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https://www.readbyqxmd.com/read/28822335/specificity-protein-1-modulated-superoxide-dismutase-2-enhances-temozolomide-resistance-in-glioblastoma-which-is-independent-of-o-6-methylguanine-dna-methyltransferase
#1
Kwang-Yu Chang, Tsung-I Hsu, Che-Chia Hsu, Shan-Yin Tsai, Jr-Jiun Liu, Shao-Wen Chou, Ming-Sheng Liu, Jing-Ping Liou, Chiung-Yuan Ko, Kai-Yun Chen, Jan-Jong Hung, Wen-Chang Chang, Cheng-Keng Chuang, Tzu-Jen Kao, Jian-Ying Chuang
Acquisition of temozolomide (TMZ) resistance is a major factor leading to the failure of glioblastoma (GBM) treatment. The exact mechanism by which GBM evades TMZ toxicity is not always related to the expression of the DNA repair enzyme O(6)-methylguanine-DNA methyltransferase (MGMT), and so remains unclear. In this study, TMZ-resistant variants derived from MGMT-negative GBM clinical samples and cell lines were studied, revealing there to be increased specificity protein 1 (Sp1) expression associated with reduced reactive oxygen species (ROS) accumulation following TMZ treatment...
August 12, 2017: Redox Biology
https://www.readbyqxmd.com/read/28822333/virtual-screening-and-repositioning-of-inconclusive-molecules-of-beta-lactamase-bioassays-a-data-mining-approach
#2
Akshata Gad, Andrew Titus Manuel, Jinuraj K R, Lijo John, Sajeev R, Shanmuga Priya V G, Abdul Jaleel U C
This study focuses on the best possible way forward in utilizing inconclusive molecules of PubChem bioassays AID 1332, AID 434987 and AID 434955, which are related to beta-lactamase inhibitors of Mycobacterium tuberculosis (Mtb). The inadequacy in the experimental methods that were observed during the invitro screening resulted in an inconclusive dataset. This could be due to certain moieties present within the molecules. In order to reconsider such molecules, insilico methods can be suggested in place of invitro methods For instance, datamining and medicinal chemistry methods: have been adopted to prioritise the inconclusive dataset into active or inactive molecules...
July 29, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28822281/an-integrative-study-to-identify-novel-scaffolds-for-sphingosine-kinase-1-inhibitors
#3
Marcela Vettorazzi, Emilio Angelina, Santiago Lima, Tomas Gonec, Jan Otevrel, Pavlina Marvanova, Tereza Padrtova, Petr Mokry, Pavel Bobal, Lina M Acosta, Alirio Palma, Justo Cobo, Janette Bobalova, Jozef Csollei, Ivan Malik, Sergio Alvarez, Sarah Spiegel, Josef Jampilek, Ricardo D Enriz
Sphingosine kinase 1 (SphK1), the enzyme that produces the bioactive sphingolipid metabolite, sphingosine-1-phosphate, is a promising new molecular target for therapeutic intervention in cancer and inflammatory diseases. In view of its importance, the main objective of this work was to find new and more potent inhibitors for this enzyme possessing different structural scaffolds than those of the known inhibitors. Our theoretical and experimental study has allowed us to identify two new structural scaffolds (three new compounds), which could be used as starting structures for the design and then the development of new inhibitors of SphK1...
August 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28822269/correlation-of-cholinergic-drug-induced-quenching-of-acetylcholinesterase-bound-thioflavin-t-fluorescence-with-their-inhibition-activity
#4
Mullah Muhaiminul Islam, Mostofa Ataur Rohman, Arun Bahadur Gurung, Atanu Bhattacharjee, Kripamoy Aguan, Sivaprasad Mitra
The development of new acetylcholinesterase inhibitors (AChEIs) and subsequent assay of their inhibition efficiency is considered to be a key step for AD treatment. The fluorescence intensity of thioflavin-T (ThT) bound in the active site of acetylcholinesterase (AChE) quenches substantially in presence of standard AChEI drugs due to the dynamic replacement of the fluorophore from the AChE active site as confirmed from steady state emission as well as time-resolved fluorescence anisotropy measurement and molecular dynamics simulation in conjunction with docking calculation...
August 5, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28822192/-taurine-affects-expression-of-icam-1-vcam-1-by-p38-pathway-in-hypoxic-endothelial-cells
#5
Xiao-Dan Zhang, Shu-Ya Zhao, Yun-Lin Li, Da-Ling Zhu, Ru Zhang, Jie-Jing Sheng, Shu-Jing Wang
To investigate the effect of taurine(Tau) on ICAM-1, VCAM-1 by p-p38 pathway in bovine pulmonary artery endothelial cells(PAECs) and explore its mechanism of action. Generation 4-12 cells in primary cultures of PAECs were used in experiments and divided into five groups: control group, hypoxia(hyp) group, inhibitor(SB203580) group, treatment(Tau) group, and treatment+inhibitor(SB+Tau) group. The concentration of Tau:100 mmol•L⁻¹; p38 inhibitor SB203580: 20 μmol•L⁻¹; and the treatment time was 12 h...
