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https://www.readbyqxmd.com/read/28453775/deconvoluting-kinase-inhibitor-induced-cardiotoxicity
#1
Sarah D Lamore, Ernst Ahlberg, Scott Boyer, Michelle L Lamb, Maria P Hortigon-Vinagre, Victor Rodriguez, Godfrey L Smith, Johanna Sagemark, Lars Carlsson, Stephanie M Bates, Allison L Choy, Jonna Stålring, Clay W Scott, Matthew F Peters
Many drugs designed to inhibit kinases have their clinical utility limited by cardiotoxicity-related label warnings or prescribing restrictions. While this liability is widely recognized, designing safer kinase inhibitors (KI) requires knowledge of the causative kinase(s). Efforts to unravel the kinases have encountered pharmacology with nearly prohibitive complexity. At therapeutically relevant concentrations, KIs show promiscuity distributed across the kinome. Here, to overcome this complexity, 65 KIs with known kinome-scale polypharmacology profiles were assessed for effects on cardiomyocyte beating...
April 26, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28448439/ykl-40-induced-inhibition-of-mir-590-3p-promotes-interleukin-18-expression-and-angiogenesis-of-endothelial-progenitor-cells
#2
Te-Mao Li, Shan-Chi Liu, Ya-Hsin Huang, Chien-Chung Huang, Chin-Jung Hsu, Chun-Hao Tsai, Shih-Wei Wang, Chih-Hsin Tang
YKL-40, also known as human cartilage glycoprotein-39 or chitinase-3-like-1, is a pro-inflammatory protein that is highly expressed in rheumatoid arthritis (RA) patients. Angiogenesis is a critical step in the pathogenesis of RA, promoting the infiltration of inflammatory cells into joints and providing oxygen and nutrients to RA pannus. In this study, we examined the effects of YKL-40 in the production of the pro-inflammatory cytokine interleukin-18 (IL-18), and the stimulation of angiogenesis and accumulation of osteoblasts...
April 27, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28445805/fak-phosphorylation-plays-a-central-role-in-thrombin-induced-rpe-cell-migration
#3
E D Aguilar-Solis, A M López-Colomé, I Lee-Rivera, A Alvarez-Arce, E López
The migration of retinal pigment epithelial (RPE) cells is an important step in various pathologic conditions including subretinal neovascularization (SRN), proliferative vitreoretinopathy (PVR) and, importantly, as a consequence of retinal surgery. Therefore, the elucidation of the mechanisms underlying RPE trans-differentiation and migration is essential for devising effective treatments aimed to the prevention of these disorders. A common event in these pathologies is the alteration of the blood-retina barrier (BRB), which allows the interaction of RPE cells with thrombin, a pro-inflammatory protease contained in serum...
April 23, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28444899/tumour-vascular-leakage-defect-due-to-endothelium-targeted-fak-kinase-dead-mutation-is-abrogated-by-fak-y397e-expression
#4
Annika N Alexopoulou, Delphine M Lees, Natalia Bodrug, Tanguy Lechertier, Isabelle Fernandez, Gabriela D'Amico, Matthew Dukinfield, Silvia Batista, Bernardo Tavora, Bryan Serrels, Kairbaan Hodivala-Dilke
Focal adhesion kinase (FAK) inhibitors have been developed as potential anti-cancer agents and are in clinical trials. In vitro activation of FAK kinase domain triggers autophosphorylation of tyrosine 397 (Y397), Src activation and subsequent phosphorylation of other FAK tyrosine residues. However, how FAK-Y397 mutations affect FAK-kinase-dead phenotypes in tumour angiogenesis in vivo is unknown. We developed three Pdgfb-iCre(ert) -driven endothelial-cell (EC)-specific, tamoxifen-inducible homozygous mutant mouse lines: FAK wild-type (WT), FAK kinase-dead (KD), and double mutant (DM); KD with a putatively phosphomimetic Y397E mutation...
April 26, 2017: Journal of Pathology
https://www.readbyqxmd.com/read/28444820/casticin-impairs-cell-migration-and-invasion-of-mouse-melanoma-b16f10-cells-via-pi3k-akt-and-nf-%C3%AE%C2%BAb-signaling-pathways
#5
Yung-Luen Shih, Hsiao-Min Chou, Hsiu-Chen Chou, Hsu-Feng Lu, Yung-Lin Chu, Hung-Sheng Shang, Jing-Gung Chung
Casticin, a polymethoxyflavone, is one of the major active components obtained from Fructus viticis, which have been shown to have anticancer activities including induce cell apoptosis in human cancer cells. The aim of this study was to investigate the molecular mechanisms by which casticin inhibits cell migration and invasion of mouse melanoma B16F10 cells. Cell viability was examined by MTT assay and the results indicated that casticin decreased the total percentages of viable cells in dose-dependent manners...
