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https://www.readbyqxmd.com/read/28734581/discovery-of-r-5-benzo-d-1-3-dioxol-5-yl-7-1-vinylsulfonyl-pyrrolidin-2-yl-methyl-7h-pyrrolo-2-3-d-pyrimidin-4-amine-b6-as-a-potent-bmx-inhibitor-for-the-treatment-of-nsclc
#1
Linhong He, Da Li, Chufeng Zhang, Peng Bai, Lijuan Chen
Described as a Btk inhibitor, ibrutinib also potently inhibits Bmx and EGFR, two good targets for lung cancer. Owing to its high CLogP (4.07) and low aqueous solubility (<0.01mg/ml), resulting in unfavorable bioavailability, ibrutinib requires high dosages to achieve good clinical response in the treatment of non-small cell lung cancer (NSCLC). In our effort to improve the CLogP of ibrutinib by structural optimization led to the discovery of a potent anti-cancer agent B6, with beneficial physicochemical parameters (CLogP=2...
July 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28650109/inducible-activation-of-fgfr2-in-adult-mice-promotes-bone-formation-after-bone-marrow-ablation
#2
Wei Xu, Fengtao Luo, Quan Wang, Qiaoyan Tan, Junlan Huang, Siru Zhou, Zuqiang Wang, Xianding Sun, Liang Kuang, Min Jin, Nan Su, Wanling Jiang, Liang Chen, Huabing Qi, Ying Zhu, Bo Chen, Hangang Chen, Shuai Chen, Yu Gao, Xiaoling Xu, Chuxia Deng, Lin Chen, Yangli Xie, Xiaolan Du
Apert syndrome is one of the most severe craniosynostoses, resulting from gain-of-function mutations in fibroblast growth factor receptor 2 (FGFR2). Previous studies have shown that gain-of-function mutations of FGFR2 (S252W or P253R) cause skull malformation of human Apert syndrome by affecting both chondrogenesis and osteogenesis, underscoring the key role of FGFR2 in bone development. However, the effects of FGFR2 on bone formation at the adult stage have not been fully investigated. To investigate the role of FGFR2 in bone formation, we generated mice with tamoxifen-inducible expression of mutant FGFR2 (P253R) at the adult stage...
June 26, 2017: Journal of Bone and Mineral Research: the Official Journal of the American Society for Bone and Mineral Research
https://www.readbyqxmd.com/read/28641100/bruton-s-tyrosine-kinase-btk-as-a-promising-target-in-solid-tumors
#3
REVIEW
J Molina-Cerrillo, T Alonso-Gordoa, P Gajate, E Grande
Bruton's tyrosine kinase (BTK) is a non-receptor intracellular kinase that belongs to the TEC-family tyrosine kinases together with bone marrow-expressed kinase (BMX), redundant-resting lymphocyte kinase (RLK), and IL-2 inducible T-Cell kinase (ITK). All these proteins play a key role in the intracellular signaling of both B and T lymphocytes. Recently, some preclinical data have demonstrated that BTK is present in certain tumor subtypes and in other relevant cells that are contributing to the tumor microenvironment such as dendritic cells, macrophages, myeloid derived suppressor cells and endothelial cells...
June 9, 2017: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/28631924/insight-into-the-bonding-mechanism-and-the-bonding-covalency-in-noble-gas-noble-metal-halides-an-nbo-nrt-investigation
#4
Guiqiu Zhang, Lei Fu, Hong Li, Xuchan Fan, Dezhan Chen
The bonding between noble gas and noble metal halide like hydrogen bonding (H-bonding) motivates us to investigate the bonding mechanism and the bonding covalency in NgMX (Ng = He, Ne, Ar, Kr, Xe, Rn; M = Cu, Ag, Au; X = F, Cl, Br, I) complexes using natural bond orbital (NBO) and natural resonance theory (NRT) methods. In this study, we introduce the new resonance bonding model in H-bonding into NgMX bonding. We provide strong evidence for resonance bonding involving two important resonance structures: Ng: M-X ↔ Ng(+)-M :X(-) in each of NgMX complexes, originating in the nNg → σ*MX hyperconjugative interaction...
July 3, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28628824/structure-activity-relationship-investigation-for-benzonaphthyridinone-derivatives-as-novel-potent-bruton-s-tyrosine-kinase-btk-irreversible-inhibitors
#5
Beilei Wang, Yuanxin Deng, Yongfei Chen, Kailin Yu, Aoli Wang, Qianmao Liang, Wei Wang, Cheng Chen, Hong Wu, Chen Hu, Weili Miao, Wooyoung Hur, Wenchao Wang, Zhenquan Hu, Ellen L Weisberg, Jinhua Wang, Tao Ren, Yinsheng Wang, Nathanael S Gray, Qingsong Liu, Jing Liu
Through a structure-based drug design approach, a tricyclic benzonaphthyridinone pharmacophore was used as a starting point for carrying out detailed medicinal structure-activity relationhip (SAR) studies geared toward characterization of a panel of proposed BTK inhibitors, including 6 (QL-X-138), 7 (BMX-IN-1) and 8 (QL47). These studies led to the discovery of the novel potent irreversible BTK inhibitor, compound 18 (CHMFL-BTK-11). Kinetic analysis of compound 18 revealed an irreversible binding efficacy (kinact/Ki) of 0...
