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https://www.readbyqxmd.com/read/29780974/metformin-targets-glucose-metabolism-in-triple-negative-breast-cancer
#1
R S Wahdan-Alaswad, S M Edgerton, H S Salem, A D Thor
Metformin is the most widely administered anti-diabetic agent worldwide. In patients receiving metformin for metabolic syndrome or diabetes, it reduces the incidence and improves the survival of breast cancer (BC) patients. We have previously shown that metformin is particularly potent against triple negative breast cancer (TNBC), with a reduction of proliferation, oncogenicity and motility, inhibition of pro-oncogenic signaling pathways and induction of apoptosis. These BCs are well recognized to be highly dependent on glucose/glucosamine (metabolized through anaerobic glycolysis) and lipids, which are metabolized for the production of energy and cellular building blocks to sustain a high rate of proliferation...
2018: Journal of Oncology Translational Research
https://www.readbyqxmd.com/read/29780415/comparison-of-efficacy-and-safety-of-lispro-and-aspart-evaluated-by-continuous-glucose-monitoring-system-in-patients-with-newly-diagnosed-type-2-diabetes
#2
Bing-Li Liu, Guo-Ping Yin, Feng-Fei Li, Yun Hu, Jin-Dan Wu, Mao-Yuan Chen, Lei Ye, Xiao-Fei Su, Jian-Hua Ma
Objective: To compare the effect of the rapid-acting insulin analogues (RAIAs) aspart (NovoRapid) and lispro (Prandilin) on glycemic variations by continuous glucose monitoring system (CGMS) in patients within newly diagnosed type 2 diabetes mellitus (T2DM) receiving continuous subcutaneous insulin infusion (CSII) and metformin intensive therapy. Methods: This is a single-blind randomized controlled trial. A total of 110 patients with newly diagnosed T2DM and with hemoglobin A1c (HbA1c%) above 9% was hospitalized and randomly divided into two groups: group Asp (NovoRapid group) and group Lis (Prandilin group)...
2018: International Journal of Endocrinology
https://www.readbyqxmd.com/read/29779196/retrospective-analysis-of-an-insulin-to-liraglutide-switch-in-patients-with-type-2-diabetes-mellitus
#3
Eveline Bruinstroop, Laura Meyer, Catherine B Brouwer, Diana E van Rooijen, P Sytze van Dam
INTRODUCTION: Insulin and the GLP-1 receptor agonist liraglutide are both effective in reaching glycemic targets. The efficacy of an insulin-to-liraglutide switch in an obese population with concurrent use of sulfonylurea and metformin is unknown. We assessed the efficacy and determinants of success of an insulin-to-liraglutide switch in these patients. METHODS: In a retrospective study we analyzed all patients that underwent an insulin-to-liraglutide switch during routine medical care (January 2009-February 2015)...
May 19, 2018: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/29779024/a-randomized-clinical-trial-of-metformin-to-treat-autosomal-dominant-polycystic-kidney-disease
#4
Stephen L Seliger, Kaleab Z Abebe, Kenneth R Hallows, Dana C Miskulin, Ronald D Perrone, Terry Watnick, Kyongtae Tae Bae
BACKGROUND: Metformin inhibits cyclic AMP generation and activates AMP-activated protein kinase (AMPK), which inhibits the cystic fibrosis transmembrane conductance regulator and Mammalian Target of Rapamycin pathways. Together these effects may reduce cyst growth in autosomal dominant polycystic kidney disease (ADPKD). METHODS: A phase II, double-blinded randomized placebo-controlled trial of 26 months duration. Participants will include nondiabetic adults (n = 96) aged 18-60 years, with an estimated glomerular filtration rate (eGFR) ≥50 mL/min/1...