April 26, 2017: Environmental Toxicology
https://www.readbyqxmd.com/read/28435977/-inhibitory-effects-of-capsaicin-on-migration-and-invasion-of-breast-cancer-mda-mb-231-cells-and-its-mechanism
#6
Bai-He Li, Lei Yuan
The aim of this study was to investigate the effects of capsaicin on migration and invasion of breast cancer MDA-MB-231 cells and its possible mechanism. The MDA-MB-231 cells were incubated in the medium containing different concentrations of capsaicin for 24 h. CCK-8 assay was employed to detect the cell viability. The cell migration and invasion were assessed by wound healing assay and transwell invasion assay, respectively. The protein levels of c-Src, p-c-Src (Tyr416), FAK, p-FAK (Tyr576), Paxillin, p-Paxillin (Tyr118), matrix metalloproteinase 2 (MMP2) and MMP9 in the MDA-MB-231 cells were detected by Western blotting...
April 25, 2017: Sheng Li Xue Bao: [Acta Physiologica Sinica]
https://www.readbyqxmd.com/read/28433634/dual-sphingosine-kinase-inhibitor-ski-ii-enhances-sensitivity-to-5-fluorouracil-in-hepatocellular-carcinoma-cells-via-suppression-of-osteopontin-and-fak-igf-1r-signalling
#7
Petra Grbčić, Ivana Tomljanović, Marko Klobučar, Sandra Kraljević Pavelić, Ksenija Lučin, Mirela Sedić
Hepatocellular carcinoma (HCC) represents the third leading cause of cancer-related deaths globally. Although 5-Fluorouracil (5-FU) is used as the first choice treatment for advanced HCC, it exerts poor efficacy and is associated with acquired and intrinsic resistance. Sphingosine kinases (Sphk) 1 and 2 play tumour-promoting roles in different cancer types including HCC and thus represent promising pharmacological targets. In the present study, we have investigated for the first time the anticancer efficacy and underlying molecular mechanisms of combined administration of 5-FU and dual Sphk1/Sphk2 inhibitor SKI-II (4-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]amino]phenol) in HepG2 hepatocellular carcinoma cells...
April 19, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28433158/characterization-of-a-sulfated-galactoglucan-from-antrodia-cinnamomea-and-its-anticancer-mechanism-via-tgf%C3%AE-fak-slug-axis-suppression
#8
Mei-Kuang Lu, Tung-Yi Lin, Chun-Hao Hu, Chi-Hsein Chao, Chia-Chuan Chang, Hsien-Yeh Hsu
A sulfated 1,4-β-d-galactoglucan (B86-III) with 1,6-branches was isolated and identified from Antrodia cinnamomea. The repeating unit of B86-III was proposed based on one-dimensional 1D ((1)H, (13)C and DEPT-135) and 2D (DQF-COSY, TOCSY, HSQC and HMBC) NMR spectra. The conformation of the sugars was hypothesized to be a rare boat form instead of a (4)C1 chair form. The sulfate substitutions were suggested to be on the C-2 and C-3 positions, resulting in the following structure: B86-III inhibited the viability of H1975 lung cancer cells via cell apoptosis, including the activation of caspase 3 and PARP...
July 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28432466/calpain-inhibition-prevents-flotillin-re-ordering-and-src-family-activation-during-capacitation
#9
Deneb Maldonado-García, Monica L Salgado-Lucio, Ana L Roa-Espitia, Tania Reyes-Miguel, Enrique O Hernández-González
Prior to fertilization, mammalian sperm undergo several molecular, biochemical and physiological changes in a process termed capacitation. However, the mechanisms explaining the involvement of cytoskeletal remodeling and membrane re-ordering in each process prior to fertilization remain poorly understood. We found that the migration of both flotillin microdomains and Src family kinases towards the apical ridge of guinea pig sperm occurs under capacitating conditions. This re-ordering is associated with spectrin cleavage by calpain...
April 22, 2017: Cell and Tissue Research
https://www.readbyqxmd.com/read/28432022/a-crosstalk-between-muscarinic-and-crf2-receptors-regulates-cellular-adhesion-properties-of-human-colon-cancer-cells
#10
M Pelissier-Rota, N T Chartier, B Bonaz, M R Jacquier-Sarlin
Patients with inflammatory bowel disease often suffer from chronic and relapsing intestinal inflammation that favor the development of colitis associated cancer. An alteration of the epithelial intestinal barrier function observed in IBD is supposed to be a consequence of stress. It has been proposed that corticotrophin-releasing factor receptor (CRF2), one of the two receptors of CRF, the principal neuromediator of stress, acts on cholinergic nerves to induce stress-mediated epithelial barrier dysfunction...