June 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28822080/soluble-epoxide-hydrolase-inhibition-attenuates-mptp-induced-neurotoxicity-in-the-nigrostriatal-dopaminergic-system-involvement-of-%C3%AE-synuclein-aggregation-and-er-stress
#6
Hui-Ju Huang, Yi-Ting Wang, Hui-Ching Lin, Yi-Hsuan Lee, Anya Maan-Yuh Lin
Soluble epoxide hydrolase (sEH) is widely expressed in the mammalian brain and possesses dual enzymatic activities, including C-terminal epoxide hydrolase (C-EH) which degrades epoxyeicosatrienoic acid (EET), a beneficial arachidonic acid metabolite. In the present study, the neuroprotective effect of sEH inhibition on 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced neurodegeneration of nigrostriatal dopaminergic system was investigated using genetic and pharmacological approaches. MPTP (15 mg/kg) was intraperitoneally injected in sEH knockout (KO) mice and C57BL/6J mice as wild-type (WT) mice...
August 18, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28822077/increased-serum-levels-of-fetuin-b-in-patients-with-coronary-artery-disease
#7
Kefu Zhu, Yuming Wang, Pengqin Shu, Qinyi Zhou, Jinzhou Zhu, Wenjing Zhou, Changqing Du, Chenkai Xu, Xiaowei Liu, Lijiang Tang
BACKGROUND: Recent evidence indicates a pivotal role for fetuin B, one of the cystatin superfamily of cysteine protease inhibitors, in the pathogenesis of metabolic diseases. This study investigated whether serum fetuin B levels are associated with the presence of coronary artery disease. METHODS: Serum fetuin B levels were assessed in 87 patients with coronary artery disease (41 with acute coronary syndromes and 46 with stable angina pectoris) and 87 healthy controls using an enzyme-linked immunosorbent assay...
August 19, 2017: Endocrine
https://www.readbyqxmd.com/read/28822076/studies-of-the-benzopyran-class-of-selective-cox-2-inhibitors-using-3d-qsar-and-molecular-docking
#8
Dharmendra K Yadav, Saloni, Praveen Sharma, Sanjeev Misra, Harpreet Singh, Ricardo L Mancera, Kang Kim, Cheongyun Jang, Mi-Hyun Kim, Horacio Pérez-Sánchez, Eun Ha Choi, Surendra Kumar
The Gaussian-based 3D-QSAR studies for 58 selective COX-2 (cyclooxygenase-2) inhibitors belonging to benzopyran chemical class were performed. Partial least squares analysis produced statistically significant model with (R training(2)  = 0.866) and predictability (Q training(2)  = 0.66, Q test(2)  = 0.846). The 3D-QSAR model includes steric, electrostatic, hydrophobic, and hydrogen bond acceptor field indicators, whereas the potential field contributions indicate that the steric and hydrophobic features of the molecules play an important role in governing their biological activity...
August 18, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28822058/immune-dysfunction-in-non-hodgkin-lymphoma-avenues-for-new-immunotherapy-based-strategies
#9
REVIEW
Lorenzo Falchi
PURPOSE OF THIS REVIEW: The present review focuses on key aspects of non-Hodgkin lymphoma (NHL) evasion of immune surveillance and how these can be leveraged to devise effective immunotherapy strategies. RECENT FINDINGS: In recent years, significant progress has been made in the field of cancer immunotherapy. In particular, the remarkable clinical results of anti-programmed death (PD)-1/PD-ligand (L)1 antibodies are revolutionizing the treatment approach to multiple solid and hematologic tumors...
August 18, 2017: Current Hematologic Malignancy Reports
https://www.readbyqxmd.com/read/28822039/stimulation-of-nachr%C3%AE-7-receptor-inhibits-tnf-synthesis-and-secretion-in-response-to-lps-treatment-of-mast-cells-by-targeting-erk1-2-and-tace-activation
#10
F Guzmán-Mejía, C López-Rubalcava, C González-Espinosa
The cholinergic anti-inflammatory pathway is recognized as one of the main mechanisms of neuromodulation of the immune system. Activation of the α7 nicotinic acetylcholine receptor (nAchRα7) suppresses cytokine synthesis in distinct immune cells but the molecular mechanisms behind this effect remain to be fully described. Mast cells (MCs) are essential players of allergic reactions and innate immunity responses related to chronic inflammation. Activation of TLR4 receptor in MCs leads to the rapid secretion of pre-synthesized TNF from intracellular pools and to the activation of NFκB, necessary for de novo synthesis of TNF and other cytokines...