May 18, 2018: American Journal of Nephrology
https://www.readbyqxmd.com/read/29777519/combination-glucose-lowering-therapy-plans-in-t2dm-case-based-considerations
#5
REVIEW
Lawrence Blonde, Susana Dipp, Daniel Cadena
Type 2 diabetes mellitus (T2DM) is a complex disease, and while lifestyle interventions remain the cornerstone of therapy, most patients will also require pharmacotherapy. Current diabetes treatment guidelines and algorithms recommend an individualized approach to setting glycemic goals and selecting treatment. Although a single antihyperglycemic agent may be appropriate as the initial T2DM pharmacotherapy, the progressive nature of the disease due to declining pancreatic β-cell function will result in the vast majority of T2DM patients eventually requiring two or more antihyperglycemic agents...
May 18, 2018: Advances in Therapy
https://www.readbyqxmd.com/read/29770821/a-size-shrinkable-nanoparticle-based-combined-anti-tumor-and-anti-inflammatory-strategy-for-enhanced-cancer-therapy
#6
Zhengze Lu, Yang Long, Xingli Cun, Xuhui Wang, Jianping Li, Ling Mei, Yiliang Yang, Man Li, Zhirong Zhang, Qin He
Cancer-related inflammation can promote tumorigenesis, tumor growth and tumor metastasis in many types of cancers. Therefore, inhibiting cancer-related inflammation significantly improves cancer therapy. It has been reported that metformin (MET) inhibits the nuclear translocation of nuclear factor-κB (NF-κB), a key factor in cancer-related inflammation. However, the short half-life and the lack of tumor targeting limit the anti-inflammatory efficacy of MET in vivo. Herein, using pH-sensitive imine bonds, MET and the chemotherapy drug doxorubicin (DOX) were loaded onto size-shrinkable RGD-DGL-GNP nanoparticles (RDG NPs) for combination therapy...
May 17, 2018: Nanoscale
https://www.readbyqxmd.com/read/29765528/metabolic-changes-associated-with-metformin-potentiates-bcl-2-inhibitor-venetoclax-and-cdk9-inhibitor-bay1143572-and-reduces-viability-of-lymphoma-cells
#7
Vineela Chukkapalli, Leo I Gordon, Parameswaran Venugopal, Jeffrey A Borgia, Reem Karmali
Metformin exerts direct anti-tumor effects by activating AMP-activated protein kinase (AMPK), a major sensor of cellular metabolism in cancer cells. This, in turn, inhibits pro-survival mTOR signaling. Metformin has also been shown to disrupt complex 1 of the mitochondrial electron transport chain. Here, we explored the lymphoma specific anti-tumor effects of metformin using Daudi (Burkitt), SUDHL-4 (germinal center diffuse large B-cell lymphoma; GC DLBCL), Jeko-1 (Mantle-cell lymphoma; MCL) and KPUM-UH1 (double hit DLBCL) cell lines...
April 20, 2018: Oncotarget
https://www.readbyqxmd.com/read/29760945/liraglutide-and-dulaglutide-therapy-in-addition-to-sglt-2-inhibitor-and-metformin-treatment-in-indian-type-2-diabetics-a-real-world-retrospective-observational-study
#8
S Ghosal, B Sinha
Background: Therapy for Type 2 diabetes (T2D) has been transformed by the introduction of newer agents like Glucagon like Peptide Receptor Agonists (GLP-1RA) and Sodium-glucose linked transporter inhibitors (SGLT2i). However with co-initiation of SGLT2i and GLP-1RA in the DURATION 8 trial an improvement in HbA1c was noted but the beneficial effect was not equal to the sum of its parts. In view of this we proceeded to test the hypothesis that sequential addition of GLP-1RA therapy to metformin and SGLT-2i may be more beneficial...
