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https://www.readbyqxmd.com/read/29227918/synthesis-anti-inflammatory-p38%C3%AE-map-kinase-inhibitory-activities-and-molecular-docking-studies-of-quinoxaline-derivatives-containing-triazole-moiety
#1
Sana Tariq, Ozair Alam, Mohd Amir
A new series of 3-[2-(5-mercapto-4-phenyl-4H-1,2,4-traiazol-3-yl)ethyl] quinoxalin-2(1H)-one (5a-v) derivatives was synthesized and subjected to in vitro evaluation for anti-inflammatory activity (BSA anti-denaturation assay) and p38α MAPK inhibition. Few selected compounds (5a, 5e, 5f, 5g, 5h, 5l, 5q and 5u) were studied for their in vivo anti-inflammatory activity, ulcerogenicity and lipid peroxidation potential. Compounds 5e and 5f were found to be the most active in the series showing 83.45% and 84.15% anti-inflammatory activity respectively when compared to diclofenac sodium (83...
December 2, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29226462/spontaneous-death-of-rat-chloroleukaemia-cells-induced-by-an-endogenous-growth-inhibitor
#2
T Rytömaa, K Grip-Rytömaa
OBJECTIVES: When rat chloroleukaemia (CHL) cells are grown undisturbed in a confined space, a genomic long interspersed nuclear element (LINE) is transcriptionally activated at a relatively low population density, followed by the retrotransposition of LINE and population death. This death programme is fundamentally different from conventional cell death pathways. MATERIALS AND METHODS: This work is essentially based on the re-analysis of relevant, old experimental data...
December 10, 2017: Cell Proliferation
https://www.readbyqxmd.com/read/29226074/characterization-of-auxiliary-iron-sulfur-clusters-in-a-radical-s-adenosylmethionine-enzyme-pqqe-from-methylobacterium-extorquens-am1
#3
Natsaran Saichana, Katsuyuki Tanizawa, Hiroshi Ueno, Jiří Pechoušek, Petr Novák, Jitka Frébortová
PqqE is a radical S-adenosyl-l-methionine (SAM) enzyme that catalyzes the initial reaction of pyrroloquinoline quinone (PQQ) biosynthesis. PqqE belongs to the SPASM (subtilosin/PQQ/anaerobic sulfatase/mycofactocin maturating enzymes) subfamily of the radical SAM superfamily and contains multiple Fe-S clusters. To characterize the Fe-S clusters in PqqE from Methylobacterium extorquens AM1, Cys residues conserved in the N-terminal signature motif (CX 3 CX 2C) and the C-terminal seven-cysteine motif (CX 9-15 GX 4 CX n CX 2 CX 5 CX 3 CX n C; n = an unspecified number) were individually or simultaneously mutated into Ser...
December 2017: FEBS Open Bio
https://www.readbyqxmd.com/read/29225844/hemoglobin-providence-%C3%AE-82-lys-asn-asp-and-lower-than-expected-hba1c-in-a-nonadherent-teenager-with-type-1-diabetes-a-case-report-and-literature-review
#4
Charles N Newman, Christine M Litwin, Deborah A Bowlby, Katherine A Lewis, Remberto C Paulo
Endocrinologists should have a high index of suspicion for a Hb variant when the HbA1c is not consistent with other indices of glycemic control.
December 2017: Clinical Case Reports
https://www.readbyqxmd.com/read/29222424/structural-insight-into-a-ce15-esterase-from-the-marine-bacterial-metagenome
#5
Concetta De Santi, Osman Absm Gani, Ronny Helland, Adele Williamson
The family 15 carbohydrate esterase (CE15) MZ0003, which derives from a marine Arctic metagenome, has a broader substrate scope than other members of this family. Here we report the crystal structure of MZ0003, which reveals that residues comprising the catalytic triad differ from previously-characterized fungal homologs, and resolves three large loop regions that are unique to this bacterial sub-clade. The catalytic triad of the bacterial CE15, which includes Asp 332 as its third member, closely resembles that of family 1 carbohydrate esterases (CE1), despite the overall lower structural similarity with members of this family...
December 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29221796/synthesis-and-antibacterial-activity-of-new-peptides-from-alfalfa-rubisco-protein-hydrolysates-and-mode-of-action-via-a-membrane-damage-mechanism-against-listeria-innocua
#6
Sabrine Kobbi, Naima Nedjar, Nourdine Chihib, Rafik Balti, Mickael Chevalier, Amandine Silvain, Semia Chaabouni, Pascal Dhulster, Ali Bougatef
In this work we evaluated the mode of action of six new synthesized peptides (Met-Asp-Asn; Glu-leu-Ala-Ala-Ala-Cys; Leu-Arg-Asp-Asp-Phe; Gly-Asn-Ala-Pro-Gly-Ala-Val-Ala; Ala-Leu-Arg-Met-Ser-Gly and Arg-Asp-Arg-Phe-Leu), previously identified, from the most active peptide fractions of RuBisCO peptic hydrolysate against Listeria innocua via a membrane damage mechanism. Antibacterial effect and the minimum inhibitory concentrations (MIC) of these peptides were evaluated against six strains and their hemolytic activities towards bovine erythrocytes were determined...
