years. He had a history of Amplatzer vascular plug device closure of right coronary-cameral fistula 8 years back. Echocardiography demonstrated a dilated aneurysmal right coronary artery with turbulent jet entering into the right ventricle (RV) and device embolized into the left pulmonary artery (LPA)...
July 2017: Annals of Cardiac Anaesthesia
https://www.readbyqxmd.com/read/28699486/stress-depression-resilience-and-ageing-a-role-for-the-lpa-lpa1-pathway
#13
Moreno-Fernández Román D, Tabbai Sara, Castilla-Ortega Estela, Pérez-Martín Margarita, Estivill-Torrús Guillermo, Rodríguez de Fonseca Fernando, Santín Luis J, Pedraza Carmen
BACKGROUND: Chronic stress affects health and the quality of life, with its effects being particularly relevant in ageing due to the psychobiological characteristics of this population. However, while some people develop psychiatric disorders, especially depression, others seem very capable of dealing with adversity. There is no doubt that along with the identification of neurobiological mechanisms involved in developing depression, discovering which factors are involved in positive adaptation under circumstances of extreme difficulty will be crucial for promoting resilience...
July 10, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28687529/design-synthesis-and-biological-evaluation-of-2-4-dihydropyrano-2-3-c-pyrazole-derivatives-as-autotaxin-inhibitors
#14
Tatu Pantsar, Prosanta Singha, Tapio J Nevalainen, Igor Koshevoy, Jukka Leppänen, Antti Poso, Juha M A Niskanen, Sanna Pasonen-Seppänen, Juha R Savinainen, Tuomo Laitinen, Jarmo T Laitinen
Inhibition of Autotaxin (ATX) is a potential treatment strategy for several diseases, including tumors with elevated ATX-lysophosphatidic acid (LPA) signaling. Combining structure-based virtual screening together with hen egg-white Autotaxin (ewATX) activity assays enabled the discovery of novel small-molecule ATX inhibitors with a 2,4-dihydropyrano[2,3-c]pyrazole scaffold. These compounds are suggested to bind to the lipophilic pocket, leaving the active site unrestrained. Our most potent compound, (S)-6-amino-4-(3,4-dichlorophenyl)-3-(4-[(4-fluorobenzyl)oxy]phenyl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile [(S)-25], inhibited human ATX (hATX) with an IC50-value of 134nM...
July 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28684865/dynamic-relocalization-of-nherf1-mediates-chemotactic-migration-of-ovarian-cancer-cells-toward-lysophosphatidic-acid-stimulation
#15
Yong-Seok Oh, Kyun Heo, Eung-Kyun Kim, Jin-Hyeok Jang, Sun Sik Bae, Jong Bae Park, Yun Hee Kim, Minseok Song, Sang Ryong Kim, Sung Ho Ryu, In-Hoo Kim, Pann-Ghill Suh
NHERF1/EBP50 (Na(+)/H(+) exchanger regulating factor 1; Ezrin-binding phosphoprotein of 50 kDa) organizes stable protein complexes beneath the apical membrane of polar epithelial cells. By contrast, in cancer cells without any fixed polarity, NHERF1 often localizes in the cytoplasm. The regulation of cytoplasmic NHERF1 and its role in cancer progression remain unclear. In this study, we found that, upon lysophosphatidic acid (LPA) stimulation, cytoplasmic NHERF1 rapidly translocated to the plasma membrane, and subsequently to cortical protrusion structures, of ovarian cancer cells...
July 7, 2017: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/28675901/visual-ratings-of-medial-temporal-lobe-atrophy-correlate-with-csf-tau-indices-in-clinical-variants-of-early-onset-alzheimer-disease
#16
Elias Granadillo, Pongsatorn Paholpak, Mario F Mendez, Edmond Teng
BACKGROUND/AIMS: Prior studies of late-onset Alzheimer disease (AD) have reported that cerebrospinal fluid (CSF) tau levels correlate with hippocampal/medial temporal lobe atrophy. These findings suggest that CSF tau indices in AD may reflect tau-related neurodegeneration in the medial temporal lobe. However, it remains uncertain whether elevated CSF tau levels in the clinically heterogeneous subtypes of early-onset AD (EOAD; amnestic, posterior cortical atrophy [PCA], and logopenic progressive aphasia [LPA]) are attributable to similar underlying mechanisms...