April 18, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28431353/discovery-of-potential-anticancer-multi-targeted-ligustrazine-based-cyclohexanone-and-oxime-analogs-overcoming-the-cancer-multidrug-resistance
#11
Gao-Feng Zha, Hua-Li Qin, Bahaa G M Youssif, Muhammad Wahab Amjad, Maria Abdul Ghafoor Raja, Ahmed H Abdelazeem, Syed Nasir Abbas Bukhari
The drug research and development nowadays is focusing on multi-target drugs. In the treatment of cancer, therapies using drugs inhibiting one numerous targets signify a novel viewpoint. In comparison with traditional therapy, multi-targeted drugs directly aim cell subpopulations which are involved in progression of tumor. The current study comprises the synthesis of 34 novel ligustrazine-containing α, β-unsaturated carbonyl-based compounds and oximes. The growth of 5 various cancer cell types was strongly inhibited by ligustrazine-containing oximes as revealed by biological evaluation...
April 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28428953/tetraspanins-function-as-regulators-of-cellular-signaling
#12
REVIEW
Christina M Termini, Jennifer M Gillette
Tetraspanins are molecular scaffolds that distribute proteins into highly organized microdomains consisting of adhesion, signaling, and adaptor proteins. Many reports have identified interactions between tetraspanins and signaling molecules, finding unique downstream cellular consequences. In this review, we will explore these interactions as well as the specific cellular responses to signal activation, focusing on tetraspanin regulation of adhesion-mediated (integrins/FAK), receptor-mediated (EGFR, TNF-α, c-Met, c-Kit), and intracellular signaling (PKC, PI4K, β-catenin)...
2017: Frontiers in Cell and Developmental Biology
https://www.readbyqxmd.com/read/28427224/ponatinib-promotes-a-g1-cell-cycle-arrest-of-merlin-nf2-deficient-human-schwann-cells
#13
Alejandra M Petrilli, Jeanine Garcia, Marga Bott, Stephani Klingeman Plati, Christine T Dinh, Olena R Bracho, Denise Yan, Bing Zou, Rahul Mittal, Fred F Telischi, Xue-Zhong Liu, Long-Sheng Chang, D Bradley Welling, Alicja J Copik, Cristina Fernández-Valle
Neurofibromatosis type 2 (NF2) is a genetic syndrome that predisposes individuals to multiple benign tumors of the central and peripheral nervous systems, including vestibular schwannomas. Currently, there are no FDA approved drug therapies for NF2. Loss of function of merlin encoded by the NF2 tumor suppressor gene leads to activation of multiple mitogenic signaling cascades, including platelet-derived growth factor receptor (PDGFR) and SRC in Schwann cells. The goal of this study was to determine whether ponatinib, an FDA-approved ABL/SRC inhibitor, reduced proliferation and/or survival of merlin-deficient human Schwann cells (HSC)...
March 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28427180/mmp-11-promoted-the-oral-cancer-migration-and-fak-src-activation
#14
Chung-Han Hsin, Ying-Erh Chou, Shun-Fa Yang, Shih-Chi Su, Yi-Ting Chuang, Shu-Hui Lin, Chiao-Wen Lin
Matrix metalloproteinase-11 (MMP-11) has been observed in most invasive human carcinomas. The current study investigated the association between the clinicopathological characteristics and MMP-11 expression in oral squamous cell carcinoma (OSCC) patients. Immunohistochemistry (IHC) staining was performed to assess MMP-11 expression in 279 patients with OSCC. In addition, the metastatic effects of the MMP-11 overexpression on the OSCC cells were also investigated. We found that MMP-11 expression was present in 118/279 (42...
March 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28424421/the-soy-derived-peptide-lunasin-inhibits-invasive-potential-of-melanoma-initiating-cells
#15
Chris Shidal, Jun-Ichi Inaba, Kavitha Yaddanapudi, Keith R Davis
Lunasin is a 44 amino acid peptide with multiple functional domains including an aspartic acid tail, an RGD domain, and a chromatin-binding helical domain. We recently showed that Lunasin induced a phenotype switch of cancer initiating cells (CIC) out of the stem compartment by inducing melanocyte-associated differentiation markers while simultaneously reducing stem-cell-associated transcription factors. In the present study, we advance the hypothesis that Lunasin can reduce pools of melanoma cells with stem cell-like properties, and demonstrate that Lunasin treatment effectively inhibits the invasive potential of CICs in vitro as well as in vivo in a mouse experimental metastasis model...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28423650/mir-425-5p-promotes-invasion-and-metastasis-of-hepatocellular-carcinoma-cells-through-scai-mediated-dysregulation-of-multiple-signaling-pathways
#16
Feng Fang, Tianqiang Song, Ti Zhang, Yunlong Cui, Gewen Zhang, Qingqing Xiong
MicroRNAs (miRNAs) play critical roles in hepatocellular carcinoma (HCC) progression and are key determinants of prognosis. In this study, we found that miR-425-5p was elevated in HCC and correlated with poor prognostic clinicopathological features and low post-operative long-term survival. Multivariate survival analysis indicated that miR-425-5p expression was an independent risk factor for overall and disease-free survival. Interestingly, miR-425-5p promoted invasion and metastasis by HCC cells, but not HCC cell proliferation or apoptosis in vitro...
