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https://www.readbyqxmd.com/read/29777964/protection-of-gnrh-analogue-by-chitosan-dextran-sulfate-nanoparticles-for-intravaginal-application-in-rabbit-artificial-insemination
#1
L Casares-Crespo, P Fernández-Serrano, M P Viudes-de-Castro
The present study was designed to prove new rabbit insemination extenders containing aminopeptidase inhibitors (AMIs) with or without chitosan (CS)-dextran sulfate (DS) nanoparticles entrapping the GnRH analogue. In addition, different hormone concentrations were tested in these extenders, evaluating their in vivo effect on rabbit reproductive performance after artificial insemination. A total of 911 females were inseminated with semen diluted with the four experimental extenders (C4 group: 4 μg buserelin/doe in control medium (Tris-citric acid-glucose supplemented with bestatin 10 μM and EDTA 20 mM), C5 group: 5 μg of buserelin/doe in control medium, Q4 group: 4 μg of buserelin/doe into CS-DS nanoparticles in control medium, Q5 group: 5 μg of busereline/doe into CS-DS nanoparticles in control medium)...
May 16, 2018: Theriogenology
https://www.readbyqxmd.com/read/29773570/hdna2-nuclease-helicase-promotes-centromeric-dna-replication-and-genome-stability
#2
Zhengke Li, Bochao Liu, Weiwei Jin, Xiwei Wu, Mian Zhou, Vincent Wenzhe Liu, Ajay Goel, Zhiyuan Shen, Li Zheng, Binghui Shen
DNA2 is a nuclease/helicase that is involved in Okazaki fragment maturation, replication fork processing, and end resection of DNA double-strand breaks. Similar such helicase activity for resolving secondary structures and structure-specific nuclease activity are needed during DNA replication to process the chromosome-specific higher order repeat units present in the centromeres of human chromosomes. Here, we show that DNA2 binds preferentially to centromeric DNA The nuclease and helicase activities of DNA2 are both essential for resolution of DNA structural obstacles to facilitate DNA replication fork movement...
May 17, 2018: EMBO Journal
https://www.readbyqxmd.com/read/29757624/steric-control-of-the-rate-limiting-step-of-udp-galactopyranose-mutase
#3
Gustavo Pierdominici-Sottile, Rodrigo Cossio-P Eacute Rez, Isabel Da Fonseca, Karina Kizjakina, John J Tanner, Pablo Sobrado
Galactose is an abundant monosaccharide found exclusively in mammals as galactopyranose (Galp), the six-membered ring form of this sugar. In contrast, galactose appears in many pathogenic microorganisms as the five-membered ring form, galactofuranose (Galf). Galf biosynthesis begins with the conversion of UDP-Galp to UDP-Galf catalyzed by the flavoenzyme UDP-galactopyranose mutase (UGM). Because UGM is essential for the survival and proliferation of several pathogens, there is interest in understanding the catalytic mechanism to aid inhibitor development...
May 14, 2018: Biochemistry
https://www.readbyqxmd.com/read/29731993/over-activation-of-akt-signaling-leading-to-5-fluorouracil-resistance-in-snu-c5-5-fu-cells
#4
Eun-Ji Kim, Gyeoung-Jin Kang, Jung-Il Kang, Hye-Jin Boo, Jin Won Hyun, Young Sang Koh, Weon-Young Chang, Young Ree Kim, Jung-Mi Kwon, Young Hee Maeng, Eun-Sook Yoo, Chang Hoon Lee, Hee-Kyoung Kang
Here, we investigated whether over-activation of AKT pathway is important in the resistance to 5-fluorouracil (5-FU) in SNU-C5/5-FU cells, 5-FU-resistant human colon cancer cells. When compared to wild type SNU-C5 cells (WT), SNU-C5/5-FU cells showed over-activation of PI3K/AKT pathway, like increased phosphorylation of AKT, mTOR, and GSK-3β, nuclear localization of β-catenin, and decreased E-cadherin. Moreover, E-cadherin level was down-regulated in recurrent colon cancer tissues compared to primary colon cancer tissues...
