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https://www.readbyqxmd.com/read/28218840/drug-repurposing-of-histone-deacetylase-inhibitors-that-alleviate-neutrophilic-inflammation-in-acute-lung-injury-and-idiopathic-pulmonary-fibrosis-via-inhibiting-leukotriene-a4-hydrolase-and-blocking-ltb4-biosynthesis
#1
Weiqiang Lu, Xue Yao, Ping Ouyang, Ningning Dong, Dang Wu, Xingwu Jiang, Zengrui Wu, Chen Zhang, Zhongyu Xu, Yun Tang, Shien Zou, Mingyao Liu, Jian Li, Ming-Hua Zeng, Ping Lin, Feixiong Cheng, Jin Huang
Acute lung injury (ALI) and idiopathic pulmonary fibrosis (IPF) are both serious public health problems with high incidence and mortality rate in adults, and with few drugs available for the efficient treatment in clinic. In this study, we identified that two known histone deacetylase (HDAC) inhibitors, suberanilohydroxamic acid (SAHA, 1) and its analog 4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide (2), are effective inhibitors of Leukotriene A4 hydrolase (LTA4H), a key enzyme in the biosynthesis of leukotriene B4 (LTB4), across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray Crystallographic investigation...
February 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28074614/mutation-analysis-and-gene-expression-profiling-of-ocular-melanomas-in-cats
#2
J G Rushton, R Ertl, D Klein, B Nell
Feline ocular melanomas show a high malignant behaviour, but adjunctive therapies are non-existent. The aim of this pilot study was to determine, whether feline ocular melanomas harbour mutations comparable to mutations in human melanomas and to evaluate the gene expression status of genes known to be involved in initiation and progression of human melanomas. Mutation hotspot regions of several genes of feline ocular melanomas were analysed by DNA sequencing and RNA expression levels of the respective genes and others were evaluated by quantitative real-time polymerase chain reaction (RT-qPCR)...
January 11, 2017: Veterinary and Comparative Oncology
https://www.readbyqxmd.com/read/28065501/synthesis-docking-cytotoxicity-and-lta4h-inhibitory-activity-of-new-gingerol-derivatives-as-potential-colorectal-cancer-therapy
#3
Mai H El-Naggar, Amira Mira, Fatma M Abdel Bar, Kuniyoshi Shimizu, Mohamed M Amer, Farid A Badria
Leukotriene A4 hydrolase (LTA4H) is a proinflammatory enzyme that generates the inflammatory mediator leukotriene which may play an important role in chronic inflammation associated carcinogenesis. [6]-gingerol, the major bioactive compound of Zingiber officinale, is a potential inhibitor of LTA4H, a highly expressed enzyme in colorectal carcinoma. Eighteen compounds; seven of natural origin (including [4]-, [6]-, [8]-, and [10]-gingerol), five new and six known semi-synthesized [6]-gingerol derivatives were examined using docking, in vitro cytotoxicity against human colon cancer cells (HCT-116) and LTA4H aminopeptidase and epoxide hydrolase inhibitory studies...
December 29, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27990118/cysteinyl-leukotrienes-pathway-genes-atopic-asthma-and-drug-response-from-population-isolates-to-large-genome-wide-association-studies
#4
REVIEW
Miles D Thompson, Valerie Capra, Mark T Clunes, G E Rovati, Jana Stankova, Mary C Maj, David L Duffy
Genetic variants associated with asthma pathogenesis and altered response to drug therapy are discussed. Many studies implicate polymorphisms in genes encoding the enzymes responsible for leukotriene synthesis and intracellular signaling through activation of seven transmembrane domain receptors, such as the cysteinyl leukotriene 1 (CYSLTR1) and 2 (CYSLTR2) receptors. The leukotrienes are polyunsaturated lipoxygenated eicosatetraenoic acids that exhibit a wide range of pharmacological and physiological actions...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27914004/hybrid-receptor-bound-mm-gbsa-per-residue-energy-based-pharmacophore-modelling-enhanced-approach-for-identification-of-selective-lta4h-inhibitors-as-potential-anti-inflammatory-drugs
#5
Patrick Appiah-Kubi, Mahmoud Soliman
Leukotriene A4 hydrolase has been identified as an enzyme with dual anti- and pro-inflammatory role, thus, the conversion of leukotriene to leukotriene B4 in the initiation stage of inflammation and the removal of the chemotactic Pro-Gly-Pro tripeptide. These findings make leukotriene A4 hydrolase an attractive drug target: suggesting an innovative approach towards the identification and design of novel class of compounds that can selectively inhibit leukotriene B4 synthesis while sparing the aminopeptidase activity...