2018: Clinical Diabetes and Endocrinology
https://www.readbyqxmd.com/read/29752759/metformin-targets-brown-adipose-tissue-in-vivo-and-reduces-oxygen-consumption-in-vitro
#9
Peter Breining, Jonas B Jensen, Elias I Sundelin, Lars C Gormsen, Steen Jakobsen, Morten Busk, Lars Rolighed, Peter Bross, Paula Fernandez-Guerra, Lasse K Markussen, Nanna E Rasmussen, Jacob B Hansen, Steen B Pedersen, Bjørn Richelsen, Niels Jessen
Metformin is the most widely prescribed oral antidiabetic drug worldwide. Despite well-documented beneficial effects on health outcomes in diabetic patients, the target organs that mediate the effects of metformin remain to be established. In adult humans, brown adipose tissue (BAT) can influence basic metabolic rate, making BAT an attractive target for treatment of type 2 diabetes. Under the hypothesis that BAT is a metformin target tissue, we investigated in vivo uptake of [11 C]-metformin tracer in mice and studied in vitro effects of metformin on cultured human brown adipocytes...
May 12, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29741792/frontline-science-pathological-conditioning-of-human-neutrophils-recruited-to-the-airway-milieu-in-cystic-fibrosis
#10
Osric A Forrest, Sarah A Ingersoll, Marcela K Preininger, Julie Laval, Dominique H Limoli, Milton R Brown, Frances E Lee, Brahmchetna Bedi, Ruxana T Sadikot, Joanna B Goldberg, Vin Tangpricha, Amit Gaggar, Rabindra Tirouvanziam
RATIONALE: Recruitment of neutrophils to the airways, and their pathological conditioning therein, drive tissue damage and coincide with the loss of lung function in patients with cystic fibrosis (CF). So far, these key processes have not been adequately recapitulated in models, hampering drug development. Here, we hypothesized that the migration of naïve blood neutrophils into CF airway fluid in vitro would induce similar functional adaptation to that observed in vivo, and provide a model to identify new therapies...
May 9, 2018: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/29740925/metformin-directly-targets-the-h3k27me3-demethylase-kdm6a-utx
#11
Elisabet Cuyàs, Sara Verdura, Laura Llorach-Pares, Salvador Fernández-Arroyo, Fedra Luciano-Mateo, Noemí Cabré, Jan Stursa, Lukas Werner, Begoña Martin-Castillo, Benoit Viollet, Jiri Neuzil, Jorge Joven, Alfons Nonell-Canals, Melchor Sanchez-Martinez, Javier A Menendez
Metformin, the first drug chosen to be tested in a clinical trial aimed to target the biology of aging per se, has been clinically exploited for decades in the absence of a complete understanding of its therapeutic targets or chemical determinants. We here outline a systematic chemoinformatics approach to computationally predict biomolecular targets of metformin. Using several structure- and ligand-based software tools and reference databases containing 1,300,000 chemical compounds and more than 9,000 binding sites protein cavities, we identified 41 putative metformin targets including several epigenetic modifiers such as the member of the H3K27me3-specific demethylase subfamily, KDM6A/UTX...
May 8, 2018: Aging Cell
https://www.readbyqxmd.com/read/29736297/anti-diabetic-activity-of-quercetin-extracted-from-phyllanthus-emblica-l-fruit-in-silico-and-in-vivo-approaches
#12
Prabhu Srinivasan, S Vijayakumar, Swaminathan Kothandaraman, Manogar Palani
In this study, molecular interactions of the ligands, quercetin, gallic acid, and metformin with various diabetes mellitus-related protein targets, such as glycogen phosphorylase and peroxisome proliferator-activated receptor gamma, were assessed. It was revealed that quercetin possesses good binding affinity to both targets. Quercetin is a major constituent of methanolic extracts of Phyllanthus emblica fruit. The antihyperglycemic effect of quercetin in streptozotocin (STZ)-induced diabetic rats was examined...
