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Donghui Zhou, Maya Z Springer, David Xu, Degang Liu, Andy Hudmon, Kay F Macleod, Samy O Meroueh
Triple-negative breast cancers (TNBCs) lack the signature targets of other breast tumors, such as HER2, estrogen receptor, and progesterone receptor. These aggressive basal-like tumors are driven by a complex array of signaling pathways that are activated by multiple driver mutations. Here we report the discovery of 6 (KIN-281), a small molecule that inhibits multiple kinases including maternal leucine zipper kinase (MELK) and the non-receptor tyrosine kinase bone marrow X-linked (BMX) with single-digit micromolar IC50s...
March 23, 2017: Bioorganic & Medicinal Chemistry
X Fang, Y Hu, Y Wang, S Liu, F Wang, X L Chen
Objective: To investigate the role of bone marrow tyrosine kinase on chromosome X (BMX) in the production of tumor necrosis factor α (TNF-α) and interleukin-1β (IL-1β) from mouse mononuclear-macrophages induced by endotoxin/lipopolysaccharide (LPS) and its related mechanism. Methods: Mouse mononuclear-macrophages RAW264.7 were inoculated in 6-well plates and routinely cultured for the following experiments. (1) Cells were collected and divided into blank control group, LPS control group, and 75, 750, 7 500, 75 000 nmol/L BMX-IN-1 pretreatment groups according to the random number table, with 8 wells in each group...
April 20, 2017: Zhonghua Shao Shang za Zhi, Zhonghua Shaoshang Zazhi, Chinese Journal of Burns
Ye Wang, Jufeng Xia, Zhaoyuan Fang, Fei Li, Duo Li, Zuoyun Wang, Yan Feng, Jian Zhang, Haiquan Chen, Hongbin Ji, Hongyan Liu
The non-receptor tyrosine kinase BMX has been reported in several solid tumors. However, the alternative splicing of BMX and its clinical relevance in lung cancer remain to be elucidated. Exon1.0 array was used to identify a novel alternative splicing of BMX, BMXΔN, which was confirmed by rapid amplification of cDNA ends and reverse transcription-polymerase chain reaction. BMXΔN, resulting from exon skipping with excluding exon 1 to exon 8 of BMX gene, was found in 12% human lung adenocarcinoma specimens...
April 3, 2017: Oncotarget
Ting Wei, Weiliang Zhu, Shun Fang, Xiangpin Zeng, Jie Huang, Jie Yang, Jian Zhang, Linlang Guo
miR-495 serves as an oncogenic miRNA or a tumor suppressor in different types of cancer. However, its role in the drug resistance of small cell lung cancer (SCLC) remains unidentified. In this study, we investigated whether miR-495 regulates the chemoresistance of SCLC through the epithelial-mesenchymal transition (EMT) via Epithelial and endothelial tyrosine kinase (Etk/BMX) using two drug-resistant cell lines. Loss- and gain-of-function experiments showed miR-495 regulated cell proliferation, tumor growth and drug resistance...
2017: American Journal of Cancer Research
Franck Di Rienzo, Guillaume Martinent, Lucie Levêque, Tadhg MacIntyre, Christian Collet, Aymeric Guillot
The critical importance of the start phase in bicycle motocross (BMX) racing is increasingly acknowledged. Past experiments underlined that the internal lane of the starting gate provides a strong positional advantage. However, how lane position affects start performance and cognitive and somatic state anxiety remains unexplored. We examined the start performance and anxiety responses of youth national-level BMX riders in both experimental and ecological contexts. We used contextualization motor imagery routines to evaluate start performance and state anxiety from the internal and external lanes...
March 24, 2017: Journal of Sports Sciences
Qianmao Liang, Yongfei Chen, Kailin Yu, Cheng Chen, Shouxiang Zhang, Aoli Wang, Wei Wang, Hong Wu, Xiaochuan Liu, Beilei Wang, Li Wang, Zhenquan Hu, Wenchao Wang, Tao Ren, Shanchun Zhang, Qingsong Liu, Cai-Hong Yun, Jing Liu
Currently there are several irreversible BTK inhibitors targeting Cys481 residue under preclinical or clinical development. However, most of these inhibitors also targeted other kinases such as BMX, JAK3, and EGFR that bear the highly similar active cysteine residues. Through a structure-based drug design approach, we discovered a highly potent (IC50: 7 nM) irreversible BTK inhibitor compound 9 (CHMFL-BTK-01), which displayed a high selectivity profile in KINOMEscan (S score (35) = 0.00) among 468 kinases/mutants at the concentration of 1 μM...