December 5, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29218757/local-and-global-anatomy-of-antibody-protein-antigen-recognition
#7
Meryl Wang, David Zhu, Jianwei Zhu, Ruth Nussinov, Buyong Ma
Deciphering antibody-protein antigen recognition is of fundamental and practical significance. We constructed an antibody structural dataset, partitioned it into human and murine subgroups, and compared it with nonantibody protein-protein complexes. We investigated the physicochemical properties of regions on and away from the antibody-antigen interfaces, including net charge, overall antibody charge distributions, and their potential role in antigen interaction. We observed that amino acid preference in antibody-protein antigen recognition is entropy driven, with residues having low side-chain entropy appearing to compensate for the high backbone entropy in interaction with protein antigens...
December 8, 2017: Journal of Molecular Recognition: JMR
https://www.readbyqxmd.com/read/29217325/protocatechuic-acid-pca-induced-a-better-antiviral-effect-by-immune-enhancement-in-spf-chickens
#8
Yongxia Guo, Qiang Zhang, Zonghui Zuo, Jun Chu, Hongzhi Xiao, M Tariq Javed, Cheng He
Protocatechuic acid (PCA) is an antiviral agent against Avian Influenza virus (AIV) and Infectious Bursal Disease (IBD) virus but its antiviral mechanism is unknown. In this study, we evaluated the humoral and cellular responses to PCA in specific pathogen-free (SPF) chickens. One hundred forty 35-day-old SPF chickens were randomly divided into 7 groups. The birds were inoculated with the commercial, attenuated Newcastle Disease Virus (NDV) vaccine and then received orally with 10, 20 or 40 mg/kg body weight of PCA for 21 days...
December 4, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29217160/interaction-between-gallic-acid-and-asparaginase-to-potentiate-anti-proliferative-effect-on-lymphoblastic-leukemia-cell-line
#9
Zahra Sourani, Hedayatollah Shirzad, Moein Shirzad, Batoul Pourgheysari
BACKGROUND: Treatment of acute lymphoblastic leukemia (ALL) fails in some cases and the side effects cause mortality in certain patients. Gallic acid (GA), a polyhydroxyphenolic compound has biological functions including anti-proliferative properties. The aim of the present study was to investigate the growth inhibition effects of GA in combination with asparaginase (ASP), as a component of combination chemotherapy, in a lymphoblastic leukemia cell line. METHODS: Jurkat cells were incubated with different concentrations of GA with or without ASP...
December 4, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29216400/activity-and-safety-of-crizotinib-in-patients-with-alveolar-soft-part-sarcoma-with-rearrangement-of-tfe3-european-organization-for-research-and-treatment-of-cancer-eortc-phase-2-trial-90101-create
#10
P Schöffski, A Wozniak, B Kasper, S Aamdal, M G Leahy, P Rutkowski, S Bauer, H Gelderblom, A Italiano, L H Lindner, I Hennig, S Strauss, B Zakotnik, A Anthoney, L Albiges, J-Y Blay, P Reichardt, J Sufliarsky, W T A van der Graaf, M Debiec-Rychter, R Sciot, T Van Cann, S Marréaud, T Raveloarivahy, S Collette, S Stacchiotti
Background: Alveolar soft part sarcoma(ASPS) is an orphan malignancy associated with a rearrangement of transcription factor E3(TFE3), leading to abnormal MET gene expression. We prospectively assessed the efficacy and safety of the tyrosine kinase inhibitor(TKI) crizotinib in patients with advanced or metastatic ASPS. Patients and methods: Eligible patients with reference pathology-confirmed ASPS received oral crizotinib 250 mg twice daily. By assessing the presence or absence of a TFE3 rearrangement, patients were attributed to MET+ and MET- sub-cohorts...
