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https://www.readbyqxmd.com/read/28088327/cftr-impairment-upregulates-c-src-activity-through-il-1%C3%AE-autocrine-signaling
#1
María Macarena Massip-Copiz, Mariángeles Clauzure, Ángel Gabriel Valdivieso, Tomás Antonio Santa-Coloma
Cystic Fibrosis (CF) is a disease caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene. Previously, we found several genes showing a differential expression in CFDE cells (epithelial cells derived from a CF patient). One corresponded to c-Src; its expression and activity was found increased in CFDE cells, acting as a signaling molecule between the CFTR activity and MUC1 overexpression. Here we report that bronchial IB3-1 cells (CF cells) also showed increased c-Src activity compared to 'CFTR-corrected' S9 cells...
January 11, 2017: Archives of Biochemistry and Biophysics
https://www.readbyqxmd.com/read/28076826/identification-of-new-pyrrolo-2-3-d-pyrimidines-as-src-tyrosine-kinase-inhibitors-in%C3%A2-vitro-active-against-glioblastoma
#2
Francesca Musumeci, Anna Lucia Fallacara, Chiara Brullo, Giancarlo Grossi, Lorenzo Botta, Pierpaolo Calandro, Mario Chiariello, Miroslava Kissova, Emmanuele Crespan, Giovanni Maga, Silvia Schenone
In the last few years, several pyrrolo-pyrimidine derivatives have been either approved by the US FDA and in other countries for the treatment of different diseases or are currently in phase I/II clinical trials. Herein we present the synthesis and the characterization of a novel series of pyrrolo[2,3-d]pyrimidines, compounds 8a-j, and their activity against Glioblastoma multiforme (GBM). Docking studies and MM-GBSA analysis revealed the ability of such compounds to efficiently interact with the ATP binding site of Src...
December 19, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28075049/src-homology-2-domain-containing-inositol-5-phosphatase-ameliorates-high-glucose-induced-extracellular-matrix-deposition-via-the-phosphatidylinositol-3-kinase-protein-kinase-b-pathway-in-renal-tubular-epithelial-cells
#3
Fan Li, Lisha Li, Jun Hao, Shuxia Liu, Huijun Duan
A typical hallmark of diabetic kidney disease (DKD) is an excessive deposition of extracellular matrix (ECM) in the glomerulus and renal tubulointerstitium, leading to glomerulosclerosis and tubular interstitial fibrosis. Src homology 2 domain-containing inositol 5'-phosphatase (SHIP) is a negative regulator of the phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt) signaling. Here, we investigated the effect of SHIP on ECM deposition in diabetic mice and high glucose-stimulated human renal tubular epithelial cells (HK2 cells)...
January 11, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28074043/correction-dasatinib-a-src-inhibitor-sensitizes-liver-metastatic-colorectal-carcinoma-to-oxaliplatin-in-tumors-with-high-levels-of-phospho-src
#4
Marco Perez, Antonio Lucena-Cacace, Luis Miguel Marín-Gómez, Javier Padillo-Ruiz, Maria Jose Robles-Frias, Carmen Saez, Rocio Garcia-Carbonero, Amancio Carnero
No abstract text is available yet for this article.
November 22, 2016: Oncotarget
https://www.readbyqxmd.com/read/28072464/genistein-and-tyrphostin-ag556-decrease-human-atrial-ultra-rapidly-activating-delayed-rectifier-potassium-current-by-inhibiting-egfr-tyrosine-kinase
#5
Guo-Sheng Xiao, Yan-Hui Zhang, Wei Wu, Hai-Ying Sun, Yan Wang, Gui-Rong Li
BACKGROUND AND PURPOSE: The ultra-rapidly activating delayed rectifier K(+) current IKur (encoded by Kv1.5 or KCNA5) plays an important role in human atrial repolarization. The present study investigates the regulation of this current by protein tyrosine kinases (PTKs). EXPERIMENTAL APPROACH: Whole-cell patch voltage-clamp technique, and immunoprecipitation/western blotting analysis were used to investigate whether the PTK inhibitors genistein, Tyrphostin AG556 (AG556) and PP2 regulate human atrial IKur , and hKv1...