April 13, 2018: Oncotarget
https://www.readbyqxmd.com/read/29716893/complement-c5-but-not-c3-is-expendable-for-tissue-factor-activation-by-cofactor-independent-antiphospholipid-antibodies
#5
Nadine Müller-Calleja, Svenja Ritter, Anne Hollerbach, Tanja Falter, Karl J Lackner, Wolfram Ruf
The complement and coagulation cascades interact at multiple levels in thrombosis and inflammatory diseases. In venous thrombosis, complement factor 3 (C3) is crucial for platelet and tissue factor (TF) procoagulant activation dependent on protein disulfide isomerase (PDI). Furthermore, C5 selectively contributes to the exposure of leukocyte procoagulant phosphatidylserine (PS), which is a prerequisite for rapid activation of monocyte TF and fibrin formation in thrombosis. Here, we show that monoclonal cofactor-independent antiphospholipid antibodies (aPLs) rapidly activate TF on myelomonocytic cells...
May 8, 2018: Blood Advances
https://www.readbyqxmd.com/read/29691485/the-activities-of-wortmannilactones-against-helminth-electron-transport-chain-enzymes-structure-activity-relationships-and-the-effect-on-trichinella-spiralis-infected-mice
#6
Wen-Cai Liu, Yi-Xin Ren, Ai-Yu Hao, Sun Yu, Xuan Shi, Xue-Qiang Zhang, Yan Xing, Zhi-Long Xiu, Yu Cui, Yue-Sheng Dong
Biotransformation of wortmannilactone F (3) using the marine-derived fungus DL1103 generated wortmannilactone M (1), a novel analog of wortmannilactone, which was a reduction product of 3 at the C-3 carbonyl group. The in vitro inhibitory activities of 10 wortmannilactones, including 1, against electron transport enzymes indicated that all the wortmannilactones were selective inhibitors of NADH-fumarate reductase and NADH-rhodoquinone reductase. The structure-activity relationship analysis showed that the relative configuration of C1" and C5", the positions of double bonds, the oxygen atoms in the dihydropyran moiety, and the keto-carbonyl group in the oxabicyclo-[2...
April 24, 2018: Journal of Antibiotics
https://www.readbyqxmd.com/read/29616034/specific-inhibition-of-complement-activation-significantly-ameliorates-autoimmune-blistering-disease-in-mice
#7
Sidonia Mihai, Misa Hirose, Yi Wang, Joshua M Thurman, V Michael Holers, B Paul Morgan, Jörg Köhl, Detlef Zillikens, Ralf J Ludwig, Falk Nimmerjahn
Epidermolysis bullosa acquisita (EBA) is an antibody-mediated blistering skin disease associated with tissue-bound and circulating autoantibodies to type VII collagen (COL7). Transfer of antibodies against COL7 into mice results in a subepidermal blistering phenotype, strictly depending on the complement component C5. Further, activation predominantly by the alternative pathway is required to induce experimental EBA, as blistering was delayed and significantly ameliorated only in factor B-/- mice. However, C5 deficiency not only blocked the activation of terminal complement components and assembly of the membrane attack complex (MAC) but also eliminated the formation of C5a...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29582550/consensus-opinion-on-diagnosis-and-management-of-thrombotic-microangiopathy-in-australia-and-new-zealand
#8
REVIEW
Lucy C Fox, Solomon J Cohney, Joshua Y Kausman, Jake Shortt, Peter D Hughes, Erica M Wood, Nicole M Isbel, Theo de Malmanche, Anne Durkan, Pravin Hissaria, Piers Blombery, Thomas D Barbour
Thrombotic microangiopathy (TMA) arises in a variety of clinical circumstances with the potential to cause significant dysfunction of the kidneys, brain, gastrointestinal tract and heart. TMA should be considered in all patients with thrombocytopenia and anaemia, with an immediate request to the haematology laboratory to look for red cell fragments on a blood film. Whilst TMA of any aetiology generally demands prompt treatment, this is especially so in thrombotic thrombocytopenic purpura (TTP) and atypical haemolytic uraemic syndrome (aHUS), where organ failure may be precipitous, irreversible and fatal...