August 18, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28822019/gypenoside-ix-suppresses-p38-mapk-akt-nf%C3%AE%C2%BAb-signaling-pathway-activation-and-inflammatory-responses-in-astrocytes-stimulated-by-proinflammatory-mediators
#11
Xiaoshuang Wang, Liu Yang, Li Yang, Faping Xing, Hua Yang, Liyue Qin, Yunyi Lan, Hui Wu, Beibei Zhang, Hailian Shi, Cheng Lu, Fei Huang, Xiaojun Wu, Zhengtao Wang
Gypenoside IX (GP IX) is a pure compound isolated from Panax notoginseng. Gypenosides have been implicated to benefit the recovery of enormous neurological disorders. By suppressing the activation of astrocytes, gypenosides can improve the cognitive impairment. However, so far, little is known about whether GP IX could restrain the inflammatory responses in astrocytes or reactive astrogliosis. In present study, the anti-inflammatory effects of GP IX were investigated in reactive astrocytes induced by proinflammatory mediators both in vitro and in vivo...
August 18, 2017: Inflammation
https://www.readbyqxmd.com/read/28822012/mtor-co-targeting-strategies-for-head-and-neck-cancer-therapy
#12
Zhiyong Wang, Juan Callejas Valera, Xuefeng Zhao, Qianming Chen, J Silvio Gutkind
Head and neck squamous cell carcinoma (HNSCC) is the sixth most common malignancy worldwide. There is an urgent need to develop effective therapeutic approaches to prevent and treat HNSCC. Recent deep sequencing of the HNSCC genomic landscape revealed a multiplicity and diversity of genetic alterations in this malignancy. Although a large variety of specific molecules were found altered in each individual tumor, they all participate in only a handful of driver signaling pathways. Among them, the PI3K/mTOR pathway is the most frequently activated, which plays a central role in cancer initiation and progression...
August 18, 2017: Cancer Metastasis Reviews
https://www.readbyqxmd.com/read/28822004/in-vitro-validation-of-the-hippo-pathway-as-a-pharmacological-target-for-canine-mammary-gland-tumors
#13
Samantha Guillemette, Charlène Rico, Philippe Godin, Derek Boerboom, Marilène Paquet
Canine mammary tumors (CMTs) are the most common neoplasms in intact female dogs. Some clinical and molecular similarities between certain CMT subtypes and breast cancer make them a potential model for the study of the human disease. As misregulated Hippo signaling is thought to play an important role in breast cancer development and also occurs in CMTs, we sought to determine if Hippo represents a valid pharmacological target for the treatment of CMTs. Six CMT cell lines were assessed for their expression of the Hippo pathway effectors YAP and TAZ and for their sensitivity to verteporfin, an inhibitor of YAP-mediated transcriptional coactivation...
August 18, 2017: Journal of Mammary Gland Biology and Neoplasia
https://www.readbyqxmd.com/read/28821924/-89-zr-labeled-nivolumab-for-imaging-of-t-cell-infiltration-in-a-humanized-murine-model-of-lung-cancer
#14
Christopher G England, Dawei Jiang, Emily B Ehlerding, Brian T Rekoske, Paul A Ellison, Reinier Hernandez, Todd E Barnhart, Douglas G McNeel, Peng Huang, Weibo Cai
PURPOSE: Nivolumab is a human monoclonal antibody specific for programmed cell death-1 (PD-1), a negative regulator of T-cell activation and response. Acting as an immune checkpoint inhibitor, nivolumab binds to PD-1 expressed on the surface of many immune cells and prevents ligation by its natural ligands. Nivolumab is only effective in a subset of patients, and there is limited evidence supporting its use for diagnostic, monitoring, or stratification purposes. METHODS: (89)Zr-Df-nivolumab was synthesized to map the biodistribution of PD-1-expressing tumor infiltrating T-cells in vivo using a humanized murine model of lung cancer...
August 19, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28821888/risk-factors-for-epistaxis-in-patients-followed-in-general-practices-in-germany
#15
D U Seidel, L Jacob, K Kostev, A M Sesterhenn
<p>BACKGROUND: The goal of the present study was to analyze the risk factors for epistaxis in patients followed in general practices in Germany.</p> <p>METHODS: The current study sample included patients aged 18 years or older who received a first epistaxis diagnosis between January 2012 and December 2016 (index date). Epistaxis patients and controls without epistaxis were matched (1:1) on the basis of age, gender, insurance status and physician. </p> <p>RESULTS: A total of 16,801 patients with epistaxis and 16,801 control subjects were included in this study...