January 10, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28072455/src-and-phospho-fak-kinases-are-activated-by-allopregnanolone-promoting-schwann-cells-motility-morphology-and-myelination
#6
Simona Melfi, Maria Magdalena Montt Guevara, Veronica Bonalume, Massimiliano Ruscica, Alessandra Colciago, Tommaso Simoncini, Valerio Magnaghi
Schwann cells' (SCs) development and maturation require coordinate and complementary interaction among several signals and intracellular pathways. Among factors controlling these processes, the signalling intermediates Src tyrosine kinase and focal adhesion kinase (FAK) are relevant for SCs' fate, participating in regulation of SC adhesion, motility and migration. Recently, the progesterone metabolite allopregnanolone (ALLO) was proved to be synthesized by SCs, whereas it acts autocrinally on SC motility and proliferation, which are crucial processes for nerve development, maturation and regeneration...
January 10, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28069687/adaptive-resistance-of-melanoma-cells-to-raf-inhibition-via-reversible-induction-of-a-slowly-dividing-de-differentiated-state
#7
Mohammad Fallahi-Sichani, Verena Becker, Benjamin Izar, Gregory J Baker, Jia-Ren Lin, Sarah A Boswell, Parin Shah, Asaf Rotem, Levi A Garraway, Peter K Sorger
Treatment of BRAF-mutant melanomas with MAP kinase pathway inhibitors is paradigmatic of the promise of precision cancer therapy but also highlights problems with drug resistance that limit patient benefit. We use live-cell imaging, single-cell analysis, and molecular profiling to show that exposure of tumor cells to RAF/MEK inhibitors elicits a heterogeneous response in which some cells die, some arrest, and the remainder adapt to drug. Drug-adapted cells up-regulate markers of the neural crest (e.g., NGFR), a melanocyte precursor, and grow slowly...
January 9, 2017: Molecular Systems Biology
https://www.readbyqxmd.com/read/28068175/cpg-methylation-signature-predicts-recurrence-in-early-stage-hepatocellular-carcinoma-results-from-a-multicenter-study
#8
Jiliang Qiu, Baogang Peng, Yunqiang Tang, Yeben Qian, Pi Guo, Mengfeng Li, Junhang Luo, Bin Chen, Hui Tang, Canliang Lu, Muyan Cai, Zunfu Ke, Wei He, Yun Zheng, Dan Xie, Binkui Li, Yunfei Yuan
Purpose Early-stage hepatocellular carcinoma (E-HCC) is being diagnosed increasingly, and in one half of diagnosed patients, recurrence will develop. Thus, it is urgent to identify recurrence-related markers. We investigated the effectiveness of CpG methylation in predicting recurrence for patients with E-HCCs. Patients and Methods In total, 576 patients with E-HCC from four independent centers were sorted by three phases. In the discovery phase, 66 tumor samples were analyzed using the Illumina Methylation 450k Beadchip...
January 9, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28054986/d-l-sulforaphane-induces-ros-dependent-apoptosis-in-human-gliomablastoma-cells-by-inactivating-stat3-signaling-pathway
#9
Ziwei Miao, Fei Yu, Yahao Ren, Jun Yang
d,l-Sulforaphane (SFN), a synthetic analogue of broccoli-derived isomer l-SFN, exerts cytotoxic effects on multiple tumor cell types through different mechanisms and is more potent than the l-isomer at inhibiting cancer growth. However, the means by which SFN impairs glioblastoma (GBM) cells remains poorly understood. In this study, we investigated the anti-cancer effect of SFN in GBM cells and determined the underlying molecular mechanisms. Cell viability assays, flow cytometry, immunofluorescence, and Western blot results revealed that SFN could induced apoptosis of GBM cells in a dose- and time-dependent manner, via up-regulation of caspase-3 and Bax, and down-regulation of Bcl-2...