March 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28423620/exosomal-mir-940-maintains-src-mediated-oncogenic-activity-in-cancer-cells-a-possible-role-for-exosomal-disposal-of-tumor-suppressor-mirnas
#17
Mohammed H Rashed, Pinar Kanlikilicer, Cristian Rodriguez-Aguayo, Martin Pichler, Recep Bayraktar, Emine Bayraktar, Cristina Ivan, Justyna Filant, Andreia Silva, Burcu Aslan, Merve Denizli, Rahul Mitra, Bulent Ozpolat, George A Calin, Anil K Sood, Mohamed F Abd-Ellah, Gouda K Helal, Gabriel Lopez Berestein
Exosomes have emerged as important mediators of diverse biological functions including tumor suppression, tumor progression, invasion, immune escape and cell-to-cell communication, through the release of molecules such as mRNAs, miRNAs, and proteins. Here, we identified differentially expressed exosomal miRNAs between normal epithelial ovarian cell line and both resistant and sensitive ovarian cancer (OC) cell lines. We found miR-940 as abundant in exosomes from SKOV3-IP1, HeyA8, and HeyA8-MDR cells. The high expression of miR-940 is associated with better survival in patients with ovarian serous cystadenocarcinoma...
March 21, 2017: Oncotarget
https://www.readbyqxmd.com/read/28423580/procollagen-lysine-2-oxoglutarate-5-dioxygenase-2-promotes-hypoxia-induced-glioma-migration-and-invasion
#18
Yangyang Xu, Lin Zhang, Yuzhen Wei, Xin Zhang, Ran Xu, Mingzhi Han, Bing Huang, Anjing Chen, Wenjie Li, Qing Zhang, Gang Li, Jian Wang, Peng Zhao, Xingang Li
Poor prognosis of glioblastoma multiforme is strongly associated with the ability of tumor cells to invade the brain parenchyma, which is believed to be the major factor responsible for glioblastoma recurrence. Therefore, identifying the molecular mechanisms driving invasion may lead to the development of improved therapies for glioblastoma patients. Here, we investigated the role of procollagen-lysine 2-oxoglutarate 5-dioxygenase 2 (PLOD2), an enzyme catalyzing collagen cross-linking, in the biology of glioblastoma invasion...
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28423567/cxcr1-2-pathways-in-paclitaxel-induced-neuropathic-pain
#19
Laura Brandolini, Elisabetta Benedetti, Pier Adelchi Ruffini, Roberto Russo, Loredana Cristiano, Andrea Antonosante, Michele d'Angelo, Vanessa Castelli, Antonio Giordano, Marcello Allegretti, Annamaria Cimini
Chemotherapy-induced peripheral neuropathy (CIPN) is a type of neuropathic pain that represents a frequent and serious consequence of chemotherapy agents. Over the last years, significant progress has been achieved in elucidating the underlying pathogenesis of CIPN. The interference of taxanes with microtubule has been proposed as a mechanism that leads to altered axonal transport and to permanent neurological damages. The inflammatory process activated by chemotherapeutic agents has been considered as a potential trigger of nociceptive process in CIPN...
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28423510/genistein-inhibits-the-growth-and-regulates-the-migration-and-invasion-abilities-of-melanoma-cells-via-the-fak-paxillin-and-mapk-pathways
#20
Shuna Cui, Juan Wang, Qingqing Wu, Jing Qian, Changshui Yang, Ping Bo
Genistein is one of the main components of soy-based foods, which are widely known for their many benefits, including anti-cancer, anti-inflammatory, and antioxidant effects. In this study, we investigated the anti-metastasis effects of genistein on B16F10 melanoma cells. Our results showed that genistein strongly inhibited B16F10 cell proliferation and induced apoptosis in time- and concentration-dependent manners. Genistein altered the morphology of B16F10 cells to an elongated shape with slim pseudopodia-like protrusions...
March 28, 2017: Oncotarget
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