March 27, 2018: Internal Medicine Journal
https://www.readbyqxmd.com/read/29578710/chemogenomic-profiling-of-human-and-microbial-fk506-binding-proteins
#9
Sebastian Pomplun, Claudia Sippel, Andreas Hähle, Donald Tay, Kensuke Shima, Alina Klages, Can Murat Ünal, Benedikt Rieß, Hui Ting Toh, Guido Hansen, Ho Sup Yoon, Andreas Bracher, Peter Rainer Preiser, Jan Rupp, Michael Steinert, Felix Hausch
FK506-binding proteins (FKBPs) are evolutionary conserved proteins that display peptidyl-prolyl isomerase activity and act as co-receptors for immunosuppressants. Microbial macrophage infectivity potentiator (Mip) type FKBPs can enhance infectivity. However, developing drug-like ligands for FKBPs or Mips has proven difficult and many FKBPs/Mips still lack a biologically useful ligand. To explore the scope and potential of C5-substituted-[4.3.1]-aza-bicyclic sulfonamides as a broadly applicable class of FKBP inhibitors, we developed a new synthesis for the bicyclic core scaffold and used it to prepare a FKBP/Mip-focused library...
March 26, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29557344/broad-spectrum-antiviral-activity-of-the-deubiquitinase-inhibitor-hbx-against-human-adenoviruses
#10
Karin Kosulin, Elena Lam, Albert Heim, Thomas Dobner, Estefanía Rodríguez
BACKGROUND: Human adenoviral (HAdV) infections are usually mild and self-limited, however, some infections from species A, B, C, D and E, can cause severe illnesses, which have raised public health concerns over the past few years. Current available antiviral therapies have limited efficacy and severe toxicity; therefore, finding new targets for specific anti-adenoviral drug design is urgently needed. Our previous work showed that the small molecule compound, HBX, inhibits HAdV type 5 (species C, HAdV-C5) replication and oncogenic transformation through inhibition of the cellular pro-viral factor ubiquitin-specific protease 7 (USP7)...
March 20, 2018: Antiviral Therapy
https://www.readbyqxmd.com/read/29518656/copper-induced-activation-of-trp-channels-promotes-extracellular-calcium-entry-and-activation-of-camk-pka-pkc-pkg-and-cblpk-leading-to-increased-expression-of-antioxidant-enzymes-in-ectocarpus-siliculosus
#11
Alberto González, Claudio A Sáez, Bernardo Morales, Alejandra Moenne
The existence of functional Transient Receptor Potential (TRP) channels was analyzed in Ectocarpus siliculosus using agonists of human TRPs and specific antagonists of TRPA1, TRPC5, TRPM8 and TRPV; intracellular calcium was detected for 60 min. Increases in intracellular calcium were observed at 13, 29, 39 and 50-52 min, which appeared to be mediated by the activation of TRPM8/V1 at 13 min, TRPV1 at 29 min, TRPA1/V1 at 39 min and TRPA1/C5 at 50-52 min. In addition, intracellular calcium increases appear to be due to extracellular calcium entry, not requiring protein kinase activation...
May 2018: Plant Physiology and Biochemistry: PPB
https://www.readbyqxmd.com/read/29486477/combined-inhibition-of-c5-and-cd14-attenuates-systemic-inflammation-in-a-piglet-model-of-meconium-aspiration-syndrome
#12
Anub Mathew Thomas, Camilla Schjalm, Per H Nilsson, Paal H H Lindenskov, Runa Rørtveit, Rønnaug Solberg, Ola Didrik Saugstad, Magnus M Berglund, Patrik Strömberg, Corinna Lau, Terje Espevik, Johan Høgset Jansen, Albert Castellheim, Tom Eirik Mollnes, Andreas Barratt-Due
BACKGROUND: Meconium aspiration syndrome (MAS) is a severe lung condition affecting newborns and it can lead to a systemic inflammatory response. We previously documented complement activation and cytokine release in a piglet MAS model. Additionally, we showed ex vivo that meconium-induced inflammation was dependent on complement and Toll-like receptors. OBJECTIVES: To assess the efficacy of the combined inhibition of complement (C5) and CD14 on systemic inflammation induced in a forceful piglet MAS model...