January 4, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28044939/inhibition-of-tgf-%C3%AE-signaling-in-tumor-cells-by-small-molecule-src-family-kinase-inhibitors
#10
Tobias Bartscht, Benjamin Rosien, Dirk Rades, Roland Kaufmann, Harald Biersack, Hendrik Lehnerta, Hendrik Ungefroren
In a series of studies carried out over the last couple of years in various cell types, it was observed that the experimentally used Src family kinase inhibitors PP1 and PP2 and the clinically used Src/Abl inhibitors AZM475271 and dasatinib are potent inhibitors of TGF-β mediated cellular responses such as Smad and p38 mitogen-activated protein kinase phosphorylation, Smad-dependent transcriptional activation, growth inhibition, epithelial-mesenchymal transition (EMT), and cell motility. While for PP1/PP2 it was demonstrated shown that these agents directly inhibit the kinase activity of the TGF-β type I receptor activin receptor-like kinase 5, the mechanism of the anti-TGF-β effect of AZM475271 and dasatinib is less clear...
January 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28042453/design-and-synthesis-of-selective-small-molecule-inhibitors-of-coactivator-associated-arginine-methyltransferase-1-carm1
#11
H Ü Kaniskan, M S Eram, J Liu, D Smil, M L Martini, Y Shen, V Santhakumar, P J Brown, C Arrowsmith, M Vedadi, J Jin
Coactivator-associated arginine methyltransferase 1 (CARM1) is a type I protein arginine methyltransferase (PRMT) that catalyzes the conversion of arginine into monomethylarginine (MMA) and further into asymmetric dimethylarginine (ADMA). CARM1 methylates histone 3 arginines 17 and 26, as well as numerous non-histone proteins including CBP/p300, SRC-3, NCOA2, PABP1, and SAP49, while also functioning as a coactivator for various proteins that have been linked to cancer such as p53, NF-κβ, β-catenin, E2F1 and steroid hormone receptor ERα...
September 1, 2016: MedChemComm
https://www.readbyqxmd.com/read/28040437/cryptotanshinone-inhibits-vegf-induced-angiogenesis-by-targeting-the-vegfr2-signaling-pathway
#12
Xiaoming Xu, Li Wu, Xinbin Zhou, Nanyang Zhou, Qin Zhuang, Jinxiu Yang, Jin Dai, Haibing Wang, Shenjie Chen, Wei Mao
OBJECTIVE: Anti-angiogenesis has been proposed as an important strategy for angiogenesis-related diseases. Cryptotanshinone (CPT), an active component of Salvia miltiorrhiza, may be a potential inhibitor of angiogenesis. However, the molecular mechanisms underlying its anti-angiogenic activities remain poorly understood. This study is to investigate the effects of CPT on VEGF-induced angiogenesis and VEGFR2 signaling pathway in human umbilical vein endothelial cells (HUVECs). METHODS: HUVECs were treated with different concentration of CPT (5-20μmol/L) and the viability, endothelial cell migration, invasion, and tubular-like structure formation of HUVECs were detected by MTT, wound-healing migration, Transwell invasion and Matrigel tube formation assays, respectively...
December 28, 2016: Microvascular Research
https://www.readbyqxmd.com/read/28034907/comparison-of-acalabrutinib-a-selective-bruton-tyrosine-kinase-inhibitor-with-ibrutinib-in-chronic-lymphocytic-leukemia-cells
#13
Viralkumar Patel, Kumudha Balakrishnan, Elena Bibikova, Mary Ayres, Michael J Keating, William Wierda, Varsha Gandhi
PURPOSE: Ibrutinib inhibits Bruton tyrosine kinase (BTK) by irreversibly binding to the Cys-481 residue in the enzyme. However, ibrutinib also inhibits several other enzymes that contain cysteine residues homologous to Cys-481 in BTK. Patients with relapsed/refractory or previously untreated chronic lymphocytic leukemia (CLL) demonstrate a high overall response rate to ibrutinib with prolonged survival. Acalabrutinib, a selective BTK inhibitor designed to minimize off-target activity, has shown promising overall response rates in patients with relapsed/refractory CLL...
