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https://www.readbyqxmd.com/read/29336874/regioselectivity-of-thiouracil-alkylation-application-to-optimization-of-darapladib-synthesis
#1
Florian Guibbal, Sébastien Bénard, Jessica Patché, Vincent Meneyrol, Joël Couprie, Jennyfer Yong-Sang, Olivier Meilhac, Emmanuelle Jestin
Darapladib is one of the most potent Lp-PLA2 (Lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 0.25 nM. We demonstrate that a crucial step of Darapladib synthesis was not correctly described in the literature, leading to the production of wrong regioisomers. Moreover we show that the inhibitory activity is directly linked to the position on N1 since compounds bearing alkylation on different sites have potentially less interaction within the active site of Lp-PLA2.
December 24, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29332572/lipoprotein-associated-phospholipase-a2-and-coronary-heart-disease
#2
Areti Sofogianni, Stelina Alkagiet, Konstantinos Tziomalos
In the last decades, the role of inflammation in the pathogenesis of atherosclerosis has been the topic of intense research. Several markers of inflammation have shown predictive value for first and recurrent coronary events in patients without and with established coronary heart disease (CHD). Among these markers, lipoprotein-associated phospholipase A2 (Lp-PLA2) has recently received considerable attention. In the present review, the potential role of Lp-PLA2 as a marker of CHD risk and as a therapeutic target is discussed...
January 10, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29321128/measurement-of-lipoprotein-associated-phospholipase-a2-by-use-of-3-different-methods-exploration-of-discordance-between-elisa-and-activity-assays
#3
Celalettin Topbas, Alan Swick, Morteza Razavi, N Leigh Anderson, Terry W Pearson, Cory Bystrom
BACKGROUND: Lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme associated with inflammation, is used as a biomarker for cardiovascular disease risk. Both the concentration and activity of Lp-PLA2 have been shown to be clinically relevant. However, there is a discordance between the serum concentration of Lp-PLA2 measured by the standard ELISA-based immunoassays and the activity of this enzyme, leading to substantial discordance in risk categorization depending on assay format...
January 10, 2018: Clinical Chemistry
https://www.readbyqxmd.com/read/29306475/chronic-inhibition-of-lipoprotein-associated-phospholipase-a2-does-not-improve-coronary-endothelial-function-a-prospective-randomized-controlled-trial
#4
Megha Prasad, Ryan Lennon, Gregory W Barsness, Abhiram Prasad, Rajiv Gulati, Lilach O Lerman, Amir Lerman
AIMS: Lipoprotein-associated phospholipase A2 (Lp-PLA2), a novel biomarker for vascular inflammation, is associated with coronary endothelial dysfunction (CED) and independently predicts cardiovascular events. The current study aimed to determine whether darapladib, an orally administered Lp-PLA2 inhibitor, improved CED. METHODS AND RESULTS: Fifty-four patients with CED were enrolled in a double-blinded randomized placebo-controlled trial, and were randomized to receive oral darapladib, 160mg daily, or placebo...
February 15, 2018: International Journal of Cardiology
https://www.readbyqxmd.com/read/29302464/the-role-of-lp-pla2-and-biochemistry-parameters-as-potential-biomarkers-of-coronary-artery-disease-in-asian-south-indians-a-case-control-study
#5
Sai Giridhar Sairam, Srikanth Sola, Asha Barooah, Sai Kiran Javvaji, Jiten Jaipuria, Vijayalakshmi Venkateshan, Janardhana Chelli, Carani Balaraman Sanjeevi
Background: Coronary artery disease (CAD) is the leading cause of death and disability worldwide. Lipoprotein associated phospholipase A2 (Lp-PLA2) is an emerging biomarker for inflammation that has shown association with CAD. Its significance in the Asian Indian population is not clearly known. We sought to compare the possible association of various biomarkers of atherosclerosis along with Lp-PLA2, in symptomatic individuals with CAD vs. healthy controls in Asian South-Indians. Methods: We conducted a cross-sectional case control study at three centers in a South Indian population...
December 2017: Cardiovascular Diagnosis and Therapy
https://www.readbyqxmd.com/read/29223817/elevated-inflammatory-lp-pla2-and-il-6-link-e-waste-pb-toxicity-to-cardiovascular-risk-factors-in-preschool-children
#6
Xueling Lu, Xijin Xu, Yu Zhang, Yuling Zhang, Chenyang Wang, Xia Huo
Cardiovascular toxicity of lead (Pb) manifests primarily as an effect on blood pressure and eventual increased risk of atherosclerosis and cardiovascular events. Therefore, we investigated vascular inflammatory biomarkers and cardiovascular effects of Pb-exposed children. A total of 590 children (3-7 years old) were recruited from Guiyu (n = 337), an electronic waste (e-waste)-exposed group, and Haojiang (n = 253), a reference group, from November to December 2016. We measured child blood Pb levels (BPbs), and systolic and diastolic blood pressure...