February 27, 2018: Neonatology
https://www.readbyqxmd.com/read/29465257/investigational-drugs-in-development-to-prevent-neuromyelitis-optica-relapses
#13
REVIEW
Friedemann Paul, Olwen Murphy, Santiago Pardo, Michael Levy
In the short time since 2014, three pivotal, worldwide studies in neuromyelitis optica spectrum disorders have been launched: eculizumab, SA237 and inebelizumab, each based on a unique mechanism. Areas covered: In this review, we provide a discussion on the trial data available for each drug, a brief description of the trial design, and our expert opinion on the potential benefits and risks. Expert opinion: Eculizumab, a C5 complement inhibitor, may prove useful in the treatment of intractable cases of NMOSD, but physicians must be aware of the known risk of meningococcal infection...
March 2018: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/29463535/grl-079-a-novel-hiv-1-protease-inhibitor-is-extremely-potent-against-multidrug-resistant-hiv-1-variants-and-has-a-high-genetic-barrier-against-the-emergence-of-resistant-variants
#14
Nicole S Delino, Manabu Aoki, Hironori Hayashi, Shin-Ichiro Hattori, Simon B Chang, Yuki Takamatsu, Cuthbert D Martyr, Debananda Das, Arun K Ghosh, Hiroaki Mitsuya
We identified four novel nonpeptidic human immunodeficiency virus type 1 (HIV-1) protease inhibitors (PIs), GRL-078, -079, -077, and -058, containing an alkylamine at the C-5 position of P2 tetrahydropyrano-tetrahydrofuran (Tp-THF) and a P2' cyclopropyl (Cp) (or isopropyl)-aminobenzothiazole (Abt) moiety. Their 50% effective concentrations (EC50 s) were 2.5 to 30 nM against wild-type HIV-1NL4-3 , 0.3 to 6.7 nM against HIV-2EHO , and 0.9 to 90 nM against laboratory-selected PI-resistant HIV-1 and clinical HIV-1 variants resistant to multiple FDA-approved PIs (HIVMDR )...
May 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29444937/maraviroc-is-associated-with-latent-hiv-1-reactivation-through-nf-%C3%AE%C2%BAb-activation-in-resting-cd4-t-cells-from-hiv-infected-individuals-on-suppressive-antiretroviral-therapy
#15
Nadia Madrid-Elena, María Laura García-Bermejo, Sergio Serrano-Villar, Alberto Díaz-de Santiago, Beatriz Sastre, Carolina Gutiérrez, Fernando Dronda, María Coronel Díaz, Ester Domínguez, María Rosa López-Huertas, Beatriz Hernández-Novoa, Santiago Moreno
Maraviroc is a CCR5 antagonist used in the treatment of HIV-1 infection. We and others have suggested that maraviroc could reactivate latent HIV-1. To test the latency reversing potential of maraviroc and the mechanisms involved, we performed a phase-II, single-center, open-label study in which maraviroc was administered for 10 days to 20 HIV-1-infected individuals on suppressive antiretroviral therapy (Eudra CT: 2012-003215-66). All patients completed full maraviroc dosing and follow up. The primary endpoint was to study whether maraviroc may reactivate HIV-1 latency, eliciting signalling pathways involved in the viral reactivation...
February 14, 2018: Journal of Virology
https://www.readbyqxmd.com/read/29437288/staphylococcus-aureus-induced-complement-activation-promotes-tissue-factor-mediated-coagulation
#16
E W Skjeflo, D Christiansen, H Fure, J K Ludviksen, T M Woodruff, T Espevik, E W Nielsen, O L Brekke, T E Mollnes
Essentials Complement, Toll-like receptors and coagulation cross-talk in the process of thromboinflammation. This is explored in a unique human whole-blood model of S. aureus bacteremia. Coagulation is here shown as a downstream event of C5a-induced tissue factor (TF) production. Combined inhibition of C5 and CD14 efficiently attenuated TF and coagulation. SUMMARY: Background There is extensive cross-talk between the complement system, the Toll-like receptors (TLRs), and hemostasis. Consumptive coagulopathy is a hallmark of sepsis, and is often mediated through increased tissue factor (TF) expression...