December 5, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/29215330/quantifying-hospital-acquired-carriage-of-extended-spectrum-beta-lactamase-producing-enterobacteriaceae-among-patients-in-dutch-hospitals
#11
Marjolein F Q Kluytmans-van den Bergh, Suzan P van Mens, Manon R Haverkate, Martin C J Bootsma, Jan A J W Kluytmans, Marc J M Bonten
BACKGROUND Extended-spectrum β-lactamase-producing Enterobacteriaceae (ESBL-E) are emerging worldwide. Contact precautions are recommended for known ESBL-E carriers to control the spread of ESBL-E within hospitals. OBJECTIVE This study quantified the acquisition of ESBL-E rectal carriage among patients in Dutch hospitals, given the application of contact precautions. METHODS Data were used from 2 cluster-randomized studies on isolation strategies for ESBL-E: (1) the SoM study, performed in 14 Dutch hospitals from 2011 through 2014 and (2) the R-GNOSIS study, for which data were limited to those collected in a Dutch hospital in 2014...
December 7, 2017: Infection Control and Hospital Epidemiology
https://www.readbyqxmd.com/read/29214088/advanced-alveolar-soft-part-sarcoma-treated-with-pazopanib-over-three-years
#12
Yoji Shido, Yukihiro Matsuyama
Alveolar soft part sarcoma (ASPS) is a rare malignant tumor that generally occurs in adolescents and young adults. It progresses slowly, but lung and brain metastases often occur in the early phase of the clinical course, and chemotherapy has been reported as not being effective for ASPS. Pazopanib is a multitargeted tyrosine kinase inhibitor that has been clinically available from November 2012 in Japan. This is a case report of a patient presented with multiple lung metastases and unresectable primary abdominal ASPS...
2017: Case Reports in Oncological Medicine
https://www.readbyqxmd.com/read/29209986/data-on-single-nucleotide-polymorphism-of-dna-repair-genes-and-breast-cancer-risk-from-poland
#13
Beata Smolarz, Magdalena Bryś, Ewa Forma, Marek Zadrożny, Jan Bieńkiewicz, Hanna Romanowicz
Single nucleotide polymorphisms (SNPs) may modify the risk of cancer. They may be then regarded as potential markers of carcinogenesis. The aim of this study was to analyze the frequency of genotypes and alleles of SNPs in DNA repair genes and to investigate the influence this genetic variation exerts on breast cancer in Polish females. The test group comprised 600 females with breast cancer and 600 healthy controls. Genomic DNA was isolated and the SNPs in DNA repair genes were determined by High-Resolution Melter (HRM) technique...
December 5, 2017: Pathology Oncology Research: POR
https://www.readbyqxmd.com/read/29207652/iqca-tavv-to-explore-the-effect-of-p-selectin-gpiib-iiia-il-2-il-6-and-il-8-on-deep-venous-thrombosis
#14
Jianhui Wu, Haimei Zhu, Guodong Yang, Yuji Wang, Yaonan Wang, Shurui Zhao, Ming Zhao, Shiqi Peng
Deep vein thrombosis (DVT) associates with considerable morbidity, functional disability and mortality. Due to the lack of suitable inhibitor the correlation of various factors in DVT onset remains unknown. In this context we analyzed the structure of anti-platelet aggregation agent, P-selectin down-regulator, GPIIb/IIIa down-regulator and anti-inflammatory agent, thereby designed N-(3S-1,2,3,4-tetrahydroisoquinoline-3-carbonyl)- Thr-Ala-Arg-Gly-Asp(Val)-Val (IQCA-TAVV) as an inhibitor of DVT to receive evaluations...
October 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/29207293/inhibition-of-apoptosis-by-caspase-inhibitor-z-vad-fmk-improves-cryotolerance-of-in%C3%A2-vitro-derived-bovine-embryos
#15
Maria Elena Pero, Gianluigi Zullo, Luigi Esposito, Alessandra Iannuzzi, Pietro Lombardi, Carolina De Canditiis, Gianluca Neglia, Bianca Gasparrini
The aim of this work was to evaluate whether the treatment with the pan-caspase inhibitor benzyloxycarbonyl-Val-Ala-Asp-fluoromethyl ketone (Z-VAD-FMK) during cryopreservation and post-warming in vitro culture improves cryotolerance of bovine in vitro produced (IVP) embryos. Abattoir derived bovine oocytes were in vitro matured, fertilized and cultured according to standard procedure. On Day 7, embryo yields were assessed and blastocysts randomly divided in 2 groups: vitrification and post-warming culture in the absence (n = 184) or presence (n = 156) of 20 μM Z-VAD-FMK...
