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https://www.readbyqxmd.com/read/28636360/proneurogenic-effects-of-trazodone-in-murine-and-human-neural-progenitors
#1
Valeria Bortolotto, Francesca Mancini, Giorgina Mangano, Rita Salem, Er Xia, Erika Del Grosso, Michele Bianchi, Pier Luigi Canonico, Lorenzo Polenzani, Mariagrazia Grilli
Several antidepressants increase adult hippocampal Neurogenesis (ahNG) in rodents, primates and, potentially, in humans. This effect may at least partially account for their therapeutic activity. The availability of antidepressants whose mechanism of action involves different neurotransmitter receptors represents an opportunity for increasing our knowledge on their distinctive peculiarities and for dissecting the contribution of receptor subtypes in ahNG modulation. The aim of this study was to evaluate, in vitro, the effects of the antidepressant trazodone (TZD) on ahNG by using primary cultures of adult hippocampal Neural Progenitor Cells (ahNPC) and human iPSC-derived NPC...
June 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28618987/synthesis-of-new-thiazolyl-coupled-pyrazoles-bearing-2-4-thiazolidinedionyl-pharmacophore-and-their-anti-inflammatory-and-antibacterial-evaluation
#2
Lalit Khillare, Manisha Bhosle, Mahendra Bhalerao, Kiran Kharat, Ramrao Mane
BACKGROUND: 2, 4-Thiazolidinedione (TZD), pyrazole and thiazole heterocyclic rings exhibit wide range of pharmacological activities. Medicinal chemists use these heterocyclic moieties as scaffolds in drug designing and discovery. The existing medicaments, celecoxib and meloxicam, used for treating inflammation and pain are having, pyrazole and thiazole, respectively as a key scaffolds. Pyrazoles coupled with 2, 4-thiazolidinediones may display enhanced anti inflammatory activity. With this hope the title work was carried...
June 16, 2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28611274/meta-analysis-of-randomized-controlled-trials-of-pharmacologic-agents-in-non-alcoholic-steatohepatitis
#3
Adnan Said, Ahmed Akhter
BACKGROUND: Currently, there is no standardized treatment regimen for non-alcoholic steatohepatitis. AIM: We performed a metaanalysis of high quality randomized controlled trials that evaluated treatment response to metformin, thiazolidinediones (TZDs), and vitamin E in adult patients with non-alcoholic steatohepatitis. Outcome measures were improvement in liver histology, biochemical, and anthropometric measures. MATERIAL AND METHODS: Nine trials met inclusion criteria (3 with TZD, 3 with Metformin, 2 with Vitamin E and 1 with both TZD and Vitamin E...
August 1, 2017: Annals of Hepatology
https://www.readbyqxmd.com/read/28597936/the-beneficial-metabolic-effects-of-insulin-sensitizers-are-not-attenuated-by-mitochondrial-pyruvate-carrier-2-hypomorphism
#4
Patrick A Vigueira, Kyle S McCommis, Wesley T Hodges, George G Schweitzer, Serena L Cole, Lalita Oonthonpan, Eric B Taylor, William G McDonald, Rolf F Kletzien, Jerry R Colca, Brian N Finck
Rosiglitazone and pioglitazone are thiazolidinedione (TZD) compounds that have been used clinically as insulin-sensitizing drugs and are generally believed to mediate their effects via activation of the peroxisome proliferator-activated receptor γ (PPARγ). Recent work has shown that it is possible to synthesize TZD compounds with potent insulin-sensitizing effects and markedly-diminished affinity for PPARγ. Both clinically-used TZDs and investigational PPARγ-sparing TZDs, such as MSDC-0602, interact with the mitochondrial pyruvate carrier (MPC) and inhibit its activity...
June 9, 2017: Experimental Physiology
https://www.readbyqxmd.com/read/28589493/a-randomized-placebo-controlled-trial-evaluating-the-safety-and-efficacy-of-adding-omarigliptin-to-antihyperglycemic-therapies-in-japanese-patients-with-type-2-diabetes-and-inadequate-glycemic-control
#5
Ira Gantz, Taro Okamoto, Yuka Ito, Asako Sato, Kotoba Okuyama, Edward A O'Neill, Samuel S Engel, Eseng Lai
INTRODUCTION: Daily dipeptidyl peptidase-4 (DPP-4) inhibitors are commonly used with other orally administered antihyperglycemic agents (AHA), as combination therapy, to treat Japanese patients with type 2 diabetes. When combination therapy is indicated, use of a once-weekly (q.w.) orally administered DPP-4 inhibitor might be an appropriate therapeutic option for some patients. METHODS: A 52-week trial was conducted to assess the safety and tolerability (primary objectives) and glycemic efficacy (secondary objectives) of the q...
