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https://www.readbyqxmd.com/read/29311579/structural-basis-for-the-enhanced-anti-diabetic-efficacy-of-lobeglitazone-on-ppar%C3%AE
#1
Jun Young Jang, Hwan Bae, Yong Jae Lee, Young Il Choi, Hyun-Jung Kim, Seung Bum Park, Se Won Suh, Sang Wan Kim, Byung Woo Han
Peroxisome proliferator-activated receptor γ (PPARγ) is a member of the nuclear receptor superfamily. It functions as a ligand-activated transcription factor and plays important roles in the regulation of adipocyte differentiation, insulin resistance, and inflammation. Here, we report the crystal structures of PPARγ in complex with lobeglitazone, a novel PPARγ agonist, and with rosiglitazone for comparison. The thiazolidinedione (TZD) moiety of lobeglitazone occupies the canonical ligand-binding pocket near the activation function-2 (AF-2) helix (i...
January 8, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29296202/cell-death-and-restoration-of-trail-sensitivity-by-ciglitazone-in-resistant-cervical-cancer-cells
#2
Marie-Laure Plissonnier, Sylvie Fauconnet, Hugues Bittard, Christiane Mougin, Jean Rommelaere, Isabelle Lascombe
Known activators of the Peroxisome Proliferator-Activated Receptor γ (PPARγ), thiazolidinediones (TZD) induce apoptosis in a variety of cancer cells through dependent and/or independent mechanisms of the receptor. We tested a panel of TZD (Rosiglitazone, Pioglitazone, Ciglitazone) to shed light on their potential therapeutic effects on three cervical cancer cell lines (HeLa, Ca Ski, C-33 A). In these cells, only ciglitazone triggered apoptosis through PPARγ-independent mechanisms and in particular via both extrinsic and intrinsic pathways in Ca Ski cells containing Human PapillomaVirus (HPV) type 16...
December 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/29296174/a-novel-thiazolidinediones-atzd2-rescues-memory-deficits-in-a-rat-model-of-type-2-diabetes-through-antioxidant-and-antiinflammation
#3
Xuan-Kang Wang, Ting Sun, Yu-Jiao Li, Yu-Hong Wang, Yan-Jiao Li, Liu-Di Yang, Dan Feng, Ming-Gao Zhao, Yu-Mei Wu
Type 2 diabetes (T2DM) has been associated with learning and memory impairment; however, drugs for diabetes could not prevent the development of cognitive decline in T2DM patients. In the present study, compounds derived from thiazolidinediones (TZD), a PPAR-γ agonist, were synthesized by conjuncting the alkyl-substituted benzimidazole group to TZD group (ATZDs). Based on the in vitro evaluation, the neuroprotection of ATZD2 was further investigated using a streptozotocin-induced T2DM rat model. Pharmacokinetic study showed that ATZD2 could pass the blood-brain barrier (BBB) while the rosiglitazone (RSG, the precursor compound of ATZD2) not...
December 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/29275147/lack-of-longitudinal-association-between-thiazolidinediones-and-incidence-and-progression-of-diabetic-eye-disease-the-accord-eye-study
#4
Emily W Gower, James F Lovato, Walter T Ambrosius, Emily Y Chew, Ronald P Danis, Matthew D Davis, David C Goff, Craig M Greven
PURPOSE: To report the longitudinal association between use of thiazolidinediones (TZDs), visual acuity (VA) change and diabetic eye disease incidence and progression. DESIGN: Cohort study ancillary to a randomized clinical trial METHODS: We analyzed baseline and four-year follow up data of 2,856 ACCORD trial participants with no history of proliferative diabetic retinopathy. Based on stereoscopic fundus photographs, we evaluated diabetic macular edema (DME) progression and DR progression...
December 21, 2017: American Journal of Ophthalmology
https://www.readbyqxmd.com/read/29236980/simultaneous-determination-of-tizanidine-nimesulide-aceclofenac-and-paracetamol-in-tablets-and-biological-fluids-using-micellar-liquid-chromatography
#5
Fathalla Belal, Mahmoud A Omar, Sayed Derayea, Mohamed A Hammad, Sahar Zayed, Safaa F Saleh
A simple, sensitive and rapid micellar liquid chromatographic method was developed and validated for simultaneous determination of four drugs, namely, paracetamol (PAR), tizanidine (TZD), aceclofenac (ACF) and nimesulide (NMD). Good chromatographic separation was achieved using Cyano column and micellar mobile phase consisting of 120 mM sodium dodecyl sulfate, 25 mM phosphate buffer and 10% (V/V) butanol. The pH was adjusted to three using phosphoric acid. The total retention time was below 10 min. The analysis was performed at a flow rate of 1 mL/min and a column temperature of 40°C with direct UV detection at 230 nm...