December 2, 2016: Cell Biochemistry and Biophysics
https://www.readbyqxmd.com/read/27856749/in-vivo-amelioration-of-endogenous-antitumor-autoantibodies-via-low-dose-p4n-through-the-lta4h-activin-a-baff-pathway
#6
Yu-Ling Lin, Nu-Man Tsai, Cheng-Hao Hsieh, Shu-Yi Ho, Jung Chang, Hsin-Yi Wu, Ming-Hua Hsu, Chia-Ching Chang, Kuang-Wen Liao, Tiffany L B Jackson, David E Mold, Ru Chih C Huang
Cancer progression is associated with the development of antitumor autoantibodies in patients' sera. Although passive treatment with antitumor antibodies has exhibited remarkable therapeutic efficacy, inhibitory effects on tumor progression by endogenous antitumor autoantibodies (EAAs) have been limited. In this study, we show that P4N, a derivative of the plant lignan nordihydroguaiaretic acid (NDGA), enhanced the production of EAAs and inhibited tumor growth at low noncytotoxic concentrations via its immunoregulatory activity...
November 29, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27761137/selection-of-reliable-reference-genes-for-gene-expression-analysis-under-abiotic-stresses-in-the-desert-biomass-willow-salix-psammophila
#7
Jianbo Li, Huixia Jia, Xiaojiao Han, Jin Zhang, Pei Sun, Mengzhu Lu, Jianjun Hu
Salix psammophila is a desert shrub willow that has extraordinary adaptation to abiotic stresses and plays an important role in maintaining local ecosystems. Moreover, S. psammophila is regarded as a promising biomass feedstock because of its high biomass yields and short rotation coppice cycle. However, few suitable reference genes (RGs) for quantitative real-time polymerase chain reaction (qRT-PCR) constrain the study on normalization of gene expression in S. psammophila until now. Here, we investigated the expression stabilities of 14 candidate RGs across tissue types and under four abiotic stress treatments, including heat, cold, salt, and drought treatments...
2016: Frontiers in Plant Science
https://www.readbyqxmd.com/read/27730172/genetic-regulation-of-expression-of-leukotriene-a4-hydrolase
#8
Tomasz Szul, Peter Castaldi, Michael H Cho, J Edwin Blalock, Amit Gaggar
In chronic inflammatory lung disorders such as chronic obstructive pulmonary disease (COPD), the concurrent organ-specific and systemic inflammatory responses lead to airway remodelling and vascular dysfunction. Although a major common risk factor for COPD, cigarette smoke alone cannot explain the progression of this disease; there is increasing evidence that genetic predisposition also plays a role in COPD susceptibility and progression. A key enzyme in chronic lung inflammation is leukotriene A4 hydrolase (LTA4H)...
January 2016: ERJ Open Research
https://www.readbyqxmd.com/read/27651294/thermodynamic-properties-of-leukotriene-a4-hydrolase-inhibitors
#9
Sandra K Wittmann, Lena Kalinowsky, Jan S Kramer, René Bloecher, Stefan Knapp, Dieter Steinhilber, Denys Pogoryelov, Ewgenij Proschak, Jan Heering
The leukotriene A4 hydrolase (LTA4H) is a bifunctional enzyme, containing a peptidase and a hydrolase activity both activities having opposing functions regulating inflammatory response. The hydrolase activity is responsible for the conversion of leukotriene A4 to pro-inflammatory leukotriene B4, and hence, selective inhibitors of the hydrolase activity are of high pharmacological interest. Here we present the thermodynamic characterization of structurally distinct inhibitors of the LTA4H that occupy different regions of the binding site using different biophysical methods...