July 5, 2017: Dementia and Geriatric Cognitive Disorders
https://www.readbyqxmd.com/read/28674249/effects-of-gintonin-enriched-fraction-in-an-atopic-dermatitis-animal-model-involvement-of-autotaxin-regulation
#17
Byung-Hwan Lee, Ho-Kyoung Kim, Minhee Jang, Hyeon-Joong Kim, Sun-Hye Choi, Sung-Hee Hwang, Hyoung-Chun Kim, Hyewhon Rhim, Ik-Hyun Cho, Seung-Yeol Nah
Ginseng extract has been used for prevention of atopic dermatitis (AD) in experimental animal models. However, little is known about its active ingredients and the molecular mechanisms underlying its anti-AD effects. Recently, we isolated a unique lysophosphatidic acid (LPA) receptor ligand, gintonin, from ginseng. Gintonin, the glycolipoprotein fraction of ginseng, contains LPAs, mainly LPA C18 : 2 with other minor lysophospholipid components. A line of evidence showed that serum autotaxin (ATX) activity and level are significantly elevated in human AD patients compared to those in normal controls, which indicates that ATX may be involved in human AD...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28671714/significant-differentiation-in-the-apolipoprotein-a-lipoprotein-a-trait-between-chimpanzees-from-western-and-central-africa
#18
Asma Noureen, Claudius Ronke, Mahmoud Khalifa, Michel Halbwax, Anne Fischer, Claudine André, Rebeca Atencia, Rosa Garriga, Lawrence Mugisha, Uta Ceglarek, Joachim Thiery, Gerd Utermann, Konrad Schmidt
Elevated Lipoprotein(a) (Lp(a)) plasma concentrations are a risk factor for cardiovascular disease in humans, largely controlled by the LPA gene encoding apolipoprotein(a) (apo(a)). Lp(a) is composed of low-density lipoprotein (LDL) and apo(a) and restricted to Catarrhini. A variable number of kringle IV (KIV) domains in LPA lead to a size polymorphism of apo(a) that is inversely correlated with Lp(a) concentrations. Smaller apo(a) isoforms and higher Lp(a) levels in central chimpanzees (Pan troglodytes troglodytes [PTT]) compared to humans from Europe had been reported...
July 3, 2017: American Journal of Primatology
https://www.readbyqxmd.com/read/28669075/origin-and-evolution-of-group-xi-secretory-phospholipase-a2-from-flax-linum-usitatissimum-based-on-phylogenetic-analysis-of-conserved-domains
#19
Payal Gupta, Raman Saini, Prasanta K Dash
Phospholipase A2 (PLA2) belongs to class of lipolytic enzymes (EC 3.1.1.4). Lysophosphatidic acid (LPA) and free fatty acids (FFAs) are the products of PLA2 catalyzed hydrolysis of phosphoglycerides at sn-2 position. LPA and FFA that act as second mediators involved in the development and maturation of plants and animals. Mining of flax genome identified two phospholipase A2 encoding genes, viz., LusPLA 2 I and LusPLA 2 II (Linum usitatissimum secretory phospholipase A2). Molecular simulation of LusPLA2s with already characterized plant sPLA2s revealed the presence of conserved motifs and signature domains necessary to classify them as secretory phospholipase A2...
July 2017: 3 Biotech
https://www.readbyqxmd.com/read/28667502/lysophosphatidic-acid-protects-against-endotoxin-induced-acute-kidney-injury
#20
Koryun Mirzoyan, Colette Denis, Audrey Casemayou, Marion Gilet, Dimitri Marsal, Dominique Goudounéche, Stanislas Faguer, Jean-Loup Bascands, Joost P Schanstra, Jean-Sébastien Saulnier-Blache
Septic shock is the most common cause of acute kidney injury (AKI), but the underlying mechanisms remain unclear and no targeted therapies exist. Lysophosphatidic acid (LPA) is a bioactive lipid which in vivo administration was reported to mitigate inflammation and injuries caused by bacterial endotoxemia in the liver and lung. The objective of the present study was to determine whether LPA can protect against sepsis-associated AKI. C57BL/6 mice were treated with LPA 18:1 (5 mg/kg, i.p.) 1 h before being injected with the endotoxin lipopolysaccharide (LPS), and AKI was evaluated after 24 h...
June 30, 2017: Inflammation
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