December 29, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28033278/delayed-onset-of-posterior-reversible-encephalopathy-syndrome-in-a-case-of-scleroderma-renal-crisis-with-maintenance-hemodialysis-case-report-and-literature-review
#14
Ching-Yang Chen, Shin-Yuan Hung, Yi-Jer Lee, Yi-Chan Lin, Chu-Cheng Pai
INTRODUCTION: In some cases, scleroderma renal crisis (SRC) is not easily distinguishable from other thrombotic microangiopathies such as thrombotic thrombocytopenic purpura, especially when the presentation includes neurological or extra-renal manifestations. Here, we present a case of SRC who developed a rare neurotoxic complication, posterior reversible encephalopathy syndrome (PRES).A 36-year-old man with a history of diffuse cutaneous systemic sclerosis developed SRC and acute-on-chronic renal failure and ultimately required maintenance hemodialysis...
December 2016: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28030426/meta-analysis-of-genome-wide-association-studies-on-the-intolerance-of-angiotensin-converting-enzyme-inhibitors
#15
Seyed H Mahmoudpour, Abirami Veluchamy, Moneeza K Siddiqui, Folkert W Asselbergs, Patrick C Souverein, Catherine E de Keyser, Albert Hofman, Chim C Lang, Alexander S F Doney, Bruno H Stricker, Anthonius de Boer, Anke-Hilse Maitland-van der Zee, Colin N A Palmer
OBJECTIVES: To identify single nucleotide polymorphisms (SNPs) associated with switching from an angiotensin-converting enzyme (ACE)-inhibitor to an angiotensin receptor blocker. METHODS: Two cohorts of patients starting ACE-inhibitors were identified within the Rotterdam Study in the Netherlands and the Genetics of Diabetes Audit and Research in Tayside Scotland study in Scotland. Cases were intolerant patients who switched from an ACE-inhibitor to an angiotensin receptor blocker and controls were individuals who used ACE-inhibitors continuously for at least 2 years and did not switch...
December 26, 2016: Pharmacogenetics and Genomics
https://www.readbyqxmd.com/read/28027319/scavenger-receptor-c-mediates-phagocytosis-of-white-spot-syndrome-virus-and-restricts-virus-proliferation-in-shrimp
#16
Ming-Chong Yang, Xiu-Zhen Shi, Hui-Ting Yang, Jie-Jie Sun, Ling Xu, Xian-Wei Wang, Xiao-Fan Zhao, Jin-Xing Wang
Scavenger receptors are an important class of pattern recognition receptors that play several important roles in host defense against pathogens. The class C scavenger receptors (SRCs) have only been identified in a few invertebrates, and their role in the immune response against viruses is seldom studied. In this study, we firstly identified an SRC from kuruma shrimp, Marsupenaeus japonicus, designated MjSRC, which was significantly upregulated after white spot syndrome virus (WSSV) challenge at the mRNA and protein levels in hemocytes...
