keyword
MENU ▼
Read by QxMD icon Read
search

Syk inhibitor

keyword
https://www.readbyqxmd.com/read/29297721/mucor-circinelloides-induces-platelet-aggregation-through-integrin-%C3%AE-iib%C3%AE-3-and-fc%C3%AE-riia
#1
Harlene Ghuman, Alicia Shepherd-Roberts, Stephanie Watson, Malou Zuidscherwoude, Steve P Watson, Kerstin Voelz
Thrombosis is a hallmark of the fatal fungal infection mucormycosis. Yet, the platelet activation pathway in response to mucormycetes is unknown. In this study we determined the platelet aggregation potential of Mucor circinelloides (M. circinelloides) NRRL3631, characterized the signaling pathway facilitating aggregation in response to fungal spores, and identified the influence of the spore developmental stage upon platelet aggregation potential. Using impedance and light-transmission aggregometry, we showed that M...
January 3, 2018: Platelets
https://www.readbyqxmd.com/read/29286114/cigarette-smoke-induced-egfr-activation-promotes-epithelial-mesenchymal-migration-of-human-retinal-pigment-epithelial-cells-through-regulation-of-the-fak-mediated-syk-src-pathway
#2
Ga Bin Park, Daejin Kim
Epithelial-mesenchymal transition (EMT) of retinal pigment epithelial (RPE) cells is inevitable change of age‑related macular degeneration (AMD). Smoking is a major risk factor for the development of EMT in several diseases, including lung cancer. Cigarette smoke‑induced stress promotes the production of epidermal growth factor (EGF) in RPE cells. However, the underlying signaling pathways induced by aberrant EGF receptor (EGFR) expression in cigarette smoke-exposed RPE cells remain largely unknown. In the present study, the morphological transformation and production of EMT-associated cytokines were investigated to analyze the effect of smoking on the retina...
December 27, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29286055/midostaurin-for-the-treatment-of-adult-patients-with-newly-diagnosed-acute-myeloid-leukemia-that-is-flt3-mutation-positive
#3
J S Garcia, M E Percival
Midostaurin is a multitargeted tyrosine kinase inhibitor (TKI) that potently inhibits activated fms-related tyrosine kinase 3 (FLT3) in the nanomolar range and other kinases including platelet-derived growth factor receptors α (PDGFR- α) and β (PDGFR- β), cyclin-dependent kinase, proto-oncogene tyrosine-protein kinase Src, tyrosine-protein kinase Fgr, spleen tyrosine kinase (Syk), KIT proto-oncogene receptor tyrosine kinase and the major vascular endothelial growth factor receptor (VEGFR). Activating mutations in FLT3, which is one of the more common acute myeloid leukemia (AML) mutations, particularly those that result in an FLT3-ITD (internal tandem duplication) mutation, confer poor prognosis and represent a therapeutic target...
October 2017: Drugs of Today
https://www.readbyqxmd.com/read/29274344/calcium-phosphate-particles-stimulate-interleukin-1%C3%AE-release-from-human-vascular-smooth-muscle-cells-a-role-for-spleen-tyrosine-kinase-and-exosome-release
#4
Yana Dautova, Alexander N Kapustin, Kevin Pappert, Matthias Epple, Hanneke Okkenhaug, Simon J Cook, Catherine M Shanahan, Martin D Bootman, Diane Proudfoot
AIMS: Calcium phosphate (CaP) particle deposits are found in several inflammatory diseases including atherosclerosis and osteoarthritis. CaP, and other forms of crystals and particles, can promote inflammasome formation in macrophages leading to caspase-1 activation and secretion of mature interleukin-1β (IL-1β). Given the close association of small CaP particles with vascular smooth muscle cells (VSMCs) in atherosclerotic fibrous caps, we aimed to determine if CaP particles affected pro-inflammatory signalling in human VSMCs...
December 20, 2017: Journal of Molecular and Cellular Cardiology
https://www.readbyqxmd.com/read/29249894/spleen-tyrosine-kinase-inhibition-modulates-p53-activity
#5
Mohammad Althubiti
Spleen tyrosine kinase (SYK) is a cytoplasmic enzyme that promotes survival and proliferation of B cells. SYK inhibition has shown promising results in the treatment of arthritis and chronic lymphocytic leukemia (CLL). However, in other context, it has been shown that SYK overexpression in epithelial cancer cells induced senescence in p53-dependent mechanism, which underscored its antineoplastic activity in vitro. Here, we show that SYK was induced in response of DNA damage in parallel with p53 levels. In addition, using chemical inhibitors of SYK reduced p53 levels in HCT116 and HT1080 cell lines, which underlines the role of SYK inhibition on p53 activity...