December 7, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/29207826/the-association-between-periodontal-status-serum-lipid-levels-lipoprotein-associated-phosholipase-a2-lp-pla2-in-chronic-periodontitis-subjects-and-healthy-controls
#7
Bittu Saira Koshy, Jaideep Mahendra
Introduction: Lipoprotein associated phospholipase A2 (Lp-PLA2) has been explored as a potential biomarker for Cardiovascular Disease (CVD). The human Lp-PLA2 is a serine-dependent, Ca2+- independent enzyme. It gives way to oxidised free fatty acids and lysophosphatidyl choline by hydrolysing oxidised phospholipids, that leads to smooth muscle cell apoptosis, inflammatory cell chemotaxis and endothelial cell dysfunction in CVD. Owing to its role in inflammation, it may influence the development and progression of periodontitis as well...
September 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/29207392/distinct-roles-of-endothelial-dysfunction-and-inflammation-in-intracranial-atherosclerotic-stroke
#8
Jong-Won Chung, Mi Jeong Oh, Yeon Hee Cho, Gyeong Joon Moon, Gyeong-Moon Kim, Chin-Sang Chung, Kwang Ho Lee, Oh Young Bang
BACKGROUND/AIMS: The aim of the study was to evaluate the differential roles of endothelial dysfunction and inflammation in intracranial atherosclerotic stroke (ICAS). METHODS: We prospectively recruited 262 patients with acute cerebral infarcts caused by ICAS and 75 individuals with no history of stroke as controls. Markers of endothelial dysfunction (asymmetric dimethylarginine, ADMA) and inflammation (lipoprotein-associated phospholipase A2, Lp-PLA2) were measured...
2017: European Neurology
https://www.readbyqxmd.com/read/29201198/comparison-of-the-effect-of-rosuvastatin-versus-rosuvastatin-ezetimibe-on-markers-of-inflammation-in-patients-with-acute-myocardial-infarction
#9
Yizhi Ren, Hao Zhu, Zhongguo Fan, Yali Gao, Nailiang Tian
Statins lower low-density lipoprotein cholesterol (LDL-C) and high-sensitivity C-reactive protein (hsCRP), and the addition of ezetimibe to statins further reduces LDL-C and hsCRP. Lipoprotein-associated phospholipase A2 (Lp-PLA2) is a potentially important pathogenic factor participating in the progression of atherosclerosis. The aim of current study was to investigate how the addition of ezetimibe to rosuvastatin treatment affects reductions in LDL-C, hsCRP and Lp-PLA2 in patients with acute myocardial infarction (AMI)...
November 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29193967/structure-guided-discovery-of-novel-potent-and-orally-bioavailable-inhibitors-of-lipoprotein-associated-phospholipase-a2
#10
Qiufeng Liu, Fubao Huang, Xiao-Jing Yuan, Kai Wang, Yi Zou, Jianhua Shen, Yechun Xu
Lipoprotein-associated phospholipase A2 (Lp-PLA2) is a promising therapeutic target for atherosclerosis, Alzheimer's disease and diabetic macular edema. Here we report the identification of novel sulfonamide scaffold Lp-PLA2 inhibitors derived from a relatively weak fragment. Similarity searching on this fragment followed by molecular docking leads to the discovery of a micromolar inhibitor with 300-fold potency improvement. By the application of a structure-guided design strategy, a successful hit-to-lead optimization was achieved and a number of Lp-PLA2 inhibitors with single-digit nanomolar activity were obtained...
December 1, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29170433/lipoprotein-associated-phospholipase-a2-and-oxidized-low-density-lipoprotein-in-young-patients-with-acute-coronary-syndrome-in-china
#11
Yuli Huang, Yu Wu, You Yang, Wensheng Li, Jianhua Lu, Yunzhao Hu
Lipoprotein-associated phospholipase A2 (Lp-PLA2) is considered to be a risk factor for acute coronary syndrome (ACS), but this remains controversial. This study investigated the role of Lp-PLA2 in young Chinese patients with ACS. 228 young patients (aged ≤55 years) with ACS and 237 age-matched controls were included. Lp-PLA2 and oxidized low-density lipoprotein (ox-LDL) levels were measured by sandwich enzyme-linked immunosorbent assay. Lp-PLA2 levels were significantly correlated with smoking, total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C) and ox-LDL levels (all P < 0...