March 2, 2017: European Journal of Medicinal Chemistry
Xiaofei Liang, Fengchao Lv, Beilei Wang, Kailin Yu, Hong Wu, Ziping Qi, Zongru Jiang, Cheng Chen, Aoli Wang, Weili Miao, Wenchao Wang, Zhenquan Hu, Juan Liu, Xiaochuan Liu, Zheng Zhao, Li Wang, Shanchuan Zhang, Zi Ye, Chu Wang, Tao Ren, Yinsheng Wang, Qingsong Liu, Jing Liu
BMX is a member of TEC family nonreceptor tyrosine kinase and is involved in a variety of critical physiological and pathological processes. Through combination of irreversible inhibitor design and type II inhibitor design approaches, we have discovered a highly selective and potent type II irreversible BMX kinase inhibitor compound 41 (CHMFL-BMX-078), which exhibited an IC50 of 11 nM by formation of a covalent bond with cysteine 496 residue in the DFG-out inactive conformation of BMX. It displayed a high selectivity profile (S score(1) = 0...
February 14, 2017: Journal of Medicinal Chemistry
Zrinka Rajic, Artak Tovmasyan, Otávio L de Santana, Isabelle N Peixoto, Ivan Spasojevic, Silmar A do Monte, Elizete Ventura, Júlio S Rebouças, Ines Batinic-Haberle
We disclose here the studies that preceded and guided the preparation of the metal-based, redox-active therapeutic Mn(III) meso-tetrakis(N-n-butoxyethylpyridyl)porphyrin, MnTnBuOE-2-PyP(5+) (BMX-001), which is currently in Phase I/II Clinical Trials at Duke University (USA) as a radioprotector of normal tissues in cancer patients. N-substituted pyridylporphyrins are ligands for Mn(III) complexes that are among the most potent superoxide dismutase mimics thus far synthesized. To advance their design, thereby improving their physical and chemical properties and bioavailability/toxicity profiles, we undertook a systematic study on placing oxygen atoms into N-alkylpyridyl chains via alkoxyalkylation reaction...
April 2017: Journal of Inorganic Biochemistry
Lee P Rylands, Howard T Hurst, Simon J Roberts, Robert W Graydon
Rylands, LP, Hurst, HT, Roberts, SJ, and Graydon, RW. The effect of "pumping" and "nonpumping" techniques on velocity production and muscle activity during field-based BMX cycling. J Strength Cond Res 31(2): 445-450, 2017-The aim of the current study was to determine if a technique called "pumping" had a significant effect on velocity production in Bicycle Motocross (BMX) cycling. Ten National standard male BMX riders fitted with surface electromyography (sEMG) sensors completed a timed lap of an indoor BMX track using the technique of pumping, and a lap without pumping...
February 2017: Journal of Strength and Conditioning Research
S Kothari, A Arunachalam, C Chen
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
Yu Shi, Wenchao Zhou, Lin Cheng, Cong Chen, Zhi Huang, Xiaoguang Fang, Qiulian Wu, Zhicheng He, Senlin Xu, Justin D Lathia, Yifang Ping, Jeremy N Rich, Xiu-Wu Bian, Shideng Bao
Glioblastoma (GBM) is the most malignant and lethal brain tumor harboring glioma stem cells (GSCs) that promote tumor propagation and therapeutic resistance. GSCs preferentially express several critical cell surface molecules that regulate the pro-survival signaling for maintaining the stem cell-like phenotype. Tetraspanin CD9 has recently been reported as a GSC biomarker that is relevant to the GSC maintenance. However, the underlying molecular mechanisms of CD9 in maintaining GSC property remain elusive. Herein, we report that CD9 stabilizes the IL-6 receptor glycoprotein 130 (gp130) by preventing its ubiquitin-dependent lysosomal degradation to facilitate the STAT3 activation in GSCs...
January 2017: Cell Death and Differentiation
Kelsey Stover, Tomoki Fukuyama, Ashlyn T Young, Michael A Daniele, Rebecca Oberley, James D Crapo, Wolfgang Bäumer
In this study, we topically administered two antioxidant compounds, the manganese-porphyrin-derivatives BMX-001 and BMX-010, in a mouse model of allergic dermatitis and compared the efficacy for reduction of itch and inflammation. In vitro effects of BMX-001 and BMX-010 on keratinocytes, bone marrow derived dendritic cells (BMDCs) and T-cells were initially analysed. For assessment of scratching behaviour, BMX-001 and BMX-010 (0.01 and 0.1 %) were topically applied 16 h and/or 1 h before compound 48/80 or toluene-2,4,-diisocyanate (TDI) challenge in a TDI induced mouse dermatitis model...
December 2016: Archives of Dermatological Research
Mohamed A Eldeeb, Richard P Fahlman
Cellular signaling leading to the initiation of apoptosis typically results in the activation of caspases, which in turn leads to the proteolytic generation of protein fragments with new or altered cellular functions. Increasing numbers of reports are demonstrating that the activity of many of these proteolytically activated protein fragments can be attenuated by their selective degradation by the N-end rule pathway. Here we report the first evidence that selective degradation of a caspase product by the N-end rule pathway can be modulated by phosphorylation...