2017: Journal of Cell Death
https://www.readbyqxmd.com/read/29246942/synergistic-targeting-of-the-regulatory-and-catalytic-subunits-of-pi3k%C3%AE-in-mature-b-cell-malignancies
#6
Jeffrey Cooney, An-Ping Lin, Daifeng Jiang, Long Wang, Avvaru N Suhasini, Jamie Myers, ZhiJun Qiu, Albert Wölfler, Heinz Sill, Ricardo C T Aguiar
PURPOSE: Aberrant activation of the B cell receptor (BCR) is implicated in the pathogenesis of mature B-cell tumors, a concept validated in part by the clinical success of inhibitors of the BCR-related kinases BTK (Bruton's tyrosine kinase) and PI3Kδ (Phosphatidylinositol-4,5-bisphosphate 3-kinase delta). These inhibitors have limitations, including the paucity of complete responses, acquired resistance, and toxicity. Here we examined the mechanism by which the cyclic-AMP/PDE4 signaling axis suppresses PI3K, towards identifying a novel mechanism-based combinatorial strategy to attack BCR-dependency in mature B-cell malignancies...
December 15, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29241811/syk-and-src-targeted-anti-inflammatory-activity-of-aripiprazole-an-atypical-antipsychotic
#7
Sulgi Yoo, Mi-Yeon Kim, Jae Youl Cho
Aripiprazole (ARP) is a partial agonist of dopamine D2 receptors that is commonly prescribed to treat schizophrenia and bipolar disorder. The anti-inflammatory effect of ARP was recently documented in a few studies, but its molecular mechanisms have not been fully elucidated. In this study, peptidoglycan (PGN)-treated macrophages (RAW264.7 cells), reporter gene assay, an overexpression strategy, immunoprecipitation, and immunoblotting analysis were employed to clarify the anti-inflammatory mechanism of ARP...
December 11, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29231998/phosphorylated-tyr142-%C3%AE-catenin-localizes-to-centrosomes-and-is-regulated-by-syk
#8
D Bhardwaj, M Náger, A Visa, M C Sallán, P J Coopman, C Cantí, J Herreros
β-catenin is a central component of adherent junctions and a key effector of canonical Wnt signalling, in which dephosphorylated Ser/Thr β-catenin regulates gene transcription. β-catenin phosphorylation at Tyr142 (PTyr142 β-catenin), which is induced by receptor and Src family Tyr kinases, represents a previously described β-catenin switch from adhesive to migratory roles. In addition to classical β-catenin roles, phosphorylated Ser/Thr β-catenin and total β-catenin were involved in centrosomal functions, including mitotic spindle formation and centrosome separation...
December 12, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29209318/the-major-chromoblastomycosis-etiologic-agent-fonsecaea-pedrosoi-activates-the-nlrp3-inflammasome
#9
Raffael Júnio Araújo de Castro, Isaque Medeiros Siqueira, Márcio Sousa Jerônimo, Angelina Maria Moreschi Basso, Paulo Henrique de Holanda Veloso Junior, Kelly Grace Magalhães, Luiza Chaves Leonhardt, Stephan Alberto Machado de Oliveira, Pedro Henrique Bürgel, Aldo Henrique Tavares, Anamélia Lorenzetti Bocca
Fonsecaea pedrosoi is the main etiologic agent of chromoblastomycosis (CBM), one of the most prevalent subcutaneous mycosis in tropical and subtropical countries. CBM is a poorly characterized chronic infection that commonly starts after transcutaneous inoculation of conidia and saprophytic hyphae of F. pedrosoi. Recently, we have shown that unlike conidia, hyphae and muriform cells (the parasitic morphotype) of F. pedrosoi promotes an intense inflammatory response pattern in vivo, which comprises the production of an inflammasome-derived cytokine, IL-1β...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/29202301/spleen-tyrosine-kinase-inhibition-ameliorates-airway-inflammation-through-modulation-of-nlrp3-inflammosome-and-th17-treg-axis
#10
Divyesh Patel, Sagar Gaikwad, Naveen Challagundla, Manish Nivsarkar, Reena Agrawal-Rajput
Repeated exposure to the fungal pathogen Aspergillus fumigates triggers spleen tyrosine kinase (SYK) signalling through dectin-1 activation, which is associated with deleterious airway inflammation. β-Glucan-induced dectin-1 signalling activates the NLRP3 inflammasome, which in turn rapidly produces IL-1β, a master regulator of inflammation. IL-1β expression results in Th17/Treg imbalance, pulmonary inflammation, and bystander tissue injury. This study reports that 3,4 methylenedioxy-β-nitrostyrene (MNS), a potent SYK inhibitor, markedly decreased the expression of pro-inflammatory cytokines and increased the expression of anti-inflammatory cytokines in vitro...