December 2016: PLoS Pathogens
https://www.readbyqxmd.com/read/28011764/inhibition-of-radiation-induced-glioblastoma-invasion-by-genetic-and-pharmacological-targeting-of-mda-9-syntenin
#17
Timothy P Kegelman, Bainan Wu, Swadesh K Das, Sarmistha Talukdar, Jason M Beckta, Bin Hu, Luni Emdad, Kristoffer Valerie, Devanand Sarkar, Frank B Furnari, Webster K Cavenee, Jun Wei, Angela Purves, Surya K De, Maurizio Pellecchia, Paul B Fisher
Glioblastoma multiforme (GBM) is an intractable tumor despite therapeutic advances, principally because of its invasive properties. Radiation is a staple in therapeutic regimens, although cells surviving radiation can become more aggressive and invasive. Subtraction hybridization identified melanoma differentiation-associated gene 9 [MDA-9/Syntenin; syndecan-binding protein (SDCBP)] as a differentially regulated gene associated with aggressive cancer phenotypes in melanoma. MDA-9/Syntenin, a highly conserved double-PDZ domain-containing scaffolding protein, is robustly expressed in human-derived GBM cell lines and patient samples, with expression increasing with tumor grade and correlating with shorter survival times and poorer response to radiotherapy...
December 23, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28008134/interacting-post-muscarinic-receptor-signaling-pathways-potentiate-matrix-metalloproteinase-1-expression-and-invasion-of-human-colon-cancer-cells
#18
Anan Said, Shien Hu, Ameer Abutaleb, Tonya Watkins, Kunrong Cheng, Ahmed Chahdi, Panjamurthy Kuppusamy, Neeraj Saxena, Guofeng Xie, Jean-Pierre Raufman
M3 muscarinic receptor (M3R) expression is increased in colon cancer; M3R activation stimulates colon cancer cell invasion via cross-talk with epidermal growth factor receptors (EGFR), post-EGFR activation of mitogen-activated protein kinase (MAPK) ERK1/2, and induction of matrix metalloproteinase-1 ( MMP1 ) expression. MMP1 expression is strongly associated with tumor metastasis and adverse outcomes. Here, we asked whether other MAPKs regulate M3R agonist-induced MMP1 expression. In addition to activating ERK1/2, we found that treating colon cancer cells with acetylcholine (ACh) stimulated robust time- and dose-dependent phosphorylation of p38 MAPK...
December 22, 2016: Biochemical Journal
https://www.readbyqxmd.com/read/28006668/design-and-synthesis-of-novel-7-aminosubstituted-pyrido-2-3-b-pyrazines-exhibiting-anti-breast-cancer-activity
#19
Orestis Argyros, Nikolaos Lougiakis, Eva Kouvari, Alexandra Papafotika, Catherine P Raptopoulou, Vassilis Psycharis, Savvas Christoforidis, Nicole Pouli, Panagiotis Marakos, Constantin Tamvakopoulos
Breast cancer (BrCa) remains an unmet medical need despite the revolutionary development of antibody treatments and protein kinase inhibitors. In the current study, a series of novel substituted pyridopyrazine derivatives have been rationally designed and evaluated as multi-kinase inhibitors in the PI3K pathway. The target compounds were prepared from 6-amino-2-picoline, which upon nitration and selective reduction was converted to suitably substituted 6-methyl-7-aminopyrido[2,3-b]pyrazines. Suitable manipulation of the former amines provided the designed analogues, which were then assessed in vitro against several BrCa cell lines using the MTT cytotoxicity assay...
December 12, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28001095/antileukemic-effects-of-midostaurin-in-acute-myeloid-leukemia-the-possible-importance-of-multikinase-inhibition-in-leukemic-as-well-as-nonleukemic-stromal-cells
#20
Tor Henrik Tvedt, Ina Nepstad, Øystein Bruserud
Midostaurin is a multikinase inhibitor that inhibits receptor tyrosine kinases (Flt3, CD117/c-kit, platelet-derived growth factor receptor, vascular endothelial growth factor receptor 2) as well as non-receptor tyrosine kinases (Frg, Src, Syk, Protein kinase C). Combination of midostaurin with conventional intensive chemotherapy followed by one year maintenance monotherapy was recently reported to improve the survival of acute myeloid leukemia (AML) patients with Flt3 mutations. Areas covered: Relevant publications were identified through literature searches in the PubMed database...
December 28, 2016: Expert Opinion on Investigational Drugs
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