April 2018: Journal of Pharmaceutical Analysis
https://www.readbyqxmd.com/read/29735394/dorzagliatin-monotherapy-in-chinese-patients-with-type-2-diabetes-a-dose-ranging-randomised-double-blind-placebo-controlled-phase-2-study
#13
Dalong Zhu, Shenglian Gan, Yu Liu, Jianhua Ma, Xiaolin Dong, Weihong Song, Jiao'e Zeng, Guixia Wang, Wenjuan Zhao, Qiu Zhang, Yukun Li, Hui Fang, Xiaofeng Lv, Yongquan Shi, Haoming Tian, Linong Ji, Xin Gao, Lihui Zhang, Yuqian Bao, Minxiang Lei, Ling Li, Longyi Zeng, Xiaoying Li, Xinghua Hou, Yu Zhao, Tianxin Hu, Xiaoyun Ge, Guiyu Zhao, Yongguo Li, Yi Zhang, Li Chen
BACKGROUND: Glucokinase acts as a glucose sensor in the pancreas and a glucose processor in the liver, and has a central role in glucose homoeostasis. Dorzagliatin is a new, dual-acting, allosteric glucokinase activator that targets both pancreatic and hepatic glucokinases. Dorzagliatin has good pharmacokinetic and pharmacodynamic properties in humans, and provides effective 24-h glycaemic control and improves glucose sensitivity in patients with type 2 diabetes. We aimed to assess the efficacy and safety of dorzagliatin monotherapy at different doses in Chinese patients with type 2 diabetes...
May 4, 2018: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/29728793/metformin-protects-against-spinal-cord-injury-by-regulating-autophagy-via-the-mtor-signaling-pathway
#14
Yue Guo, Fang Wang, Haopeng Li, Hui Liang, Yuhuan Li, Zhengchao Gao, Xijing He
Spinal cord injury (SCI) is a serious central trauma, leading to severe dysfunction of motor and sensory systems. Secondary injuries, such as apoptosis and cell autophagy, significantly impact the motor function recovery process. Metformin is a widely used oral anti-diabetic agent for type 2 diabetes in the world. It has been demonstrated to promote autophagy and inhibit apoptosis in the nervous system. However, its role in recovery following SCI is still unknown. In this study, we determined that motor function, assessed using the Basso, Beattie, and Bresnahan (BBB) locomotor assessment scale, was significantly higher in rats treated with metformin following injury...
May 4, 2018: Neurochemical Research
https://www.readbyqxmd.com/read/29727301/design-graph-theoretical-analysis-and-in-silico-modeling-of-dunaliella-bardawil-biomass-encapsulated-keratin-nanoparticles-a-scaffold-for-effective-glucose-utilization
#15
Selvaraj Kunjiappan, Theivendren Panneerselvam, Parvathy Prasad, Sunija Sukumaran, Balasubramanian Somasundaram, Murugesan Sankaranarayanan, Indhumathy Murugan, Pavadai Parasuraman
The aim of the present study is to develop keratin nanoparticles (NPs) encapsulated in Dunaliella bardawil (D. bardawil) biomass, in order to improve their glucose uptake in 3T3-L1 adipocytes. The graph theoretical approach has provided a platform to identify PTP-1B and AMPK as an effective drug target. Docking results of the active constituents of D. bardawil showed a strong interaction with binding pockets of identified PTP-1B and AMPK. The encapsulation efficiency, drug release, stability and physicochemical properties of prepared NPs were analyzed using UV-visible spectrophotometry, Fourier transform infrared spectrophotometry, x-ray diffraction, scanning and tunneling electron microscopy, and Zeta size analysis...
May 4, 2018: Biomedical Materials
https://www.readbyqxmd.com/read/29718742/an-rnai-mediated-screen-identifies-novel-targets-for-next-generation-antiepileptic-drugs-based-on-increased-expression-of-the-homeostatic-regulator-pumilio
#16
Wei-Hsiang Lin, Miaomiao He, Yuen Ngan Fan, Richard A Baines
Despite availability of a diverse range of anti-epileptic drugs (AEDs), only about two-thirds of epilepsy patients respond well to drug treatment. Thus, novel targets are required to catalyse the design of next-generation AEDs. Manipulation of neuron firing-rate homoeostasis, through enhancing Pumilio (Pum) activity, has been shown to be potently anticonvulsant in Drosophila. In this study, we performed a genome-wide RNAi screen in S2R + cells, using a luciferase-based dPum activity reporter and identified 1166 genes involved in dPum regulation...