September 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28595865/profiling-of-translational-and-rotational-head-accelerations-in-youth-bmx-with-and-without-neck-brace
#6
Howard T Hurst, Lee Rylands, Stephen Atkins, Kevin Enright, Simon J Roberts
OBJECTIVES: To investigate the influence of BMX helmets and neck braces on translational and rotational accelerations in youth riders. DESIGN: Mixed model, repeated measure and correlation. METHODS: Twenty three competitive youth BMX riders classified by age group (6-9 years, 10-13 years and 14-18 years) completed 6 laps of an indoor BMX track at race pace, 3 laps without a neck brace (NB) and 3 without brace (WB). A triaxial accelerometer with gyroscope was placed behind the right ear to determine the mean number of accelerations, translational and rotational, of the head between conditions and by age group...
May 25, 2017: Journal of Science and Medicine in Sport
https://www.readbyqxmd.com/read/28514765/bmx-etk-promotes-cell-proliferation-and-tumorigenicity-of-cervical-cancer-cells-through-pi3k-akt-mtor-and-stat3-pathways
#7
Yuanyuan Li, Nan Cui, Peng-Sheng Zheng, Wen-Ting Yang
Bone marrow X-linked kinase (BMX, also known as Etk) has been reported to be involved in cell proliferation, differentiation, apoptosis, migration and invasion in several types of tumors, but its role in cervical carcinoma remains poorly understood. In this study, we showed that BMX expression exhibits a gradually increasing trend from normal cervical tissue to cervical cancer in situ and then to invasive cervical cancer tissue. Through BMX-IN-1, a potent and irreversible BMX kinase inhibitor, inhibited the expression of BMX, the cell proliferation was significantly decreased...
April 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/28462479/age-has-a-minimal-effect-on-the-impact-performance-of-field-used-bicycle-helmets
#8
Alyssa L DeMarco, Craig A Good, Dennis D Chimich, Jeff A Bakal, Gunter P Siegmund
Helmet manufacturers recommend replacing a bicycle helmet after an impact or after anywhere from 2 to 10 years of use. The goal of this study was to quantify the effect of helmet age on peak headform acceleration during impact attenuation testing of field-used bicycle helmets. Helmets were acquired by donation from consumers and retail stores, and were included in the study if they were free of impact-related damage, had a legible manufacture date label, and were certified to at least one helmet standard. Helmets (n = 770) spanning 0-26 years old were drop tested to measure peak linear headform acceleration during impacts to the right and left front regions of the helmets at two impact speeds (3...
May 1, 2017: Annals of Biomedical Engineering
https://www.readbyqxmd.com/read/28438385/small-molecules-inhibit-stat3-activation-autophagy-and-cancer-cell-anchorage-independent-growth
#9
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
https://www.readbyqxmd.com/read/28427134/-role-of-bone-marrow-tyrosine-kinase-on-chromosome-x-in-the-production-of-pro-inflammatory-cytokines-from-mouse-mononuclear-macrophages-raw264-7-induced-by-endotoxin-lipopolysaccharide-and-its-mechanism
#10
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
https://www.readbyqxmd.com/read/28422715/a-novel-bmx-variant-promotes-tumor-cell-growth-and-migration-in-lung-adenocarcinoma
#11
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...
May 16, 2017: Oncotarget
https://www.readbyqxmd.com/read/28401017/mir-495-promotes-the-chemoresistance-of-sclc-through-the-epithelial-mesenchymal-transition-via-etk-bmx
#12
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
https://www.readbyqxmd.com/read/28337944/the-influence-of-gate-start-position-on-physical-performance-and-anxiety-perception-in-expert-bmx-athletes
#13
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
https://www.readbyqxmd.com/read/28315597/discovery-of-n-3-5-3-acrylamido-4-morpholine-4-carbonyl-phenyl-amino-1-methyl-6-oxo-1-6-dihydropyridin-3-yl-2-methylphenyl-4-tert-butyl-benzamide-chmfl-btk-01-as-a-highly-selective-irreversible-bruton-s-tyrosine-kinase-btk-inhibitor
#14
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...
May 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28140585/discovery-of-2-3-acrylamido-4-methylphenyl-amino-n-2-methyl-5-3-4-5-trimethoxybenzamido-phenyl-4-methylamino-pyrimidine-5-carboxamide-chmfl-bmx-078-as-a-highly-potent-and-selective-type-ii-irreversible-bone-marrow-kinase-in-the-x-chromosome-bmx-kinase-inhibitor
#15
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
https://www.readbyqxmd.com/read/28131001/challenges-encountered-during-development-of-mn-porphyrin-based-potent-redox-active-drug-and-superoxide-dismutase-mimic-mntnbuoe-2-pyp-5-and-its-alkoxyalkyl-analogues
#16
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
https://www.readbyqxmd.com/read/28125546/the-effect-of-pumping-and-nonpumping-techniques-on-velocity-production-and-muscle-activity-during-field-based-bmx-cycling
#17
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
https://www.readbyqxmd.com/read/27973175/treatment-patterns-biomarker-testing-bmx-practices-and-healthcare-resource-use-hcru-in-patients-with-advanced-non-small-cell-lung-cancer-nsclc-in-taiwan
#18
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
https://www.readbyqxmd.com/read/27740621/tetraspanin-cd9-stabilizes-gp130-by-preventing-its-ubiquitin-dependent-lysosomal-degradation-to-promote-stat3-activation-in-glioma-stem-cells
#19
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
https://www.readbyqxmd.com/read/27709295/topically-applied-manganese-porphyrins-bmx-001-and-bmx-010-display-a-significant-anti-inflammatory-response-in-a-mouse-model-of-allergic-dermatitis
#20
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
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