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https://www.readbyqxmd.com/read/29785088/insight-into-resistance-mechanism-of-anaplastic-lymphoma-kinase-to-alectinib-and-jh-viii-157-02-caused-by-g1202r-solvent-front-mutation
#1
Han Wang, Yao Wang, Wentao Guo, Bin Du, Xiaobing Huang, Riping Wu, Baoyu Yang, Xiaoyan Lin, Yilan Wu
Background: Mutated anaplastic lymphoma kinase (ALK) drives the development of advanced non-small cell lung cancer (NSCLC). Most reported small-molecule inhibitors targeting the ALK domain do not display good inhibition of the G1202R solvent front mutation. The solvent front mutation was assumed to hinder drug binding. However, a different fact could be uncovered by the simulations reported in this study through a structural analog of alectinib (JH-VIII-157-02), which demonstrated potent effects against the G1202R mutation...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29784364/protein-binding-protection-in-combination-with-dna-masking-for-sensitive-and-reliable-transcription-factor-detection
#2
Xiaowen Xu, Lei Wang, Desong Zhu, Yan Wang, Wei Jiang
Sensitive and reliable detection of transcription factors (TFs) is crucial for disease diagnosis and drug discovery. Herein, a protein binding protection in combination with DNA masking-based strategy is developed for sensitive and reliable detection of NF-κB p50. First, NF-κB p50 binds specifically to a hairpin probe to form a protein-DNA complex. Then, the formed complex protects the hairpin probe from hybridization with the masking strand and subsequently triggers the cascade signal amplification of strand displacement amplification (SDA) and exponential rolling circle amplification (ERCA)...
August 15, 2018: Talanta
https://www.readbyqxmd.com/read/29784049/identification-and-therapeutic-modulation-of-a-pro-inflammatory-subset-of-disease-associated-microglia-in-alzheimer-s-disease
#3
Srikant Rangaraju, Eric B Dammer, Syed Ali Raza, Priyadharshini Rathakrishnan, Hailian Xiao, Tianwen Gao, Duc M Duong, Michael W Pennington, James J Lah, Nicholas T Seyfried, Allan I Levey
BACKGROUND: Disease-associated-microglia (DAM) represent transcriptionally-distinct and neurodegeneration-specific microglial profiles with unclear significance in Alzheimer's disease (AD). An understanding of heterogeneity within DAM and their key regulators may guide pre-clinical experimentation and drug discovery. METHODS: Weighted co-expression network analysis (WGCNA) was applied to existing microglial transcriptomic datasets from neuroinflammatory and neurodegenerative disease mouse models to identify modules of highly co-expressed genes...
May 21, 2018: Molecular Neurodegeneration
https://www.readbyqxmd.com/read/29782863/analysis-of-mulberry-leaf-components-in-the-treatment-of-diabetes-using-network-pharmacology
#4
Qi Ge, Liang Chen, Min Tang, Shu Zhang, Lu Gao, Shangshang Ma, Lanlan Liu, Ming Kong, Qin Yao, Keping Chen, Fan Feng
Mulberry leaves are one of the most commonly used medicinal and herbaceous traditional Chinese medicines that are currently considered for the treatment of diabetes mellitus and its complications. The alkaloids, flavonoids, and polysaccharides in mulberry leaves impart regulatory effects on blood sugar levels. To identify the hypoglycemia-related active components in mulberry leaves and their targets, the present study conducted gas chromatography-mass spectrometer (GC/MS), which identified 202 components of mulberry leaf, of which 22 components may have significant curative effects on diabetes mellitus and its complications and chronic inflammation...
May 18, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29776956/integrin-%C3%AE-3-inhibition-enhances-the-antitumor-activity-of-alk-inhibitor-in-alk-rearranged-nsclc
#5
Ka-Won Noh, Insuk Sohn, Ji-Young Song, Hyun-Tae Shin, Yu Jin Kim, Kyungsoo Jung, Minjung Sung, Mingi Kim, Sungbin An, Joungho Han, Se-Hoon Lee, Mi-Sook Lee, Yoon-La Choi
BACKGROUND: Anaplastic lymphoma kinase (ALK)-positive cancers are sensitive to small molecule ALK kinase inhibitors, but most cases experience failure following treatment. Hence, additional drug targets and combination therapeutic treatments are needed. We investigated gene expression that is regulated by the expression of ALK and explored its roles in cancer progression and therapeutic implication. PATIENTS AND METHODS: We screened ALK-rearranged non-small cell lung cancer (NSCLC) cases using immunohistochemistry and fluorescence in situ hybridization, and then conducted multiplex gene expression analysis...
