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https://www.readbyqxmd.com/read/29760222/erk-mutations-and-amplification-confer-resistance-to-erk-inhibitor-therapy
#1
Bijay S Jaiswal, Steffen Durinck, Eric Stawiski, Jianping Yin, Weiru Wang, Eva Lin, John G Moffat, Scott Martin, Zora Modrusan, Somasekar Seshagiri
PURPOSE: MAPK pathway inhibitors targeting BRAF and MEK have shown clinical efficacy in patients with RAF and/or RAS mutated tumors. However, acquired resistance to these agents has been an impediment to improved long-term survival in the clinic. In such cases, targeting ERK downstream of BRAF/MEK has been proposed as a potential strategy for overcoming acquired resistance. Preclinical studies suggest that ERK inhibitors are effective at inhibiting BRAF/RAS mutated tumor growth and overcome BRAF or/and MEK inhibitor resistance...
May 14, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29758494/uncovering-potential-anti-neuroinflammatory-components-of-modified-wuziyanzong-prescription-through-a-target-directed-molecular-docking-fingerprint-strategy
#2
Jinfeng Chen, Jinlong Wang, Yingyuan Lu, Shaoyang Zhao, Qian Yu, Xuemei Wang, Pengfei Tu, Kewu Zeng, Yong Jiang
Neuroinflammation is a main factor in the pathogenesis of neurodegenerative diseases, such as Alzheimer disease. Our previous studies indicated that the modified Wuziyanzong Prescription (MWP) can suppress neuroinflammatory responses via nuclear factor-kappa B (NF-κB) and mitogen-activated protein kinases (MAPKs) signaling pathways. However, the anti-neuroinflammatory components of MWP remain unclear. Herein, a target-directed molecular docking fingerprint (TMDF) strategy, via integrating the chemical profiling and molecular docking approaches, was developed to identify the potential anti-neuroinflammatory components of MWP...
May 1, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29756334/effect-of-cell-phone-radiofrequency-on-angiogenesis-and-cell-invasion-in-human-head-and-neck-cancer-cells
#3
Yaman M Alahmad, Mohammed Aljaber, Alaaeldin I Saleh, Huseyin C Yalcin, Tahar Aboulkassim, Amber Yasmeen, Gerald Batist, Ala-Eddin Al Moustafa
BACKGROUND: Today, the cell phone is the most widespread technology globally. However, the outcome of cell-phone radiofrequency on head and neck cancer progression has not yet been explored. METHODS: The chorioallantoic membrane (CAM) and human head and neck cancer cell lines, FaDu and SCC25, were used to explore the outcome of cell-phone radiofrequency on angiogenesis, cell invasion, and colony formation of head and neck cancer cells, respectively. Western blot analysis was used to investigate the impact of the cell phone on the regulation of E-cadherin and Erk1/Erk2 genes...
May 13, 2018: Head & Neck
https://www.readbyqxmd.com/read/29752775/microrna-92a-promotes-tumor-growth-and-suppresses-immune-function-through-activation-of-mapk-erk-signaling-pathway-by-inhibiting-pten-in-mice-bearing-u14-cervical-cancer
#4
Zeng-Hui Li, Lei Li, Lin-Ping Kang, Yan Wang
Cervical cancer is known as the possible outcome of genital infection, while the molecular mechanisms of initiation, development, and metastasis of cervical cancer have not yet been fully elucidated. Our study aims to investigate the effects of microRNA-92a (miR-92a) on tumor growth and immune function by targeting PTEN via the MAPK/ERK signaling pathway in tumor-bearing mice. C57BL/6 female mice were used for tumor-bearing mouse models and their tumor and adjacent normal tissues were collected, and normal cervical tissues were obtained from normal mice...
May 11, 2018: Cancer Medicine
https://www.readbyqxmd.com/read/29741735/widespread-epigenomic-transcriptomic-and-proteomic-differences-between-hip-osteophytic-and-articular-chondrocytes-in-osteoarthritis
#5
Julia Steinberg, Roger A Brooks, Lorraine Southam, Sahir Bhatnagar, Theodoros I Roumeliotis, Konstantinos Hatzikotoulas, Eleni Zengini, J Mark Wilkinson, Jyoti S Choudhary, Andrew W McCaskie, Eleftheria Zeggini
Objectives: To identify molecular differences between chondrocytes from osteophytic and articular cartilage tissue from OA patients. Methods: We investigated genes and pathways by combining genome-wide DNA methylation, RNA sequencing and quantitative proteomics in isolated primary chondrocytes from the cartilaginous layer of osteophytes and matched areas of low- and high-grade articular cartilage across nine patients with OA undergoing hip replacement surgery. Results: Chondrocytes from osteophytic cartilage showed widespread differences to low-grade articular cartilage chondrocytes...