May 2, 2018: Journal of Neurogenetics
https://www.readbyqxmd.com/read/29713286/the-wnt-signaling-pathway-effector-tcf7l2-mediates-olanzapine-induced-weight-gain-and-insulin-resistance
#17
Ranran Li, Jianjun Ou, Li Li, Ye Yang, Jingping Zhao, Renrong Wu
Olanzapine is a widely used atypical antipsychotic medication for treatment of schizophrenia and is often associated with serious metabolic abnormalities including weight gain and impaired glucose tolerance. These metabolic side effects are severe clinical problems but the underpinning mechanism remains poorly understood. Recently, growing evidence suggests that Wnt signaling pathway has a critical role in the pathogenesis of schizophrenia and molecular cascades of antipsychotics action, of which Wnt signaling pathway key effector TCF7L2 is strongly associated with glucose homeostasis...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29710715/targeting-insulin-for-alzheimer-s-disease-mechanisms-status-and-potential-directions
#18
Jung Hyun Lee, Jordan B Jahrling, Larry Denner, Kelly T Dineley
Insulin resistance can occur when the body is unable to respond to insulin even in excess. In the brain, insulin manages glucose metabolism in regions such as the hippocampus and plays a key role in directly regulating ERK, a kinase required for the type of memory compromised in early Alzheimer's disease (AD). Human imaging studies show that brain glucose utilization declines with age and is notably impaired in subjects with early AD. Likewise, animal models of AD or insulin resistance, or both, demonstrate that dysfunctional insulin signaling and insulin resistance in the brain have reciprocity with neuroinflammation and aberrant accumulation of amyloid-β (Aβ), pathological hallmarks in AD...
April 27, 2018: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29710606/suspect-screening-and-target-quantification-of-human-pharmaceutical-residues-in-the-surface-water-of-wuhan-china-using-uhplc-q-orbitrap-hrms
#19
Muhammad Ali Asghar, Qingxin Zhu, Shutang Sun, Yue'e Peng, Qin Shuai
In this study we developed a systematic method for suspect screening and target quantification of the human pharmaceutical residues in water, via solid phase extraction (SPE) followed by liquid chromatography-high resolution mass spectrometry (LC-HRMS). We then proceeded to study the occurrences and distribution of the pharmaceuticals in the surface waters of Wuhan, China, by analyzing water samples from lakes, rivers and municipal sewage. Initially, 33 human pharmaceuticals were identified from East Lake without using purchasing standards...
April 20, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/29691295/metformin-targets-mitochondrial-glycerophosphate-dehydrogenase-mgpdh-to-control-rate-of-oxidative-phosphorylation-and-growth-of-thyroid-cancer-in-vitro-and-in-vivo
#20
Shilpa Thakur, Brianna Daley, Kelli Gaskins, Vasyl V Vasko, Myriem Boufraqech, Dhaval Patel, Carole Sourbier, Jeff M Reece, Sheue-Yann Cheng, Electron Kebebew, Sunita K Agarwal, Joanna Klubo-Gwiezdzinska
PURPOSE: Mitochondrial glycerophosphate dehydrogenase (mGPDH) is the key enzyme connecting oxidative phosphorylation (OXPHOS) and glycolysis as well as a target of the antidiabetic drug metformin (MF) in the liver. There are no data on the expression and role of mGPDH as a metformin target in cancer. In this study, we evaluated mGPDH as a potential target of metformin in thyroid cancer and investigated its contribution in thyroid cancer metabolism. EXPERIMENTAL DESIGN: We analyzed mGPDH expression in 253 thyroid cancer and normal tissues by immunostaining and examined its expression and localization in thyroid cancer-derived cell lines (FTC133, BCPAP) by confocal microscopy...
April 24, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
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