May 18, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29768207/defective-replication-stress-response-is-inherently-linked-to-the-cancer-stem-cell-phenotype
#6
Daniel J McGrail, Curtis Chun-Jen Lin, Hui Dai, Wei Mo, Yang Li, Clifford Stephan, Peter Davies, Zhimin Lu, Gordon B Mills, Ju-Seog Lee, Shiaw-Yih Lin
Extensive spontaneous DNA damage from oncogene-induced replication stress is ubiquitous in precancerous lesions. While this damage induces differentiation, senescence, or apoptosis in normal cells, defects in DNA replication stress response (RSR) allow cells to continue proliferating, ultimately leading to early tumorigenesis. Using systems-level approaches, we developed a replication stress response defect gene signature that predicted risk of cancer development from hyperplastic lesions. Intriguingly, we found that replication stress response defects rewire non-malignant cells into a cancer stem cell (CSC)-like state, and analysis of CSCs indicated that they inherently harbor replication stress response defects...
May 15, 2018: Cell Reports
https://www.readbyqxmd.com/read/29768183/ndrg1-disruption-alleviates-cisplatin-sodium-glycididazole-induced-dna-damage-response-and-apoptosis-in-ercc1-defective-lung-cancer-cells
#7
Lang He, Kang Liu, Xiaoshan Wang, Hong Chen, Jin Zhou, Xun Wu, Tao Liu, Yongxue Yang, Xuemei Yang, Dandan Cui, Guiqin Song, Jianguo Lei, Jun Wang
BACKGROUND: Resistance to platinum-based chemotherapy becomes a major obstacle in lung cancer treatment. Compensatory activation of nucleotide excision repair (NER) pathway is the major mechanism accounting for cisplatin-resistance. We aimed at identifying additional regulators in NER-mediated chemoresistance in a hypoxic setting induced by sodium glycididazole (CMNa)-sensitized cisplatin chemotherapy of non-small cell lung cancer (NSCLC). METHODS: We performed an RNA-sequencing (RNA-Seq) analysis to identify the genes whose expression had been differentially regulated in NER-deficient cells that had been treated by cisplatin/CMNa...
May 13, 2018: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/29766327/characterization-of-carfilzomib-resistant-non-small-cell-lung-cancer-cell-lines
#8
Neale T Hanke, Elliot Imler, Marilyn T Marron, Bruce E Seligmann, Linda L Garland, Amanda F Baker
PURPOSE: We previously showed that carfilzomib (CFZ) has potent anti-proliferative and cytotoxic activity in a broad range of lung cancer cell lines. Here we investigate possible mechanisms of CFZ acquired resistance in lung cancer cell lines. METHODS: CFZ-resistant non-small cell lung cancer (NSCLC) cell lines were developed by exposing A549 and H520 cells to stepwise increasing concentrations of CFZ. Resistance to CFZ and cross-resistance to bortezomib and other chemotherapy drugs was measured using the MTT assay...
May 15, 2018: Journal of Cancer Research and Clinical Oncology
https://www.readbyqxmd.com/read/29765556/antibody-assisted-target-identification-reveals-afatinib-an-egfr-covalent-inhibitor-down-regulating-ribonucleotide-reductase
#9
Cheng-Han Yu, Chi-Chi Chou, Hsin-Fang Tu, Wei-Chieh Huang, Ya-Yeh Ho, Kay-Hooi Khoo, Ming-Shyue Lee, Geen-Dong Chang
Afatinib, used for the first-line treatment of non-small-cell lung carcinoma (NSCLC) patients with distinct epidermal growth factor receptor (EGFR) mutations, inactivates EGFR by mimicking ATP structure and forming a covalent adduct with EGFR. We developed a method to unravel potential targets of afatinib in NSCLC cells through immunoprecipitation of afatinib-labeling proteins with anti-afatinib antiserum and mass spectrometry analysis. Ribonucleotide reductase (RNR) is one of target proteins of afatinib revealed by this method...
April 20, 2018: Oncotarget
https://www.readbyqxmd.com/read/29765515/cancer-cell-selective-clathrin-mediated-endocytosis-of-aptamer-decorated-nanoparticles
#10
Shira Engelberg, Julia Modrejewski, Johanna G Walter, Yoav D Livney, Yehuda G Assaraf
Lung cancer is the leading cause of cancer mortality worldwide, resulting in 88% deaths of all diagnosed patients. Hence, novel therapeutic modalities are urgently needed. Single-stranded oligonucleotide-based aptamers (APTs) are excellent ligands for tumor cell targeting. However, the molecular mechanisms underlying their internalization into living cells have been poorly studied. Towards the application of APTs for active drug targeting to cancer cells, we herein studied the mechanism underlying S15-APT internalization into human non-small cell lung cancer A549 cells...