May 8, 2018: Rheumatology
https://www.readbyqxmd.com/read/29732117/isoform-selective-activity-based-profiling-of-erk-signaling
#6
Myungsun Shin, Caroline E Franks, Ku-Lung Hsu
Extracellular signal-regulated kinases (ERKs) mediate downstream signaling of RAS-RAF-MEK as key regulators of the mitogen-activated protein kinase (MAPK) pathway. Activation of ERK signaling is a hallmark of cancer and upstream MAPK proteins have been extensively pursued as drug targets for cancer therapies. However, the rapid rise of resistance to clinical RAF and MEK inhibitors has prompted interest in targeting ERK (ERK1 and ERK2 isoforms) directly for cancer therapy. Current methods for evaluating activity of inhibitors against ERK isoforms are based primarily on analysis of recombinant proteins...
March 7, 2018: Chemical Science
https://www.readbyqxmd.com/read/29677548/combination-of-curcumin-and-vagus-nerve-stimulation-attenuates-cerebral-ischemia-reperfusion-injury-induced-behavioral-deficits
#7
Jian Xu, Xinjuan Kong, Hong Xiu, Yihe Dou, Zeyu Wu, Peng Sun
AIM: Previous studies indicated that cerebral ischemia/reperfusion injury (CI/RI) could induce behavioral deficits. Single treatment of vagus nerve stimulation (VNS) or curcumin is reported to restore CI/RI-induced behavioral deficits. However, the synergic effect remains unclear. MATERIALS AND METHODS: Rats were divided into 6 groups: sham, CI/RI, VNS, CI/RI + VNS, VNS + curcumin and CI/RI + VNS + curcumin groups. Each group was further divided into three or four subgroups for further assessments...
April 17, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29670075/the-novel-trail-receptor-agonist-apg350-exerts-superior-therapeutic-activity-in-pancreatic-cancer-cells
#8
Karen Legler, Charlotte Hauser, Jan-Hendrik Egberts, Anna Willms, Carola Heneweer, Susann Boretius, Christoph Röcken, Claus-Christian Glüer, Thomas Becker, Michael Kluge, Oliver Hill, Christian Gieffers, Harald Fricke, Holger Kalthoff, Johannes Lemke, Anna Trauzold
Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) has raised attention as a novel anticancer therapeutic as it induces apoptosis preferentially in tumor cells. However, first-generation TRAIL-receptor agonists (TRAs), comprising recombinant TRAIL and agonistic receptor-specific antibodies, have not demonstrated anticancer activity in clinical studies. In fact, cancer cells are often resistant to conventional TRAs. Therefore, in addition to TRAIL-sensitizing strategies, next-generation TRAs with superior apoptotic activity are warranted...
April 18, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29661693/phosphorylation-of-beta-3-adrenergic-receptor-at-serine-247-by-erk-map-kinase-drives-lipolysis-in-obese-adipocytes
#9
Shangyu Hong, Wei Song, Peter-James H Zushin, Bingyang Liu, Mark P Jedrychowski, Amir I Mina, Zhaoming Deng, Dimitrije Cabarkapa, Jessica A Hall, Colin J Palmer, Hassan Aliakbarian, John Szpyt, Steven P Gygi, Ali Tavakkoli, Lydia Lynch, Norbert Perrimon, Alexander S Banks
OBJECTIVE: The inappropriate release of free fatty acids from obese adipose tissue stores has detrimental effects on metabolism, but key molecular mechanisms controlling FFA release from adipocytes remain undefined. Although obesity promotes systemic inflammation, we find activation of the inflammation-associated Mitogen Activated Protein kinase ERK occurs specifically in adipose tissues of obese mice, and provide evidence that adipocyte ERK activation may explain exaggerated adipose tissue lipolysis observed in obesity...
March 29, 2018: Molecular Metabolism
https://www.readbyqxmd.com/read/29644902/interleukin-il-36-gamma-induces-mucin-5ac-oligomeric-mucus-gel-forming-expression-via-il-36-receptor-extracellular-signal-regulated-kinase-1-and-2-and-p38-nuclear-factor-kappa-light-chain-enhancer-of-activated-b-cells-in-human-airway-epithelial-cells
#10
Chang Hoon Bae, Yoon Seok Choi, Hyung Gyun Na, Si-Youn Song, Yong-Dae Kim
BACKGROUND: Mucin 5AC, oligomeric mucus/gel-forming (MUC5AC) expression is significantly increased in allergic and inflammatory airway diseases. Interleukin (IL) 36 gamma is predominantly expressed in airway epithelial cells and plays an important role in innate and adaptive immune responses. IL-36 gamma is induced by many inflammatory mediators, including cytokines and bacterial and viral infections. However, the association between IL-36 gamma and mucin secretion in human airway epithelial cells has not yet been fully investigated...