June 6, 2017: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/28548941/withdrawn-prognostic-role-of-anti-diabetic-drugs-in-pancreatic-cancer-a-systematic-review-and-meta-analysis
#6
Lei Zheng, Shinan Yin, Fenghua Yao, Hua Bai, Danqing Jing
Ahead of Print article withdrawn by publisher.
May 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28542373/comparative-effectiveness-of-oral-antidiabetic-drugs-in-preventing-cardiovascular-mortality-and-morbidity-a-network-meta-analysis
#7
Gyeongsil Lee, Seung-Won Oh, Seung-Sik Hwang, Ji Won Yoon, Sungchan Kang, Hee-Kyung Joh, Hyuktae Kwon, Jeehyun Kim, Danbee Park
In the Guidance for Industry from the Food and Drug Administration in 2008, excess cardiovascular risk should be ruled out in trials of all new antidiabetic drugs; however, relatively few studies have focused on cardiovascular safety with antidiabetic drug use. We aimed to examine mortality and cardiovascular risk using a network meta-analysis. We searched the Medline, Embase, Cochrane, and ClinicalTrials.gov registry databases in March 2016 to identify randomized controlled trials reporting cardiovascular risk with the following oral antidiabetic drugs: metformin, sulfonylureas, thiazolidinedione (TZD), dipeptidyl peptidase-4 (DPP4) inhibitors, and sodium-glucose co-transporter-2 (SGLT2) inhibitors...
2017: PloS One
https://www.readbyqxmd.com/read/28539218/switching-subtype-selectivity-fragment-replacement-strategy-affords-novel-class-of-peroxisome-proliferator-activated-receptor-%C3%AE-%C3%AE-ppar%C3%AE-%C3%AE-dual-agonists
#8
Ryuta Shioi, Shogo Okazaki, Tomomi Noguchi-Yachide, Minoru Ishikawa, Makoto Makishima, Yuichi Hashimoto, Takao Yamaguchi
Peroxisome proliferator-activated receptors (PPARs) are important drug targets for treatment of dyslipidemia, type 2 diabetes, cardiovascular disease, nonalcoholic fatty liver disease and nonalcoholic steatohepatitis, and great efforts have been made to develop novel PPAR ligands. However, most existing PPAR ligands contain a carboxylic acid (CA) or thiazolidinedione (TZD) structure (acidic head group) that is essential for activity. We recently discovered non-CA/TZD class PPARα/δ partial agonists, which contain an acetamide moiety and adjacent methyl group, linked to a 1,2,4-oxadiazole ring ("fragment a")...
May 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28523719/cardiovascular-events-associated-with-second-line-anti-diabetes-treatments-analysis-of-real-world-korean-data
#9
K H Ha, B Kim, H Choi, D J Kim, H C Kim
AIM: To compare the risks of cardiovascular disease (CVD) and all-cause mortality associated with sulfonylurea (SU), dipeptidyl peptidase-4 inhibitor (DPP4i) and thiazolidinedione (TZD) as add-on medications to metformin (MET) therapy in people with Type 2 diabetes. METHODS: We identified 40 263 individuals who used SU (n = 11 582), DPP4i (n = 26 623) or TZD (n = 2058) in addition to MET between January 2013 and June 2015 from the database of the Korean National Health Insurance, the single-payer healthcare system in South Korea...
May 19, 2017: Diabetic Medicine: a Journal of the British Diabetic Association
https://www.readbyqxmd.com/read/28506609/ageing-kinetics-and-strength-of-airborne-particle-abraded-3y-tzp-ceramics
#10
Jasna Cotič, Peter Jevnikar, Andraž Kocjan
OBJECTIVE: The combined effects of alumina airborne-particle abrasion and prolonged in vitro ageing on the flexural strength of 3Y-TZP ceramic have been studied. The aim was to identify the different effects on the surface and subsurface regions that govern the performance of this popular bioceramic known for its susceptibility to low-temperature degradation (LTD). METHODS: As-sintered or airborne-particle abraded 3Y-TZP discs were subjected to ageing at 134°C for up to 480h...