April 20, 2018: Oncotarget
https://www.readbyqxmd.com/read/29763580/detailed-investigation-of-anticancer-activity-of-sulfamoyl-benz-sulfon-amides-and-1h-pyrazol-4-yl-benzamides-an-experimental-and-computational-study
#11
Jamshed Iqbal, Syeda Abida Ejaz, Mariya Al-Rashida, Aamer Saeed
Cancer is the second leading cause of mortality worldwide. Therapeutic approach to cancer is a multi-faceted one, whereby many cellular/enzymatic pathways have been discovered as important drug targets for the treatment of cancer. A major disadvantage of most of the currently available anticancer drugs is their non-selective cytotoxicity towards cancerous as well as healthy cells. Another major hurdle in cancer therapy is the development of resistance to anticancer drugs. This necessitates the discovery of new molecules with potent and selective cytotoxic activity towards only cancerous cells, with minimum or no damage to the normal/healthy cells...
May 12, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29763465/expression-of-the-three-components-of-linear-ubiquitin-assembly-complex-in-breast-cancer
#12
Amirhossein Kharman-Biz, Hui Gao, Reza Ghiasvand, Lars-Arne Haldosen, Kazem Zendehdel
Proteins belonging to the linear ubiquitin assembly complex (LUBAC) are believed to be important in tumorigenesis. LUBAC has been demonstrated to be composed of RBCK1, RNF31 and SHARPIN. The aim of this study was to explore all members of the LUBAC complex as novel biomarkers in breast cancer. We have already reported that RNF31 mRNA levels are higher in breast cancer samples compared to adjacent non-tumor tissue. In this study we extend these findings by demonstrating that the mRNA levels of RBCK1 and SHARPIN are also higher in tumors compared to adjacent non-tumor tissue in the same cross sectional study of samples (p < 0...
2018: PloS One
https://www.readbyqxmd.com/read/29754040/synthetic-cannabinoid-bb-22-quchic-human-hepatocytes-metabolism-with-liquid-chromatography-high-resolution-mass-spectrometry-detection
#13
Jeremy Carlier, Xingxing Diao, Marilyn A Huestis
Clandestine laboratories continue producing new synthetic cannabinoids that mimic and magnify natural cannabinoids effects to circumvent drug scheduling legislation. New synthetic cannabinoids are highly potent and responsible for many acute intoxications and deaths. Characterization of metabolic pathways is critical to identify metabolite markers whose detection can prove intake. BB-22 is a new potent synthetic cannabinoid whose toxicological and metabolic properties are currently unavailable. Analytical methods require constant updating and are challenging due to extensive synthetic cannabinoid metabolism and low marker concentrations...
May 7, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29749447/chemoresistance%C3%A2-related-long-non%C3%A2-coding-rna-expression-profiles-in-human-breast-cancer-cells
#14
Lei Huang, Lihua Zeng, Jiahui Chu, Pengfei Xu, Mingming Lv, Juan Xu, Juan Wen, Wenqu Li, Luyu Wang, Xiaowei Wu, Ziyi Fu, Hui Xie, Shui Wang
Breast cancer is the most commonly diagnosed cancer and the leading cause of cancer death in females worldwide. Chemoresistance has been a major reason for the drug therapy failure. The present study performed a microarray analysis between MCF‑7 and MCF‑7/adriamycin (ADR) cells, and intended to identify long non‑coding (lnc)RNA expression character in drug resistant breast cancer cells. MCF‑7/ADR cells were induced from MCF‑7 cells via pulse‑selection with doxorubicin for 4 weeks, and the resistance to doxorubicin of ADR cells was confirmed by MTT assay...
April 27, 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29746394/pharmacokinetics-of-doripenem-in-healthy-koreans-and-monte-carlo-simulations-to-explore-optimal-dosage-regimens-in-patients-with-normal-and-enhanced-renal-function
#15
So Won Kim, Sangmin Choe, Dong Jin Kim, Dae Young Zang, Dong-Hwan Lee
BACKGROUND: Dose adjustment is often required in patients with normal or enhanced renal function. The aim of this study is to investigate the pharmacokinetic (PK) properties of doripenem and explore optimal dosing regimens in patients with normal or enhanced renal function according to various minimum inhibitory concentrations (MIC). METHODS: The authors conducted a clinical trial and analyzed PK samples in 11 healthy Korean subjects applying non-compartmental analysis (NCA) and a population approach...