March 2018: American Journal of Rhinology & Allergy
https://www.readbyqxmd.com/read/29629569/reversible-versus-irreversible-inhibition-modes-of-erk2-a-comparative-analysis-for-erk2-protein-kinase-in-cancer-therapy
#11
Shama Khan, Imane Bjij, Robin M Betz, Mahmoud Es Soliman
AIM: Irreversible covalent drug inhibition is an emerging paradigm; however, critical gaps in unraveling the efficacy of molecular determinants still persist. METHODOLOGY: We compare two ERK2 inhibitors with different binding modes. A 5-7-Oxozeaenol is selective inhibitor which irreversibly binds ERK2 by the formation of covalent bond with Cys166 while 5-iodotubercidin binds noncovalently. Result & discussion: Covalent inhibition showed greater protein stability, favorable binding energetics (irreversible inhibition binding free energy [ΔGbind ] = -40...
April 9, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29626628/hepatocyte-specific-deletion-of-lass2-protects-against-diet-induced-hepatic-steatosis-and-insulin-resistance
#12
Shaohua Fan, Yanyan Wang, Cun Wang, Haojie Jin, Zheng Wu, Jun Lu, Zifeng Zhang, Chunhui Sun, Qun Shan, Dongmei Wu, Juan Zhuang, Ning Sheng, Ying Xie, Mengqiu Li, Bin Hu, Jingyuan Fang, Yuanlin Zheng, Wenxin Qin
Homo sapienslongevity assurance homolog 2 of yeast LAG1 (LASS2) is expressed mostly in human liver. Here, we explored roles of LASS2 in pathogenesis of hepatic steatosis. Hepatocyte-specific LASS2 knockout (LASS2-/- ) mice were generated using Cre-LoxP system. LASS2-/- and wild-type (WT) mice were fed with chow or high-fat diet (HFD). We found LASS2-/- mice were resistant to HFD-induced hepatic steatosis and insulin resistance. In HFD-fed mice, LASS2 deficiency significantly inhibited p38 MAPK and ERK1/ERK2 signaling in mouse liver...
April 4, 2018: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/29604345/inflammation-insulin-signaling-and-cognitive-function-in-aged-app-ps1-mice
#13
Paul Denver, Andrew English, Paula L McClean
Cognitive dysfunction and neuroinflammation are typical in Alzheimer's disease (AD), but are also associated with normal aging, albeit less severely. Insulin resistance in the brain has been demonstrated in AD patients and is thought to be involved in AD pathophysiology. Using 15-18 month-old APP/PS1 mice, this study measured peripheral and central insulin signaling and sensitivity, inflammatory markers in brain and plasma and oxidative stress and synapse density in the brain. Novel object recognition, Morris water maze and reversal water maze tasks were performed to assess cognitive function in aged APP/PS1 mice and wild type littermates...
March 29, 2018: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/29604272/resistin-upregulates-muc5ac-b-mucin-gene-expression-in-human-airway-epithelial-cells
#14
Soyoung Kwak, Yong-Dae Kim, Hyung Gyun Na, Chang Hoon Bae, Si-Youn Song, Yoon Seok Choi
Adipokines, a group of proteins including leptin, visfatin, resistin, and adiponectin, are produced by adipocytes. Among adipokines, resistin is implicated in insulin resistance and inflammatory response modulation. Mucus hypersecretion has been greatly linked to airway diseases, such as asthma, chronic obstructive pulmonary disease, and rhinosinusitis. Increasing evidence has indicated that adipokines, such as leptin and visfatin, play important regulatory roles in various biological processes involved in mucus secretion...
March 28, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29578035/ras-inhibitor-s-trans-trans-farnesylthiosalicylic-acid-enhances-spatial-memory-and-hippocampal-long-term-potentiation-via-up-regulation-of-nmda-receptor
#15
Ya Wang, Tingting Chen, Zihao Yuan, Yajie Zhang, Baofeng Zhang, Liandong Zhao, Ling Chen
Statins by reducing farnesyl-pyrophosphate or farnesyl transferase inhibitors have been demonstrated to enhance spatial memory and long-term potentiation (LTP). The objective of this study was to investigate effects of the synthetic Ras inhibitor S-trans, trans-farnesylthiosalicylic acid (FTS) on spatial cognitive function in adult mice, synaptic plasticity in hippocampal CA1 regions, and NMDA receptor (NMDAr) activity of pyramidal cells. Here, we show that administering FTS (5 mg/kg, i.p.) enhanced spatial cognitive performance, as assessed via Morris water maze and Y-maze tests...