November 1, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27643598/role-of-lta4h-polymorphism-in-tuberculosis-associated-immune-reconstitution-inflammatory-syndrome-occurrence-and-clinical-severity-in-patients-infected-with-hiv
#10
Gopalan Narendran, Dhanasekaran Kavitha, Ramesh Karunaianantham, Leonardo Gil-Santana, Jilson L Almeida-Junior, Sirasanambatti Devarajulu Reddy, Marimuthu Makesh Kumar, Haribabu Hemalatha, Nagesh Nalini Jayanthi, Narayanan Ravichandran, Raja Krishnaraja, Angamuthu Prabhakar, Tamizhselvan Manoharan, Lokeswaran Nithyananthan, Gunasundari Arjunan, Mohan Natrajan, Soumya Swaminathan, Bruno B Andrade
BACKGROUND: Paradoxical tuberculosis-associated immune reconstitution inflammatory syndrome (TB-IRIS) is an inflammatory phenomenon complicating HIV management in coincidental tuberculosis (TB) infection, upon immune reconstitution driven by antiretroviral therapy (ART). Leukotriene A4 hydroxylase (LTA4H), an enzyme which converts LTA4 to LTB4, regulates the balance between the anti-inflammatory lipoxins and pro-inflammatory LTB4, with direct implications in TB-driven inflammation. In humans, a single nucleotide polymorphism (SNP) in the LTA4H promoter which regulates its transcriptional activity (rs17525495) has been identified and described to impact clinical severity of TB presentation and response to corticosteroid therapy...
2016: PloS One
https://www.readbyqxmd.com/read/27379098/aerobic-exercise-reduces-asthma-phenotype-by-modulation-of-the-leukotriene-pathway
#11
Ricardo Wesley Alberca-Custódio, Flávia Regina Greiffo, BreAnne MacKenzie, Manoel Carneiro Oliveira-Junior, Adilson Santos Andrade-Sousa, Gustavo Silveira Graudenz, Angela Batista Gomes Santos, Nilsa Regina Damaceno-Rodrigues, Hugo Caire Castro-Faria-Neto, Fernanda Magalhaes Arantes-Costa, Milton De Arruda Martins, Asghar Abbasi, Chin Jia Lin, Marco Idzko, Ana Paula Ligeiro Oliveira, Hinnak Northoff, Rodolfo Paula Vieira
INTRODUCTION: Leukotrienes (LTs) play a central role in asthma. Low- to moderate-intensity aerobic exercise (AE) reduces asthmatic inflammation in clinical studies and in experimental models. This study investigated whether AE attenuates LT pathway activation in an ovalbumin (OVA) model of asthma. METHODS: Sixty-four male, BALB/c mice were distributed into Control, Exercise (Exe), OVA, and OVA + Exe groups. Treadmill training was performed at moderate intensity, 5×/week, 1 h/session for 4 weeks...
2016: Frontiers in Immunology
https://www.readbyqxmd.com/read/27293319/differential-expression-of-inflammation-related-genes-in-children-with-down-syndrome
#12
Cláudia Regina Santos Silva, Joice Matos Biselli-Périco, Bruna Lancia Zampieri, Wilson Araujo Silva, Jorge Estefano Santana de Souza, Matheus Carvalho Bürger, Eny Maria Goloni-Bertollo, Érika Cristina Pavarino
OBJECTIVE: The aim of the study was to investigate the expression patterns of a specific set of genes involved in the inflammation process in children with Down Syndrome (DS) and children without the syndrome (control group) to identify differences that may be related to the immune abnormalities observed in DS individuals. METHOD: RNA samples were obtained from peripheral blood, and gene expression was quantified using the TaqMan® Array Plate Human Inflammation Kit, which facilitated the investigation into 92 inflammation-related genes and four reference genes using real-time polymerase chain reaction (qPCR)...