December 1, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/29137913/neutrophil-cd16b-crosslinking-induces-lipid-raft-mediated-activation-of-shp-2-and-affects-cytokine-expression-and-retarded-neutrophil-apoptosis
#11
H Yang, H Jiang, Y Song, D J Chen, X J Shen, J H Chen
Two different types of FcRs for IgG are constitutively expressed on the surface of human neutrophils, namely, FcγRIIA (CD32a) and FcγRIIIB (CD16b). Unlike FcγRIIA, FcγRIIIb is GPI anchored to the cell membrane and its signal transduction is still ambiguous. To further understand the signal transduction of CD16b, we compared neutrophil cytokine expression and apoptosis by the cross-linking of CD32a and CD16b respectively. We found that both CD32a and CD16b crosslinking can activate neutrophils, but did not exactly share cytokine expression profiles...
November 11, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/29137391/activated-spleen-tyrosine-kinase-promotes-malignant-progression-of-oral-squamous-cell-carcinoma-via-mtor-s6-signaling-pathway-in-an-erk1-2-independent-manner
#12
Pan Gao, Xianghe Qiao, Haibin Sun, Yi Huang, Jie Lin, Longjiang Li, Xiaoyi Wang, Chunjie Li
Spleen tyrosine kinase (SYK), a non-receptor cytoplasmic tyrosine enzyme, is well known for its ability in certain pathways through immune receptors. Recently, SYK role in cancer has been widely studied. SYK plays a dual role as a tumor suppressor and tumor promoter. Nevertheless, its role in oral squamous cell carcinoma (OSCC) has not been fully investigated. In the current study, samples from OSCC tumors and adjacent normal counterparts were collected and SYK expression was evaluated by real-time qPCR. SYK mRNA expression in tumors was higher than the normal tissues...
October 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/29125705/mycobacterium-tuberculosis-mce3c-promotes-mycobacteria-entry-into-macrophages-through-activation-of-%C3%AE-2-integrin-mediated-signalling-pathway
#13
Yong Zhang, Jie Li, Bingxi Li, Jing Wang, Cui Hua Liu
Establishment of infection by facultative intracellular pathogen Mycobacterium tuberculosis (Mtb) requires adherence to and internalisation by macrophages. However, the effector molecules exploited by Mtb for entry into macrophages remain to be fully understood. The mammalian cell entry (Mce) proteins play an essential role in facilitating the internalisation of mycobacteria into mammalian cells. Here, we characterized Mtb Mce3C as a new mycobacterial surface protein that could promote mycobacterial adhesion to and invasion of macrophages in an RGD motif-dependent manner...
November 10, 2017: Cellular Microbiology
https://www.readbyqxmd.com/read/29122993/microenvironmental-stromal-cells-abrogate-nf-%C3%AE%C2%BAb-inhibitor-induced-apoptosis-in-chronic-lymphocytic-leukemia
#14
Carl Philipp Simon-Gabriel, Katharina Foerster, Shifa Saleem, Dorothee Bleckmann, Marco Benkisser-Petersen, Nicolas Thornton, Kazuo Umezawa, Sarah Decker, Meike Burger, Hendrik Veelken, Rainer Claus, Christine Dierks, Justus Duyster, Katja Zirlik
Nuclear factor κ-light-chain-enhancer of activated B cells (NF-κB) is known to play an important role in the pathogenesis of chronic lymphocytic leukemia (CLL). Several NF-κB inhibitors were shown to successfully induce apoptosis of CLL cells in vitro Since the microenvironment is known to be crucial for the survival of CLL cells, herein, we tested whether NF-κB inhibition may still induce apoptosis in these leukemic cells in the presence of protective stromal interaction. We used the specific NF-κB inhibitor dehydroxymethylepoxyquinomicin (DHMEQ)...
January 2018: Haematologica
https://www.readbyqxmd.com/read/29108825/targeting-interferons-and-their-pathways-in-systemic-lupus-erythematosus
#15
REVIEW
François Chasset, Laurent Arnaud
Significant advances in the understanding of the molecular basis of innate immunity have led to the identification of interferons (IFNs), particularly IFN-α, as central mediators in the pathogenesis of Systemic Lupus Erythematosus. Therefore, targeting of IFNs and of their downstream pathways has emerged as important developments for novel drug research in SLE. Based on this, several specific interferon blocking strategies using anti-IFN-α antibodies, anti-type I interferon receptor antibodies, Interferon-α-kinoid, or anti-IFN-γ antibodies have all been assessed in recent clinical trials...