May 9, 2018: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/29745330/metabolism-of-synthetic-cannabinoids-encountered-in-clinical-casework-major-in-vivo-metabolites-of-jwh-007-jwh-019-jwh-203-jwh-307-ur-144-xlr-11-am-2201-mam-2201-and-am-694-in-human-urine-using-lc-ms-ms
#16
Volker Auwarter, Melanie Hutter, S Broecker, Stefan Kneisel, Floria Franz, Simon D Brandt
BACKGROUND: `Herbal mixtures` containing synthetic cannabinoid receptor agonists (SCRAs) are promoted as legal alternative to marihuana and are easily available via the Internet. Keeping analytical methods for the detection of these SCRAs up-to-date is a continuous challenge for clinicians and toxicologists due to the high diversity of the chemical structures and the frequent emergence of new compounds. Since many SCRAs are extensively metabolized, analytical methods used for urine testing require previous identification of the major metabolites of each compound...
May 9, 2018: Current Pharmaceutical Biotechnology
https://www.readbyqxmd.com/read/29743718/expressional-analysis-of-disease-relevant-signalling-pathways-in-primary-tumours-and-metastasis-of-head-and-neck-cancers
#17
Dorothee Goesswein, Negusse Habtemichael, Aslihan Gerhold-Ay, Johanna Mazur, Désirée Wünsch, Shirley K Knauer, Julian Künzel, Christoph Matthias, Sebastian Strieth, Roland H Stauber
Head and neck squamous cell carcinoma (HNSCC) often metastasize to lymph nodes resulting in poor prognosis for patients. Unfortunately, the underlying molecular mechanisms contributing to tumour aggressiveness, recurrences, and metastasis are still not fully understood. However, such knowledge is key to identify biomarkers and drug targets to improve prognosis and treatments. Consequently, we performed genome-wide expression profiling of 15 primary HNSSCs compared to corresponding lymph node metastases and non-malignant tissue of the same patient...
May 9, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29740493/bioinformatic-analysis-and-prediction-of-the-function-and-regulatory-network-of-long-non-coding-rnas-in-hepatocellular-carcinoma
#18
Ming-Rong Cao, Ze-Ping Han, Ji-Ming Liu, Yu-Guang Li, Yu-Bing Lv, Jia-Bin Zhou, Jin-Hua He
Computational analysis and bioinformatics have significantly advanced the ability of researchers to process and analyze biological data. Molecular data from human and model organisms may facilitate drug target validation and identification of biomarkers with increased predictive accuracy. The aim of the present study was to investigate the function of long non-coding RNAs (lncRNAs) in hepatocellular carcinoma (HCC) using online databases, and to predict their regulatory mechanism. HCC-associated lncRNAs, their downstream transcription factors and microRNAs (miRNAs/miRs), as well as the HCC-associated target genes, were identified using online databases...
May 2018: Oncology Letters
https://www.readbyqxmd.com/read/29739130/a-cross-sectional-analysis-of-patterns-and-predictors-of-medication-adherence-in-bipolar-disorder-single-center-experience-from-south-india
#19
Nivedhitha Selvakumar, Vikas Menon, Shivan Kattimani
Objective: Our objective was to determine patterns and predictors of medication adherence in bipolar disorder. Methods: Between August 2015 and December 2016, we recruited 160 patients with a diagnosis of bipolar disorder as per International Classification of Diseases-10: Clinical Descriptions and Diagnostic Guidelines. The diagnosis was further confirmed by using the MINI International Neuropsychiatric Inventory. All of them were currently in remission (confirmed by standard measures) and on stable dosing of medication for at least a year...
May 31, 2018: Clinical Psychopharmacology and Neuroscience: the Official Scientific Journal of the Korean College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29730258/a-combination-of-interdisciplinary-analytical-tools-for-evaluation-of-multi-layered-coatings-on-medical-grade-stainless-steel-for-biomedical-applications
#20
Uroš Maver, Klodian Xhanari, Marko Žižek, Dorota Korte, Lidija Gradišnik, Mladen Franko, Matjaž Finšgar
In this comprehensive study several analytical techniques were used in order to evaluate multi--layered biomedical surface coatings composed of a drug (diclofenac) and a polymer (chitosan). Such a thorough examination is of paramount importance in order to assure safety and prove efficiency of potential biomedical materials already at the in vitro level, hence leading to their potentially faster introduction to clinical trials. For the first time a novel technique based on thermal diffusivity and conductivity measurement (photothermal beam deflection spectroscopy - BDS) was employed in order to analyse in a non-destructive way the thickness of respective layers, together with their thermal diffusivity and conductivity...
May 3, 2018: European Journal of Pharmaceutics and Biopharmaceutics
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