December 11, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/29205774/comparison-of-glucose-lowering-agents-following-dual-therapy-failure-in-type-2-diabetes-systematic-review-and-network-meta-analysis-of-randomised-controlled-trials
#6
Francesco Zaccardi, Nafeesa N Dhalwani, Jolyon Dales, Hamid Mani, Kamlesh Khunti, Melanie J Davies, David R Webb
AIMS: To assess the evidence supporting the choice of third-line agents in adults with inadequately controlled type 2 diabetes. MATERIALS AND METHODS: We searched RCTs published between Jan 2000 and July 2017 reporting data on cardiometabolic outcomes and hypoglycaemia for glucose-lowering agents added to metformin-based dual treatments. Data were stratified by background therapy and RCT duration and synthesised, when possible, with network meta-analyses. RESULTS: 43 RCTs (16590 participants) were included, with metformin combined to sulphonylurea (SU) in 20 RCTs; thiazolidinedione (TZD) in 10; basal or rapid acting insulin in 6; DPP-4i in 3; GLP-1RA in 2; and SGLT-2i in 2...
December 5, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29203903/structures-of-ppar%C3%AE-complexed-with-lobeglitazone-and-pioglitazone-reveal-key-determinants-for-the-recognition-of-antidiabetic-drugs
#7
Min A Lee, Lingchen Tan, Huiseon Yang, Yeong-Gwan Im, Young Jun Im
Peroxisome proliferator-activator receptor (PPAR) γ is a nuclear hormone receptor that regulates glucose homeostasis, lipid metabolism, and adipocyte function. PPARγ is a target for thiazolidinedione (TZD) class of drugs which are widely used for the treatment of type 2 diabetes. Recently, lobeglitazone was developed as a highly effective TZD with reduced side effects by Chong Kun Dang Pharmaceuticals. To identify the structural determinants for the high potency of lobeglitazone as a PPARγ agonist, we determined the crystal structures of the PPARγ ligand binding domain (LBD) in complex with lobeglitazone and pioglitazone at 1...
December 4, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29189151/assorted-applications-of-n-substituted-2-4-thiazolidinediones-in-various-pathological-conditions
#8
Rakesh Gupta, Hardik Joshi, C S Ramaa
Thiazolidine-2,4-dione (TZD), one of the most frequently encountered heterocyclic ring which has been implicated in design and synthesis of entities for various pathogenic conditions including cancer. Since its discoveryvarious substitutions at 5th position has been carried out and reviewed. Various substitutions at 5th position has led to generation of glitazones, whose target peroxisome proliferating activated receptor γ (PPARγ) was found decade after their discovery.Acidichydrogen (-NH) of TZD is prime pharmacophoric requirement for activation of PPARγ...
November 29, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29165364/the-rosiglitazone-like-effects-of-vitexilactone-a-constituent-from-vitex-trifolia-l-in-3t3-l1-preadipocytes
#9
Atsuyoshi Nishina, Masaya Itagaki, Daisuke Sato, Hirokazu Kimura, Yasuaki Hirai, Nyunt Phay, Makoto Makishima
The increased number of patients with type 2 diabetes (T2D) has become a worldwide problem, and insulin sensitizers such as thiazolidinediones (TZDs) are used as therapeutic agents. We found that extracts of Vitex trifolia L. (V. trifolia), a medicinal plant from Myanmar, induced adipogenesis similar to rosiglitazone (ROS), which is a TZD, in 3T3-L1 preadipocytes. In the present study, we attempted to isolate from V. trifolia those compounds that showed ROS-like effects. Among the extracts of hexane, ethyl acetate, and methanol obtained from V...
November 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29130039/a-sustained-release-membrane-of-thiazolidinedione-8-effect-on-formation-of-a-candida-bacteria-mixed-biofilm-on-hydroxyapatite-in-a-continuous-flow-model
#10
Mark Feldman, Julia Shenderovich, Eran Lavy, Michael Friedman, Doron Steinberg
Thiazolidinediones (TZDs) have been found to act as effective quorum sensing quenchers, capable of preventing biofilm formation. Our previous studies demonstrated a profound antibiofilm effect of the TZD derivative thiazolidinedione-8 (S-8), either in solution or incorporated into a sustained-release membrane (SRM-S-8) under batch conditions. In the present study, we used a constant depth film fermenter model in order to investigate the impact of SRM-S-8 on mixed C. albicans-S. mutans biofilm development, under flow conditions...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29125710/thiazolidinedione-therapy-and-breast-cancer-risk-in-diabetic-women-a-systematic-review-and-meta-analysis
#11
REVIEW
Rui Du, Lin Lin, Di Cheng, Yu Xu, Min Xu, Yuhong Chen, Weiqing Wang, Yufang Bi, Donghui Li, Jieli Lu
BACKGROUND: Rising experimental evidence suggests that thiazolidinediones (TZDs) exert a protective effect on breast cancer. However, studies concerning this issue were inconsistent and limited. Hence, we performed a meta-analysis with data from currently available studies to evaluate the effect of TZDs on breast cancer risk among diabetic women. METHODS: We comprehensively searched for all pertinent studies addressing TZDs use and breast cancer risk published before January 1, 2016 in PubMed, Clinical Trials and Cochrane library...