May 12, 2017: Dental Materials: Official Publication of the Academy of Dental Materials
https://www.readbyqxmd.com/read/28499821/x-ray-crystal-structure-of-rivoglitazone-bound-to-ppar%C3%AE-and-ppar-subtype-selectivity-of-tzds
#11
Harinda Rajapaksha, Harpreet Bhatia, Kate Wegener, Nikolai Petrovsky, John B Bruning
Thiazolidinedione (TZD) compounds targeting the nuclear receptor peroxisome proliferator-activated receptor gamma (PPARγ) demonstrate unique benefits for the treatment of insulin resistance and type II diabetes. TZDs include rosiglitazone, pioglitazone and rivoglitazone, with the latter being the most potent. The TZDs are only marginally selective for the therapeutic target PPARγ as they also activate PPARα and PPARδ homologues to varying degrees, causing off-target effects. While crystal structures for TZD compounds in complex with PPARγ are available, minimal structural information is available for TZDs bound to PPARα and PPARδ...
August 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28469599/the-role-of-thyrotropin-receptor-activation-in-adipogenesis-and-modulation-of-fat-phenotype
#12
Mohd Shazli Draman, Michael Stechman, David Scott-Coombes, Colin M Dayan, Dafydd Aled Rees, Marian Ludgate, Lei Zhang
Evidence from clinical and experimental data suggests that thyrotropin receptor (TSHR) signaling is involved in energy expenditure through its impact on white adipose tissue (WAT) and brown adipose tissue (BAT). TSHR expression increases during mesenchymal stem cell (MSC) differentiation into fat. We hypothesize that TSHR activation [TSHR*, elevated thyroid-stimulating hormone, thyroid-stimulating antibodies (TSAB), or activating mutation] influences MSC differentiation, which contributes to body composition changes seen in hypothyroidism or Graves' disease (GD)...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28438542/identification-of-low-micromolar-dual-inhibitors-for-aldose-reductase-alr2-and-poly-adp-ribose-polymerase-parp-1-using-structure-based-design-approach
#13
Navriti Chadha, Om Silakari
Clinical studies have revealed that diabetic retinopathy is a multifactorial disorder. Moreover, studies also suggest that ALR2 and PARP-1 co-occur in retinal cells, making them appropriate targets for the treatment of diabetic retinopathy. To find the dual inhibitors of ALR2 and PARP-1, the structure based design was carried out in parallel for both the target proteins. A series of novel thiazolidine-2,4-dione (TZD) derivatives were therefore rationally designed, synthesized and their in vitro inhibitory activities against ALR2 and PARP-1 were evaluated...
April 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28384299/in-depth-study-of-dna-binding-of-cys2his2-finger-domains-in-testis-zinc-finger-protein
#14
Chun-Chi Chou, Shu-Yi Wei, Yuan-Chao Lou, Chinpan Chen
Previously, we identified that both fingers 1 and 2 in the three Cys2His2 zinc-finger domains (TZD) of testis zinc-finger protein specifically bind to its cognate DNA; however, finger 3 is non-sequence-specific. To gain insights into the interaction mechanism, here we further investigated the DNA-binding characteristics of TZD bound to non-specific DNAs and its finger segments bound to cognate DNA. TZD in non-specific DNA binding showed smaller chemical shift perturbations, as expected. However, the direction of shift perturbation, change of DNA imino-proton NMR signal, and dynamics on the 15N backbone atom significantly differed between specific and non-specific binding...
2017: PloS One
https://www.readbyqxmd.com/read/28383181/effects-of-silica-coating-by-physical-vapor-deposition-and-repeated-firing-on-the-low-temperature-degradation-and-flexural-strength-of-a-zirconia-ceramic
#15
Tutku Cakir-Omur, Rifat Gozneli, Yasemin Ozkan
PURPOSE: To examine the application of physical vapor deposition (PVD) silica coating as an approach to retard low temperature degradation (LTD) for dental applications. Accelerated aging characteristics of heat- and surface-treated zirconia material were also investigated by exposing specimens to hydrothermal treatment. MATERIALS AND METHODS: The specimens (90 disc-shaped specimens [15 mm ×1.2 mm]) were divided into 9 groups (n = 10) according to the test protocol: Ctrl, control (no surface treatment); Ag, autoclave aging; GrAg, grinding + aging; SiAg, silica coating + aging; GrSiAg, grinding + silica coating + aging; 3FAg, 3-time firing + aging; Gr3FAg, grinding + 3-time firing + aging; 5FAg, 5-time firing + aging; Gr5FAg, grinding + 5-time firing + aging...