March 22, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29557644/structural-regulation-of-a-neurofilament-inspired-intrinsically-disordered-protein-brush-by-multisite-phosphorylation
#16
Ruoxing Lei, Jessica P Lee, Matthew B Francis, Sanjay Kumar
Intrinsically disordered proteins (IDPs) play central roles in numerous cellular processes. While IDP structure and function are often regulated by multisite phosphorylation, the biophysical mechanisms linking these post-translational modifications to IDP structure remain elusive. For example, the intrinsically disordered C-terminal sidearm domain of the neurofilament heavy subunit (NFH-SA) forms a dense brush along axonal NF backbones and is subject to extensive serine phosphorylation. Yet, biophysical insight into the relationship between phosphorylation and structure has been limited by the lack of paradigms in which NF brush conformational responses can be measured in the setting of controlled phosphorylation...
March 20, 2018: Biochemistry
https://www.readbyqxmd.com/read/29555954/aqueous-extract-of-sapindus-mukorossi-induced-cell-death-of-a549-cells-and-exhibited-antitumor-property-in-vivo
#17
Min Liu, Yen-Lin Chen, Yao-Haur Kuo, Mei-Kuang Lu, Chia-Ching Liao
Sapindus mukorossi is a deciduous plant and has recently been recognized to have anticancer property. In the present study, we discovered that S. mukorossi leaf and stem aqueous extract (SaM) contained two polysaccharides mainly made of myo-inositol, galactose, glucose, and fructose and the aim of this study was to investigate the antitumor property the aqueous extract SaM. In vitro treatment of SaM diminished proliferative potential of lung adenocarcinomic cells and induced intracellular oxidative stress, as well as necrotic cell death...
March 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29551366/dictyostelium-erk2-is-an-atypical-mapk-required-for-chemotaxis
#18
David J Schwebs, Miao Pan, Nirakar Adhikari, Nick A Kuburich, Tian Jin, Jeffrey A Hadwiger
The Dictyostelium genome encodes only two MAPKs, Erk1 and Erk2, and both are expressed during growth and development. Reduced levels of Erk2 expression have been shown previously to restrict cAMP production during development but still allow for chemotactic movement. In this study the erk2 gene was disrupted to eliminate Erk2 function. The absence of Erk2 resulted in a complete loss of folate and cAMP chemotaxis suggesting that this MAPK plays an integral role in the signaling mechanisms involved with this cellular response...
March 15, 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29551131/extracellular-regulated-kinases-signaling-from-ras-to-erk-substrates-to-control-biological-outcomes
#19
Scott T Eblen
The extracellular-regulated kinases ERK1 and ERK2 are evolutionarily conserved, ubiquitous serine-threonine kinases that are involved in regulating cellular signaling in both normal and pathological conditions. Their expression is critical for development and their hyperactivation is a major factor in cancer development and progression. Since their discovery as one of the major signaling mediators activated by mitogens and Ras mutation, we have learned much about their regulation, including their activation, binding partners and substrates...
2018: Advances in Cancer Research
https://www.readbyqxmd.com/read/29550383/liposomal-grb2-antisense-oligodeoxynucleotide-bp1001-in-patients-with-refractory-or-relapsed-haematological-malignancies-a-single-centre-open-label-dose-escalation-phase-1-1b-trial
#20
Maro Ohanian, Ana Tari Ashizawa, Guillermo Garcia-Manero, Naveen Pemmaraju, Tapan Kadia, Elias Jabbour, Farhad Ravandi, Gautam Borthakur, Michael Andreeff, Marina Konopleva, Miranda Lim, Sherry Pierce, Susan O'Brien, Yesid Alvarado, Srdan Verstovsek, William Wierda, Hagop Kantarjian, Jorge Cortes
BACKGROUND: Activating mutations of tyrosine kinases are common in leukaemias. Oncogenic tyrosine kinases use the growth factor receptor-bound protein 2 (Grb2) for signal transduction, leading to activation of mitogen-activated protein kinase (MAPK) 1 and MAPK3 (ERK2 and ERK1). We hypothesised that inhibition of Grb2 would suppress ERK1 and ERK2 activation and inhibit leukaemia progression. To inhibit Grb2, a liposome-incorporated antisense oligodeoxynucleotide that blocks Grb2 protein expression, BP1001, was developed...
April 2018: Lancet Haematology
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