2016: Mediators of Inflammation
https://www.readbyqxmd.com/read/27232150/ultrapressure-liquid-chromatography-tandem-mass-spectrometry-assay-using-atmospheric-pressure-photoionization-uplc-appi-ms-ms-for-quantification-of-4-methoxydiphenylmethane-in-pharmacokinetic-evaluation
#13
Nashid Farhan, Sean Fitzpatrick, Yun M Shim, Mikell Paige, Diana Shu-Lian Chow
4-Methoxydiphenylmethane (4-MDM), a selective augmenter of Leukotriene A4 Hydrolase (LTA4H), is a new anti-inflammatory compound for potential treatment of chronic obstructive pulmonary disease (COPD). Currently, there is no liquid chromatography tandem mass spectrometric (LC-MS/MS) method for the quantification of 4-MDM. A major barrier for developing the LC-MS/MS method is the inability of electrospray ionization (ESI) and atmospheric pressure chemical ionization (APCI) to ionize 4-MDM due to its hydrophobicity and lack of any functional group for ionization...
September 5, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27187064/corpus-luteum-as-a-novel-target-of-weight-changes-that-contribute-to-impaired-female-reproductive-physiology-and-function
#14
Satu Kuokkanen, Alex J Polotsky, Justin Chosich, Andrew P Bradford, Anna Jasinska, Tzu Phang, Nanette Santoro, Susan E Appt
UNLABELLED: Obesity and malnutrition are associated with decreased fecundity in women. Impaired reproductive capacity in obese women is often attributed to anovulation. However, obese women with ovulatory cycles also have reduced fertility, but the etiology of their impaired reproduction is only partially understood. Accumulating evidence suggests that obesity directly impairs oocyte and embryo quality as well as endometrial receptivity. In obese women, urinary progesterone metabolite excretion is decreased, but in excess of what can be explained by suppressed gonadotropin secretion, suggesting that apart from its central effect obesity may directly affect progesterone (P4) production...
August 2016: Systems Biology in Reproductive Medicine
https://www.readbyqxmd.com/read/27126280/bufexamac-ameliorates-lps-induced-acute-lung-injury-in-mice-by-targeting-lta4h
#15
Qiang Xiao, Ningning Dong, Xue Yao, Dang Wu, Yanli Lu, Fei Mao, Jin Zhu, Jian Li, Jin Huang, Aifang Chen, Lu Huang, Xuehai Wang, Guangxiao Yang, Guangyuan He, Yong Xu, Weiqiang Lu
Neutrophils play an important role in the occurrence and development of acute lung injury (ALI). Leukotriene B4 (LTB4), a hydrolysis product of epoxide leukotriene A4 (LTA4) catalyzed by LTA4 hydrolase (LTA4H), is one of the most potent chemoattractants for neutrophil. Bufexamac is a drug widely used as an anti-inflammatory agent on the skin, however, the mechanism of action is still not fully understood. In this study, we found bufexamac was capable of specifically inhibiting LTA4H enzymatic activity and revealed the mode of interaction of bufexamac and LTA4H using X-ray crystallography...
2016: Scientific Reports
https://www.readbyqxmd.com/read/26959888/germline-genetics-of-cancer-of-unknown-primary-cup-and-its-specific-subtypes
#16
Kari Hemminki, Bowang Chen, Abhishek Kumar, Olle Melander, Jonas Manjer, Göran Hallmans, Ulrika Pettersson-Kymmer, Claes Ohlsson, Gunnar Folprecht, Harald Löffler, Alwin Krämer, Asta Försti
Cancer of unknown primary site (CUP) is a fatal cancer diagnosed through metastases at various organs. Little is known about germline genetics of CUP which appears worth of a search in view of reported familial associations in CUP. In the present study, samples from CUP patients were identified from 2 Swedish biobanks and a German clinical trial, totaling 578 CUP patients and 7628 regionally matched controls. Diagnostic data specified the organ where metastases were diagnosed. We carried out a genome-wide association study on CUP cases and controls...