April 6, 2017: Journal of Prosthodontics: Official Journal of the American College of Prosthodontists
https://www.readbyqxmd.com/read/28381265/thiazolidinedione-use-and-atrial-fibrillation-in-diabetic-patients-a-meta-analysis
#16
Zhiwei Zhang, Xiaowei Zhang, Panagiotis Korantzopoulos, Konstantinos P Letsas, Gary Tse, Mengqi Gong, Lei Meng, Guangping Li, Tong Liu
BACKGROUND: Accumulating evidence suggests that thiazolidinediones (TZDs) may exert protective effects in atrial fibrillation (AF). The present meta-analysis investigated the association between TZD use and the incidence of AF in diabetic patients. METHODS: Electronic databases were searched until December 2016. Of the 346 initially identified records, 3 randomized clinical trials (RCTs) and 4 observational studies with 130,854 diabetic patients were included in the final analysis...
April 5, 2017: BMC Cardiovascular Disorders
https://www.readbyqxmd.com/read/28348577/deciphering-the-roles-of-thiazolidinediones-and-ppar%C3%AE-in-bladder-cancer
#17
REVIEW
Melody Chiu, Lucien McBeth, Puneet Sindhwani, Terry D Hinds
The use of thiazolidinedione (TZD) therapy in type II diabetic patients has proven useful in the lowering of blood glucose levels. However, recent investigations have shown that there may be potential health concerns associated, including the risk of developing bladder cancer as well as complications in the cardiovasculature. TZDs are ligands for the nuclear receptor PPARγ, and activation causes lipid uptake and insulin sensitization, both of which are critical processes for diabetic patients whose bodies are unable to utilize insulin effectively...
2017: PPAR Research
https://www.readbyqxmd.com/read/28314484/impact-of-health-policy-and-practice-on-finding-the-best-fit-for-patients-with-type-2-diabetes-after-metformin-failure-croatian-pilot-study
#18
Maja Cigrovski Berković, Davorka Herman Mahečić, Marina Gradišer, Ines Bilić-Ćurčić
AIM: We assessed the impact of clinical practice and health policy on the choice and efficacy of different second-line therapies for the treatment of type 2 diabetes (T2DM) after failure of metformin. METHODS: This retrospective database analysis included 200 patients with a follow-up period of 6 months. The primary end-point was achievement of HbA1c <7% and fasting (FBG) and postprandial glucose levels (PPG) <7.2mmol/L and <10mmol/L, respectively after three and six months of different add-on treatments...
June 2017: Primary Care Diabetes
https://www.readbyqxmd.com/read/28302016/validation-of-tzd-scaffold-as-potential-aris-pharmacophore-modelling-atom-based-3d-qsar-and-docking-studies
#19
Lalita Dahiya, Manoj Kumar Mahapatra, Ramandeep Kaur, Vipin Kumar, Manoj Kumar
Metabolic disorders associated with diabetic patients are a serious concern. Aldose reductase (ALR2) has been identified as first rate-limiting enzyme in the polyol pathway which catalyzes the reduction of glucose to sorbitol. It represents one of the validated targets to develop potential new chemical entities for the prevention and subsequent progression of microvascular diabetic complications. In order to further understand the intricate structural prerequisites of molecules to act as ALR2 inhibitors, ligand-based pharmacophore model, atom-based 3D-QSAR and structure based drug design studies have been performed on a series of 2,4-thiazolidinedione derivatives with ALR2 inhibitory activity...
March 15, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28248890/effect-of-contraindicated-drugs-for-heart-failure-on-hospitalization-among-seniors-with-heart-failure-a-nested-case-control-study
#20
Catherine Girouard, Jean-Pierre Grégoire, Paul Poirier, Jocelyne Moisan
Little is known about the effect of nonsteroidal anti-inflammatory drugs (NSAIDs), thiazolidinediones (TZDs), nifedipine and nondihydropyridine calcium channel blockers (CCBs) usage on the risk of all-cause hospitalization among seniors with heart failure (HF). We assessed the risk of all-cause hospitalization associated with exposure to each of these drug classes, in a population of seniors with HF.Using the Quebec provincial databases, we conducted a nested case-control study in a population of individuals aged ≥65 with a first HF diagnosis between 2000 and 2009...
March 2017: Medicine (Baltimore)
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