December 2, 2017: Theriogenology
https://www.readbyqxmd.com/read/29203646/structural-and-biochemical-characterization-of-the-catalytic-domains-of-gdpp-reveals-a-unified-hydrolysis-mechanism-for-the-dhh-dhha1-phosphodiesterase
#16
Feng Wang, Qing He, Kaixuan Su, Tiandi Wei, Sujuan Xu, Lichuan Gu
The Asp-His-His and Asp-His-His-associated (DHH/DHHA1) domain-containing phosphodiesterases (PDEs) that catalyze degradation of cyclic di-adenosine monophosphate (c-di-AMP) could be subdivided into two subfamilies based on the final product is 5'-phosphadenylyl-adenosine (5'-pApA) or AMP. In previous study we revealed that Rv2837c, a stand-alone DHH/DHHA1 PDE, employs a 5'-pApA internal flipping mechanism to produce AMPs. However, why the membrane-bound DHH/DHHA1 PDE can only degrade c-di-AMP to 5'-pApA remains obscure...
December 4, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/29203459/mobile-phone-apps-for-quality-of-life-and-well-being-assessment-in-breast-and-prostate-cancer-patients-systematic-review
#17
REVIEW
Esther Rincon, Francisco Monteiro-Guerra, Octavio Rivera-Romero, Enrique Dorronzoro-Zubiete, Carlos Luis Sanchez-Bocanegra, Elia Gabarron
BACKGROUND: Mobile phone health apps are increasingly gaining attention in oncological care as potential tools for supporting cancer patients. Although the number of publications and health apps focusing on cancer is increasing, there are still few specifically designed for the most prevalent cancers diagnosed: breast and prostate cancers. There is a need to review the effect of these apps on breast and prostate cancer patients' quality of life (QoL) and well-being. OBJECTIVE: The purposes of this study were to review the scientific literature on mobile phone apps targeting breast or prostate cancer patients and involving QoL and well-being (anxiety and depression symptoms) and analyze the clinical and technological characteristics, strengths, and weaknesses of these apps, as well as patients' user experience with them...
December 4, 2017: JMIR MHealth and UHealth
https://www.readbyqxmd.com/read/29203165/sex-hormone-levels-in-the-brain-of-d-aspartate-treated-rats
#18
Maria Maddalena Di Fiore, Alessandra Santillo, Sara Falvo, Gabriella Chieffi Baccari, Massimo Venditti, Federica Di Giacomo Russo, Monica Lispi, Antimo D'Aniello
d-Aspartate (d-Asp) is an endogenous amino acid present in the central nervous system and endocrine glands of various animal taxa. d-Asp is implicated in neurotransmission, physiology of learning, and memory processes. In gonads, it plays a crucial role in sex hormone synthesis. We have investigated the effects of chronic (30 days d-Asp drinking solution) and acute (i.p. injection of 2μmol/g bw d-Asp) treatments on sex steroid synthesis in rat brain. Furthermore, to verify the direct effect of d-Asp on neurosteroidogenic enzyme activities, brain homogenates were incubated with different substrates (cholesterol, progesterone, or testosterone) with or without the addition of d-Asp...
December 1, 2017: Comptes Rendus Biologies
https://www.readbyqxmd.com/read/29202131/multifunctional-system-for-observing-measuring-and-analyzing-stimulation-evoked-neurochemical-signaling
#19
Christopher J Kimble, Joshua B Boesche, Diane R Eaker, Kenneth R Kressin, James K Trevathan, Seungleal Paek, Anders J Asp, Malcolm B McIntosh, J Luis Lujan
The ability to measure neurotransmitter activity using implanted electrochemical sensors offers researchers a potent technique for analyzing neural activity across specific neural circuitry. We have developed a wirelessly controlled device, WINCS Harmoni, to observe and measure neurotransmitter dynamics at up to four separate sensors, with high temporal and spatial resolution. WINCS Harmoni also incorporates a versatile neurostimulator that can be synchronized with electrochemical recording. The WINCS Harmoni platform is thus optimally suited for probing the neurochemical effects of neurostimulation, and may in turn enable the development of personalized therapies for multiple brain disorders...
May 2017: IEEE International Symposium on Medical Measurements and Applications: proceedings
https://www.readbyqxmd.com/read/29196663/a-ser75-to-asp-phospho-mimicking-mutation-in-src-accelerates-ageing-related-loss-of-retinal-ganglion-cells-in-mice
#20
Kenji Kashiwagi, Sadahiro Ito, Shuichiro Maeda, Goro Kato
Src knockout mice show no detectable abnormalities in central nervous system (CNS) post-mitotic neurons, likely reflecting functional compensation by other Src family kinases. Cdk1- or Cdk5-dependent Ser75 phosphorylation in the amino-terminal Unique domain of Src, which shares no homology with other Src family kinases, regulates the stability of active Src. To clarify the roles of Src Ser75 phosphorylation in CNS neurons, we established two types of mutant mice with mutations in Src: phospho-mimicking Ser75Asp (SD) and non-phosphorylatable Ser75Ala (SA)...
December 1, 2017: Scientific Reports
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