November 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29169030/lipoprotein-associated-phospholipase-a2-and-risk-of-incident-peripheral-arterial-disease-findings-from-the-atherosclerosis-risk-in-communities-study-aric
#12
Parveen K Garg, Faye L Norby, Linda M Polfus, Eric Boerwinkle, Richard A Gibbs, Megan L Grove, Aaron R Folsom, Pranav S Garimella, Kunihiro Matsushita, Ron C Hoogeveen, Christie M Ballantyne
BACKGROUND AND AIMS: Results from prospective studies evaluating the relationship between elevated lipoprotein-associated phospholipase A2 (Lp-PLA2) activity and incident peripheral arterial disease (PAD) have been mixed. We investigated whether higher Lp-PLA2 levels are associated with increased risk of incident PAD and whether PLA2G7 gene variants, which result in lower Lp-PLA2 levels, are associated with reduced risk of incident PAD. METHODS: Our analysis included 9922 participants (56% female; 21% African-American; mean age 63 years) without baseline PAD at ARIC Visit 4 (1996-1998), who had Lp-PLA2 activity measured and were subsequently followed for the development of PAD, defined by occurrence of a PAD-related hospitalization, through 2012...
November 14, 2017: Atherosclerosis
https://www.readbyqxmd.com/read/29138849/elevated-serum-levels-of-lipoprotein%C3%A2-associated-phospholipase%C3%A2-a2-predict-mortality-rates-in-patients-with-sepsis
#13
Zhongwei Huang, Haiyan Jiang, Xiaohui Cui, Guiwen Liang, Yu Chen, Ting Wang, Zhichao Sun, Lei Qi
Sepsis remains one of the leading contributors to mortality rates in the intensive care unit (ICU) and emergency intensive care unit (EICU). Therefore, any treatments against the agents which produce sepsis in a medical emergency, are welcome. Elevated serum levels of lipoprotein‑associated phospholipase A2 (Lp‑PLA2) have been reported in a small cohort of patients with inflammation. The present study evaluated serum levels of Lp‑PLA2 in patients with sepsis and investigated the role of Lp‑PLA2 in sepsis...
November 13, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29135482/long-term-darapladib-use-does-not-affect-coronary-plaque-composition-assessed-using-multimodality-intravascular-imaging-modalities-a-randomized-controlled-study
#14
Woong Gil Choi, Megha Prasad, Ryan Lennon, Rajiv Gulati, Abhiram Prasad, Lilach O Lerman, Amir Lerman
BACKGROUND: Lipoprotein-associated phospholipase A2 (Lp-PLA2) may play a role in plaque progression and vulnerability. We aimed to define plaque characteristics on multimodality intravascular imaging in patients with coronary endothelial dysfunction in response to long-term inhibition of Lp-PLA2 by darapladib. PATIENTS AND METHODS: This is a double-blinded, randomized study screening 70 patients, and enrolling 54 patients with suspected ischemia, without obstructive disease on angiography and with coronary endothelial dysfunction by invasive assessment...
November 10, 2017: Coronary Artery Disease
https://www.readbyqxmd.com/read/29121808/the-prognostic-value-of-lipoprotein-associated-phospholipase-a2-in-the-long-term-care-of-patients-with-acute-coronary-syndrome-undergoing-percutaneous-coronary-intervention
#15
Lijiao Yang, Hong Wang, Yida Zhang, Tingting Han, Wenfeng Wang
Lipoprotein-associated phospholipase A2 (Lp-PLA2) is an independent risk factor for cardiovascular disease. Accordingly, studies from many countries around the world have shown an association between Lp-PLA2 and cardiovascular events in patients with acute coronary syndrome (ACS) undergoing percutaneous coronary intervention (PCI), but this association has not been documented among the Chinese. The aim of this study was to assess the use of Lp-PLA2 as a useful marker for predicting the long-term prognosis of Chinese patients with ACS undergoing PCI...
January 1, 2017: Clinical and Applied Thrombosis/hemostasis
https://www.readbyqxmd.com/read/29101839/community-based-statins-and-advanced-carotid-plaque-role-of-cd163-positive-macrophages-in-lipoprotein-associated-phospholipase-a2-activity-in-atherosclerotic-plaque
#16
Fumiyuki Otsuka, XiaoQing Zhao, Hugh H Trout, Ye Qiao, Bruce A Wasserman, Masataka Nakano, Colin H Macphee, Martin Brandt, Sue Krug-Gourley, Liang Guo, Elena R Ladich, Qi Cheng, Harry R Davis, Aloke V Finn, Renu Virmani, Frank D Kolodgie
BACKGROUND AND AIMS: Lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzymatic inflammatory biomarker primarily bound to low-density lipoprotein cholesterol, is associated with an approximate twofold increased risk of cardiovascular disease and stroke. Despite indications that circulating Lp-PLA2 is sensitive to statins, it remains largely unknown whether statin usage exerts local effects on Lp-PLA2 expression at the site of atheromatous plaque. METHODS: Carotid plaques (n = 38) were prospectively collected from symptomatic (n = 18) and asymptomatic (n = 20) patients with (n = 20) or without (n = 18) documented statin history...