November 10, 2017: Diabetes/metabolism Research and Reviews
https://www.readbyqxmd.com/read/29122042/peroxisome-proliferator-activated-receptor-gamma-ppar%C3%AE-agonist-fails-to-overcome-trans-10-cis-12-conjugated-linoleic-acid-cla-inhibition-of-milk-fat-in-dairy-sheep
#12
E C Sandri, M Camêra, E M Sandri, K J Harvatine, D E De Oliveira
The trans-10, cis-12 conjugated linoleic acid (CLA) causes milk fat depression by downregulating expression of genes and transcription factors involved in lipogenesis and it has been proposed that peroxisome proliferator-activated receptor gamma (PPARγ) can be inhibited by trans-10, cis-12 CLA. The PPARγ is a nuclear receptor activated by natural or synthetic ligands and promotes expression of lipogenic genes and its effect on mammary lipogenesis and the interaction with trans-10, cis-12 CLA in lactating ewes was evaluated using thiazolidinedione (TZD), a chemical PPARγ agonist...
November 10, 2017: Animal: An International Journal of Animal Bioscience
https://www.readbyqxmd.com/read/29108837/factors-associated-with-type-2-diabetes-mellitus-treatment-choice-across-four-european-countries
#13
Edith M Heintjes, Jetty A Overbeek, Gillian C Hall, Daniel Prieto-Alhambra, Francesco Lapi, Niklas Hammar, Irene D Bezemer
PURPOSE: The aim of this analysis was to identify factors associated with the choice of type 2 diabetes mellitus (T2DM) therapy at the time of intensification of antidiabetic treatment across 4 European countries. METHODS: Antidiabetic drug prescription/dispensing records and patients' characteristics were obtained from the electronic health care records of patients with T2DM from the Netherlands (NL), Italy, and Spain (ES) (all, 2007-2011); and the United Kingdom (UK; 2008-2012)...
November 3, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/29089569/novel-benzylidene-thiazolidinedione-derivatives-as-partial-ppar%C3%AE-agonists-and-their-antidiabetic-effects-on-type-2-diabetes
#14
Sabina Yasmin, Fabio Capone, Antonio Laghezza, Fabrizio Dal Piaz, Fulvio Loiodice, Viswanathan Vijayan, Velmurugan Devadasan, Susanta K Mondal, Özlem Atlı, Merve Baysal, Ashok K Pattnaik, Venkatesan Jayaprakash, Antonio Lavecchia
Peroxisome proliferator-activated receptor γ (PPARγ) has received significant attention as a key regulator of glucose and lipid homeostasis. In this study, we synthesized and tested a library of novel 5-benzylidene-thiazolidin-2,4-dione (BTZD) derivatives bearing a substituent on nitrogen of TZD nucleus (compounds 1a-1k, 2i-10i, 3a, 6a, and 8a-10a). Three compounds (1a, 1i, and 3a) exhibited selectivity towards PPARγ and were found to be weak to moderate partial agonists. Surface Plasmon Resonance (SPR) results demonstrated binding affinity of 1a, 1i and 3a towards PPARγ...
October 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29071111/impact-of-pioglitazone-and-bradykinin-type-1-receptor-antagonist-on-type-2-diabetes-in-high-fat-diet-fed-c57bl-6j-mice
#15
S El Akoum, Y Haddad, R Couture
AIM: Type 2 diabetes (T2D) is a major complication of obesity and a leading cause of morbidity and mortality. Antagonizing bradykinin type 1 receptor (B1R) improved body and tissue fat mass and reversed vascular and adipose tissue inflammation in a rat model of insulin resistance. This study aimed at evaluating further the role of B1R in a mouse model of T2D by comparing the antidiabetic and anti-inflammatory effects of the B1R antagonist SSR240612 (SSR) in adipose tissue with those of pioglitazone (TZD), an activator of peroxisome proliferator-activated receptor gamma...