August 19, 2017: Rhinology
https://www.readbyqxmd.com/read/28821840/antiviral-properties-of-resveratrol-against-pseudorabies-virus-are-associated-with-the-inhibition-of-i%C3%AE%C2%BAb-kinase-activation
#16
Xinghong Zhao, Qiankun Cui, Qiuting Fu, Xu Song, Renyong Jia, Yi Yang, Yuanfeng Zou, Lixia Li, Changliang He, Xiaoxia Liang, Lizi Yin, Juchun Lin, Gang Ye, Gang Shu, Ling Zhao, Fei Shi, Cheng Lv, Zhongqiong Yin
Pseudorabies virus (PRV) is a pathogen of swine resulting in devastating disease and economic losses worldwide. Resveratrol (Res) exhibits inhibitory activity against a wide range of viruses. Despite these important advances, the molecular mechanism(s) by which Res exerts its broad biological effects have not yet been elucidated. In this paper, the antiviral activity of Res against PRV and its mechanism of action were investigated. The results showed that Res potently inhibited PRV replication in a dose-dependent manner, with a 50% inhibition concentration of 17...
August 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28821821/the-inhibitory-mechanism-of-hal3-on-the-yeast-ppz1-phosphatase-a-mutagenesis-analysis
#17
Cristina Molero, Carlos Casado, Joaquín Ariño
The Ser/Thr protein phosphatase (PPase) Ppz1 is an enzyme related to the ubiquitous type-1 PPases (PP1c) but found only in fungi. It is regulated by an inhibitory subunit, Hal3, which binds to its catalytic domain. Overexpression of Ppz1 is highly toxic for yeast cells, so its de-regulation has been proposed as a target for novel antifungal therapies. While modulation of PP1c by its many regulatory subunits has been extensively characterized, the manner by which Hal3 controls Ppz1 remains unknown. We have used error-prone PCR mutagenesis to construct a library of Ppz1 variants and developed a functional assay to identify mutations affecting the binding or/and the inhibitory capacity of Hal3...
August 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28821796/cathepsin-k-knockout-protects-against-cardiac-dysfunction-in-diabetic-mice
#18
Rui Guo, Yinan Hua, Olivia Rogers, Travis E Brown, Jun Ren, Sreejayan Nair
Diabetes is a major risk factor for cardiovascular disease and the lysosomal cysteine protease cathepsin K plays a critical role in cardiac pathophysiology. To expand upon our previous findings, we tested the hypothesis that, knockout of cathepsin K protects against diabetes-associated cardiac anomalies. Wild-type and cathepsin K knockout mice were rendered diabetic by streptozotocin (STZ) injections. Body weight, organ mass, fasting blood glucose, energy expenditure, cardiac geometry and function, cardiac histomorphology, glutathione levels and protein levels of cathepsin K and those associated with Ca(2+) handling, calcineurin/NFAT signaling, insulin signaling, cardiac apoptosis and fibrosis were determined...
August 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28821780/selective-inhibition-mechanism-of-rvx-208-to-the-second-bromodomain-of-bromo-and-extraterminal-proteins-insight-from-microsecond-molecular-dynamics-simulations
#19
Qianqian Wang, Ying Li, Jiahui Xu, Yuwei Wang, Elaine Lai-Han Leung, Liang Liu, Xiaojun Yao
RVX-208 is a recently reported inhibitor of bromo and extraterminal (BET) family proteins (including BRD2-4 and BRDT) with selectivity for the second bromodomain (BD2), currently in phase III clinical trials. Despite of its promising antitumor activity, due to the conserved folds of the first and second bromodomains (BD1 and BD2), the detailed selectivity mechanism of RVX-208 towards BD2 over BD1 is still unknown. To elucidate selective inhibition mechanism of RVX-208 to BD2, microsecond molecular dynamics simulations were performed in this study for BRD2-BD1, BRD2-BD2 and BRD4-BD1 with and without RVX-208, respectively...
August 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28821734/transcriptional-transitions-in-alphonso-mango-mangifera-indica-l-during-fruit-development-and-ripening-explain-its-distinct-aroma-and-shelf-life-characteristics
#20
Ashish B Deshpande, Krishanpal Anamika, Vineet Jha, Hemangi G Chidley, Pranjali S Oak, Narendra Y Kadoo, Keshav H Pujari, Ashok P Giri, Vidya S Gupta
Alphonso is known as the "King of mangos" due to its unique flavor, attractive color, low fiber pulp and long shelf life. We analyzed the transcriptome of Alphonso mango through Illumina sequencing from seven stages of fruit development and ripening as well as flower. Total transcriptome data from these stages ranged between 65 and 143 Mb. Importantly, 20,755 unique transcripts were annotated and 4,611 were assigned enzyme commission numbers, which encoded 142 biological pathways. These included ethylene and flavor related secondary metabolite biosynthesis pathways, as well as those involved in metabolism of starch, sucrose, amino acids and fatty acids...
August 18, 2017: Scientific Reports
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