May 2018: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/29434593/-leishmania-donovani-inhibitor-of-serine-peptidases-2-mediated-inhibition-of-lectin-pathway-and-upregulation-of-c5ar-signaling-promote-parasite-survival-inside-host
#17
Sudha Verma, Abhishek Mandal, Md Yousuf Ansari, Ajay Kumar, Kumar Abhishek, Ayan Kumar Ghosh, Ashish Kumar, Vinod Kumar, Sushmita Das, Pradeep Das
Leishmania donovani , the causative agent of Indian visceral leishmaniasis has to face several barriers of the immune system inside the mammalian host for its survival. The complement system is one of the first barriers and consists of a well-balanced network of proteases including S1A family serine proteases (SPs). Inhibitor of serine peptidases (ISPs) is considered as inhibitor of S1A family serine peptidases and is reported to be present in trypanosomes, including Leishmania . In our previous study, we have deciphered the role of ISPs [LdISP1 and L...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29419916/consensus-opinion-on-diagnosis-and-management-of-thrombotic-microangiopathy-in-australia-and-new-zealand
#18
REVIEW
Lucy C Fox, Solomon J Cohney, Joshua Y Kausman, Jake Shortt, Peter D Hughes, Erica M Wood, Nicole M Isbel, Theo de Malmanche, Anne Durkan, Pravin Hissaria, Piers Blombery, Thomas D Barbour
Thrombotic microangiopathy (TMA) arises in a variety of clinical circumstances with the potential to cause significant dysfunction of the kidneys, brain, gastrointestinal tract and heart. TMA should be considered in all patients with thrombocytopenia and anaemia, with an immediate request to the haematology laboratory to look for red cell fragments on a blood film. Whilst TMA of any aetiology generally demands prompt treatment, this is especially so in thrombotic thrombocytopenic purpura (TTP) and atypical haemolytic uraemic syndrome (aHUS), where organ failure may be precipitous, irreversible and fatal...
February 8, 2018: Nephrology
https://www.readbyqxmd.com/read/29407333/eculizumab-for-prevention-of-antibody-mediated-rejection-in-blood-group-incompatible-renal-transplantation
#19
P West-Thielke, K Progar, M Campara, N Jasiak, L Gallon, I Tang, M Spaggiari, I Tzvetanov, E Benedetti
Antibody-mediated rejection (AMR) is one of the leading causes of allograft failure especially in patients undergoing ABO-incompatible (ABOi) renal transplantation. We hypothesized that complement inhibition with eculizumab, a C5 inhibitor, would protect against AMR and maintain graft function in ABOi renal transplant recipients. Four patients undergoing living donor kidney transplant from ABOi donors were treated with a 9-week eculizumab course without therapeutic plasma exchange, intravenous immunoglobulin, or splenectomy...
January 2018: Transplantation Proceedings
https://www.readbyqxmd.com/read/29383821/carboxypeptidase-b2-and-n-play-different-roles-in-regulation-of-activated-complements-c3a-and-c5a-in-mice
#20
J Morser, Z Shao, T Nishimura, Q Zhou, L Zhao, J Higgins, L L K Leung
Essentials Two basic carboxypeptidases are present in plasma, B2 (CPB2) and N (CPN). Cpb2-/- and Cpn-/- mice were challenged in a hemolytic uremic syndrome (HUS) model vs. wild type. Cpb2-/- exacerbates HUS while Cpn-/- exacerbates cobra venom factor challenge vs. wild type mice. CPB2 and CPN have overlapping but non-redundant roles. SUMMARY: Background There are two basic carboxypeptidases in plasma. Carboxypeptidase B2 (CPB2) is activated from a circulating zymogen, proCPB2, and carboxypeptidase N (CPN) is constitutively active with both inactivating complement C3a and C5a...
January 31, 2018: Journal of Thrombosis and Haemostasis: JTH
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