October 21, 2016: Journal of Biological Chemistry
Ben Beck, Mark Stevenson, Stuart Newstead, Peter Cameron, Rodney Judson, Elton R Edwards, Andrew Bucknill, Marilyn Johnson, Belinda Gabbe
The aim of this study was to describe the crash characteristics and patient outcomes of a sample of patients admitted to hospital following bicycle crashes. Injured cyclists were recruited from the two major trauma services for the state of Victoria, Australia. Enrolled cyclists completed a structured interview, and injury details and patient outcomes were extracted from the Victorian State Trauma Registry (VSTR) and the Victorian Orthopaedic Trauma Outcomes Registry (VOTOR). 186 cyclists consented to participate in the study...
November 2016: Accident; Analysis and Prevention
Lee P Rylands, Simon J Roberts, Howard T Hurst
The aim of this study was to ascertain if gear ratio selection would have an effect on peak power and time to peak power production in elite Bicycle Motocross (BMX) cyclists. Eight male elite BMX riders volunteered for the study. Each rider performed three, 10-s maximal sprints on an Olympic standard indoor BMX track. The riders' bicycles were fitted with a portable SRM power meter. Each rider performed the three sprints using gear ratios of 41/16, 43/16 and 45/16 tooth. The results from the 41/16 and 45/16 gear ratios were compared to the current standard 43/16 gear ratio...
March 2017: European Journal of Sport Science
Lee P Rylands, Simon J Roberts, Howard T Hurst, Ian Bentley
The aims of this study were to analyse the optimal cadence for peak power production and time to peak power in bicycle motocross (BMX) riders. Six male elite BMX riders volunteered for the study. Each rider completed 3 maximal sprints at a cadence of 80, 100, 120 and 140 revs · min(-1) on a laboratory Schoberer Rad Messtechnik (SRM) cycle ergometer in isokinetic mode. The riders' mean values for peak power and time of power production in all 3 tests were recorded. The BMX riders produced peak power (1105 ± 139 W) at 100 revs · min(-1) with lower peak power produced at 80 revs · min(-1) (1060 ± 69 W, (F(2,15) = 3...
July 2017: Journal of Sports Sciences
Jenny Veitch, Jo Salmon, Kate Parker, Shaun Bangay, Benedicte Deforche, Anna Timperio
BACKGROUND: The neighbourhood environment such as the availability of parks are a key, but under-researched, influence on adolescents' physical activity. In addition to overall physical activity levels, park-based physical activity and park visitation is low in this age group. Thus, it is critical to identify park features that may encourage or discourage adolescents from visiting parks. This study used a novel methodology to identify key physical characteristics of parks that are perceived to be important for park visitation and park-based physical activity among adolescents...
July 4, 2016: International Journal of Behavioral Nutrition and Physical Activity
Monica E Burgett, Justin D Lathia, Patrick Roth, Amy S Nowacki, Deni S Galileo, Elena Pugacheva, Ping Huang, Amit Vasanji, Meizhang Li, Tatiana Byzova, Tom Mikkelsen, Shideng Bao, Jeremy N Rich, Michael Weller, Candece L Gladson
The secretion of soluble pro-angiogenic factors by tumor cells and stromal cells in the perivascular niche promotes the aggressive angiogenesis that is typical of glioblastoma (GBM). Here, we show that angiogenesis also can be promoted by a direct interaction between brain tumor cells, including tumor cells with cancer stem-like properties (CSCs), and endothelial cells (ECs). As shown in vitro, this direct interaction is mediated by binding of integrin αvβ3 expressed on ECs to the RGD-peptide in L1CAM expressed on CSCs...
July 12, 2016: Oncotarget
Hyoung-Joo Lee, Hye-Jung Kim, Daniel C Liebler
Analysis of small biological samples would benefit from an efficient microscale fractionation strategy that minimizes sample handling, transfer steps, and accompanying losses. Here we describe a microscale basic reverse phase liquid chromatographic (bRPLC) fractionation method that offers high reproducibility and efficiency for peptide mixtures from small (5-20 μg) samples. We applied our platform to detect differentially expressed proteins from lung tumor cell lines that are sensitive (11-18) and resistant (11-18R) to the tyrosine kinase inhibitor erlotinib...
July 1, 2016: Journal of Proteome Research
Lee P Rylands, Howard T Hurst, Simon J Roberts, Robert Graydon
The aim of the current study was to determine if a technique called 'pumping' had a significant effect on velocity production in BMX cycling. Ten National standard male BMX riders fitted with sEMG sensors completed a timed lap of an indoor BMX track using the technique of pumping, and a lap without pumping. The lap times were recorded for both trials and their surface sEMG recorded to ascertain any variation in muscle activation of the biceps brachii, triceps brachii, vastus lateralis and medial gastrocnemius...
May 28, 2016: Journal of Strength and Conditioning Research
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