November 4, 2017: Autoimmunity Reviews
https://www.readbyqxmd.com/read/29104084/orthopaedic-implant-materials-drive-m1-macrophage-polarization-in-a-spleen-tyrosine-kinase-and-mitogen-activated-protein-kinase-dependent-manner
#16
Olwyn R Mahon, Sarah O'Hanlon, Clare C Cunningham, Geraldine M McCarthy, Christopher Hobbs, Valeria Nicolosi, Daniel J Kelly, Aisling Dunne
Total joint replacements (TJR) are costly procedures required to relieve pain and restore function in patients suffering from end-stage arthritis. Despite great progress in the development and durability of TJRs, the generation of prosthesis-associated wear particles over time leads to an inflammatory cascade which culminates in periprosthetic osteolysis. Studies suggest that wear particles drive the polarization/differentiation of immature macrophages towards a pro-inflammatory M1 phenotype rather than an anti-inflammatory M2 phenotype associated with normal bone and wound healing...
November 2, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/29078091/hmgb1-mediates-aspergillus-fumigatus-induced-inflammatory-response-in-alveolar-macrophages-of-copd-mice-via-activating-myd88-nf-%C3%AE%C2%BAb-and-syk-pi3k-signalings
#17
Pengpeng Zhang, Xiaofeng Xin, Liping Fang, Hao Jiang, Xiaoyong Xu, Xin Su, Yi Shi
The incidence and mortality of Aspergillus fumigatus (A. fumigatus) infected chronic obstructive pulmonary disease (COPD) patients are increasing. HMGB1, which mediates inflammatory response, is increased in COPD patients. However, the role and mechanism of HMGB1 in A. fumigatus-infected alveolar macrophages of COPD mice remain unknown. Alveolar macrophages isolated from COPD mice were infected with A. fumigatus conidia and then HMGB1 expression was assayed. The levels of pro-inflammatory cytokines, which was confirmed by TLR2/4 or Dectin-1 siRNA, RAGE, Dectin-1, and TLR2/4 levels were assayed after HMGB1 knockdown...
October 24, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/29056373/jte-852-a-novel-spleen-tyrosine-kinase-inhibitor-blocks-immunoglobulin-g-mediated-cellular-responses-and-autoimmune-reactions-in-vivo
#18
Toshinobu Kato, Takeshi Ohta, Hidenori Iwasaki, Hatsue Kobayashi, Akira Matsuo, Takahiro Hata, Mutsuyoshi Matsushita
AIMS: Immune and inflammatory responses mediated by immunoglobulin (Ig) G are largely responsible for the pathogenesis of autoimmune diseases. Spleen tyrosine kinase (Syk) plays a pivotal role in the IgG-mediated responses; therefore, Syk has emerged as a new therapeutic target for the treatment of autoimmune diseases. In this study, we investigated the inhibitory actions of JTE-852, a novel Syk inhibitor, on IgG-mediated cellular responses and autoimmune reactions in vivo. MAIN METHODS: We examined mediator secretion from human monocytes...
October 19, 2017: Life Sciences
https://www.readbyqxmd.com/read/29055830/pharmacological-inhibition-of-tankyrase-induces-bone-loss-in-mice-by-increasing-osteoclastogenesis
#19
Shunichi Fujita, Tomoyuki Mukai, Takafumi Mito, Shoko Kodama, Akiko Nagasu, Mizuho Kittaka, Teruki Sone, Yasuyoshi Ueki, Yoshitaka Morita
Tankyrase is a poly (ADP-ribose) polymerase that leads to ubiquitination and degradation of target proteins. Since tankyrase inhibitors suppress the degradation of AXIN protein, a negative regulator of the canonical Wnt pathway, they effectively act as Wnt inhibitors. Small molecule tankyrase inhibitors are being investigated as drug candidates for cancer and fibrotic diseases, in which the Wnt pathways are aberrantly activated. Tankyrase is also reported to degrade the adaptor protein SH3BP2 (SH3 domain-binding protein 2)...
October 18, 2017: Bone
https://www.readbyqxmd.com/read/29047397/tyrosine-kinase-4-is-involved-in-the-reproduction-of-the-platyhelminth-parasite-schistosoma-japonicum
#20
Han Ding, Fengchun Liu, Lulu Zhu, Fei Wu, Quan Liu, Siyu He, Wei Shao, Yinan Du, Cuiping Ren, Jijia Shen, Miao Liu
BACKGROUND: Schistosomiasis is one of the most common parasitic diseases affecting millions of humans and animals worldwide. Understanding the signal transduction pathways and the molecular basis of reproductive regulation in schistosomes is critically important for developing new strategies for preventing and treating these infections. Syk kinases regulate the proliferation, differentiation, morphogenesis, and survival of various types of cells and have been identified in invertebrates...
October 18, 2017: Parasites & Vectors
keyword
keyword
7247
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"