September 2017: Obesity Science & Practice
https://www.readbyqxmd.com/read/29056962/chiglitazar-preferentially-regulates-gene-expression-via-configuration-restricted-binding-and-phosphorylation-inhibition-of-ppar%C3%AE
#16
De-Si Pan, Wei Wang, Nan-Song Liu, Qian-Jiao Yang, Kun Zhang, Jing-Zhong Zhu, Song Shan, Zhi-Bin Li, Zhi-Qiang Ning, Laiqiang Huang, Xian-Ping Lu
Type 2 diabetes mellitus is often treated with insulin-sensitizing drugs called thiazolidinediones (TZD), which improve insulin resistance and glycemic control. Despite their effectiveness in treating diabetes, these drugs provide little protection from eminent cardiovascular disease associated with diabetes. Here we demonstrate how chiglitazar, a configuration-restricted non-TZD peroxisome proliferator-activated receptor (PPAR) pan agonist with moderate transcription activity, preferentially regulates ANGPTL4 and PDK4, which are involved in glucose and lipid metabolism...
2017: PPAR Research
https://www.readbyqxmd.com/read/29047219/addition-of-dipeptidyl-peptidase-4-inhibitors-to-insulin-treatment-in-type-2-diabetes-patients-a-meta-analysis
#17
Wenjia Yang, Xiaoling Cai, Xueying Gao, Yifei Chen, Chen Ling, Linong Ji
AIMS: To evaluate the efficacy and safety of combining insulin therapy with dipeptidyl peptidase 4 (DPP-4) inhibitors compared to combining insulin therapy with placebo or other antihyperglycaemic agents. MATERIALS AND METHODS: A literature search was conducted via electronic databases. The inclusion criteria were randomized controlled trials (RCTs) comparing the addition of DPP-4 inhibitors to insulin with the addition of placebo or other active hypoglycaemic agents to insulin therapy, study duration of no less than 12 weeks performed in type 2 diabetes patients, and the availability of outcome data to evaluate a change in the HbA1c ...
October 19, 2017: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/29046921/pioglitazone-reduces-cold-induced-brown-fat-glucose-uptake-despite-induction-of-browning-in-cultured-human-adipocytes-a-randomised-controlled-trial-in-humans
#18
Rebecca K C Loh, Melissa F Formosa, Nina Eikelis, David A Bertovic, Mitchell J Anderson, Shane A Barwood, Shane Nanayakkara, Neale D Cohen, Andre La Gerche, Anne T Reutens, Kenneth S Yap, Thomas W Barber, Gavin W Lambert, Martin H Cherk, Stephen J Duffy, Bronwyn A Kingwell, Andrew L Carey
AIMS/HYPOTHESIS: Increasing brown adipose tissue (BAT) activity is a possible therapeutic strategy to increase energy expenditure and glucose and lipid clearance to ameliorate obesity and associated comorbidities. The thiazolidinedione (TZD) class of glucose-lowering drugs increase BAT browning in preclinical experimental models but whether these actions extend to humans in vivo is unknown. The aim of this study was to determine the effect of pioglitazone treatment on adipocyte browning and adaptive thermogenesis in humans...
October 18, 2017: Diabetologia
https://www.readbyqxmd.com/read/29023313/mini-scleral-lenses-for-correction-of-refractive-errors-after-radial-keratotomy
#19
Hsiao-Sang Chu, I-Jong Wang, Grace A Tseng, Wei-Li Chen, Yu-Chih Hou, Fung-Rong Hu
OBJECTIVE: To evaluate the factors affecting clinical outcomes of correcting cumulative refractive errors or irregular astigmatism after radial keratotomy (RK) using mini-scleral lenses. METHODS: We retrospectively analyzed 36 eyes receiving mini-scleral lenses after RK from July 2011 to June 2016. Analyses included age, refractive errors, best spectacle-corrected visual acuity (BSCVA), best contact lens-corrected visual acuity (BCLCVA), topographic indices, RK treatment zone diameter (TZD), power difference (PrD) within the RK treatment zone, and decentration distance (DD) of the RK treatment zone center...
October 11, 2017: Eye & Contact Lens
https://www.readbyqxmd.com/read/28979777/changes-in-treatment-of-hyperglycemia-in-a-hypertensive-type-2-diabetes-population-as-renal-function-declines
#20
Larry A Weinrauch, Alissa R Segal, George P Bayliss, Jiankang Liu, Eric Wisniewski, John A D'Elia
BACKGROUND: Cardiovascular complications associated with expensive noninsulin agents for type 2 diabetes are the focus of concern in light of the risk of kidney dysfunction with aging. Head-to-head comparisons are unavailable to guide the choice of new drugs for hyperglycemia in patients with type 2 diabetes, decreased estimated glomerular filtration rate (eGFR) and increased cardiovascular risk. A first approach would be to document current medication choices. METHODS: All prescriptions for 10 151 patients (5623 males/4528 females) with both type 2 diabetes and hypertension seen two or  more times during a 5-year period (2007-12) at Joslin Diabetes Center were evaluated...
October 2017: Clinical Kidney Journal
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