October 14, 2017: Atherosclerosis
https://www.readbyqxmd.com/read/29051098/impact-of-tyrosine-nitration-at-positions-tyr307-and-tyr335-on-structural-dynamics-of-lipoprotein-associated-phospholipase-a2-a-therapeutically-important-cardiovascular-biomarker-for-atherosclerosis
#17
Arun Bahadur Gurung, Atanu Bhattacharjee
Protein tyrosine nitration (PTN) is a post translational event which results in the generation of 3-Nitrotyrosine (3-NT). High levels of 3-NT were reported in several human diseases such as Parkinson's disease, Alzheimer's disease, amylotrophic lateral sclerosis and coronary artery disease. It was reported that PTN at positions 307 and 335 of Lipoprotein-associated phospholipase A2 (Lp-PLA2) curtails its enzymatic activity but the mechanism of inhibition at the structure level is still incomprehensible. The present study is an in silico endeavor to understand nitrative stress induced structural changes in Lp-PLA2...
October 16, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29027597/lipoprotein-associated-phospholipase-a2-activity-in-obese-adolescents-with-and-without-type-2-diabetes
#18
Julia Seyfarth, Thomas Reinehr, Annika Hoyer, Christina Reinauer, Christina Bächle, Beate Karges, Ertan Mayatepek, Michael Roden, Sabine E Hofer, Susanna Wiegand, Joachim Woelfle, Wieland Kiess, Joachim Rosenbauer, Reinhard W Holl, Thomas Meissner
Lipoprotein-associated phospholipase A2 (Lp-PLA2) was identified as a strong predictor for cardiovascular events. Furthermore, it is highly associated with obesity. The role of Lp-PLA2 in diabetes mellitus is controversial and analyses, especially in adolescents with type 2 diabetes (T2D), are missing. Therefore, we compared Lp-PLA2 activity between two obese age-, sex-, and BMI-matched cohorts of adolescents with and without T2D. Relationships between Lp-PLA2 activity and age, BMI, hemoglobin A1c, lipids, and adipokines were evaluated...
October 13, 2017: Journal of Inherited Metabolic Disease
https://www.readbyqxmd.com/read/28960681/association-of-lp-pla2-g994t-gene-polymorphism-with-risk-of-ischemic-stroke-in-chinese-population
#19
Jing Ni, Hong Gu, Wuhao Hu, Fang Zhou, Xue Zhu, Ke Wang
The association between lipoprotein-associated phospholipase A2 (Lp-PLA2) G994T gene polymorphism and the risk of ischemic stroke is unclear. The aim of this study is to investigate the influence of Lp-PLA2 G994T genetic variant on the pathogenesis of ischemic stroke in Chinese population. A total of 348 patients with a clinical diagnosis of ischemic stroke and 260 gender-matched control subjects under physical examination were recruited from hospitals and genotyped for G994T gene polymorphism. The results showed that there was a significant difference in the genotype distribution between the two groups and people with GT or TT genotype were associated with the higher risk of ischemic stroke even after adjusting the effects of potential confounding factors...
September 28, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28951620/lipoprotein-associated-phospholipase-a2-is-associated-with-risk-of-mild-cognitive-impairment-in-chinese-patients-with-type-2-diabetes
#20
Rongrong Cai, Rong Huang, Jing Han, Haixia Sun, Jie Sun, Wenqing Xia, Sai Tian, Xue Dong, Yanjue Shen, Shaohua Wang
Type 2 diabetes mellitus (T2DM) is a low-grade chronic inflammatory diseases, which have been implicated in the pathogenesis of cognitive decline. We aim to evaluate associations between inflammatory markers and the risk of mild cognitive impairment (MCI) in T2DM. This study of 140 diabetic patients involved 71 with MCI and 69 controls. Clinical parameters, neuropsychological tests, high sensitivity C reactive protein (hsCRP), interleukin-6 (IL-6), lipoprotein-associated Phospholipase A2 (Lp-PLA2) mass and activity were measured...
September 26, 2017: Scientific Reports
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