April 19, 2016: Oncotarget
https://www.readbyqxmd.com/read/26714527/-study-on-the-association-between-leukotriene-a4-hydrolase-gene-polymorphism-and-ischemic-stroke
#17
Yiqun Wu, Shuai Li, Kuo Liu, Xun Tang, Kai Fang, Na Li, Jin Li, Tao Wu, Dafang Chen, Yonghua Hu
OBJECTIVE: To investigate the association between polymorphism of leukotriene A4 hydrolase (LTA4H) gene among ischemic stroke patients and the related subtypes in the discordant sib pairs. METHODS: Families including ischemic stroke patients and their siblings were recruited. Four single nucleotide polymorphisms (SNPs) of LTA4H as rs2072512, rs2540489, rs2540500 and rs6538697 were selected. Generalized estimating equation (GEE) was used to adjust for in-family correlation in the analysis of discordant sib pairs...
August 2015: Zhonghua Liu Xing Bing Xue za Zhi, Zhonghua Liuxingbingxue Zazhi
https://www.readbyqxmd.com/read/26641739/ustekinumab-in-hidradenitis-suppurativa-clinical-results-and-a-search-for-potential-biomarkers-in-serum
#18
J L Blok, K Li, C Brodmerkel, P Horvátovich, M F Jonkman, B Horváth
BACKGROUND: Treatment of hidradenitis suppurativa (HS) is difficult and the search for effective therapies continues. OBJECTIVES: To evaluate the efficacy of ustekinumab and to discover a potential biomarker for HS. METHODS: Seventeen patients were included in this open-label study and treated with 45 or 90 mg ustekinumab at weeks 0, 4, 16 and 28. Proteomic technology and enzyme-linked assay analysis was applied to sera. RESULTS: Twelve patients completed the protocol...
April 2016: British Journal of Dermatology
https://www.readbyqxmd.com/read/26555301/dual-anti-inflammatory-and-selective-inhibition-mechanism-of-leukotriene-a4-hydrolase-aminopeptidase-insights-from-comparative-molecular-dynamics-and-binding-free-energy-analyses
#19
Patrick Appiah-Kubi, Mahmoud E S Soliman
Human leukotriene A4 hydrolase/aminopeptidase (LTA4H) is a zinc metalloenzyme with a dual catalytic activity; conversion of LTA4 into LTB4 and degradation of chemotactic tripeptide Pro-Gly-Pro (PGP). Existing inhibitors, such as SC-57461A, block both catalytic activities of the enzyme, leading to drug failures. Recently, a novel compound, ARM1, was reported to selectively inhibit the hydrolase activity of LTA4H while sparing its aminopeptidase activity. However, the molecular understanding of such preferential inhibitory mechanism remains obscure...
November 2016: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/26488221/gene-expression-of-proresolving-lipid-mediator-pathways-is-associated-with-clinical-outcomes-in-trauma-patients
#20
Sarah K Orr, Kathryn L Butler, Douglas Hayden, Ronald G Tompkins, Charles N Serhan, Daniel Irimia
OBJECTIVES: Specialized proresolving lipid mediators have emerged as powerful modulators of inflammation and activators of resolution. Animal models show significant benefits of specialized proresolving lipid mediators on survival and wound healing after major burn trauma. To date, no studies have investigated specialized proresolving lipid mediators and their relation to other lipid mediator pathways in humans after trauma. Here we determine if patients with poor outcomes after trauma have dysregulated lipid mediator pathways...
December 2015: Critical Care Medicine
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