• Introduction Gestational diabetes mellitus GDM is one of the

  2022-04-26

  

  Introduction Gestational diabetes mellitus (GDM) is one of the most common complications associated with pregnancy [1]. Approximately 7.6% of pregnancies in the United States are complicated by GDM [2,3], which significantly increases the mother's risk of developing type 2 diabetes (T2D) later in l

• In addition researchers studying GPR agonists favor

  2022-04-26

  

  In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it SM-164 is unclear why Sanofi-Aventis chose to terminate collaboration with Metabolex (no

• It appears that not all GPR agonists require a high

  2022-04-26

  

  It appears that not all GPR119 agonists require a high dose to elicit acceptable thz1 sale control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/kg sitag

• br Opportunities The ever expanding diabetes

  2022-04-26

  

  Opportunities The ever-expanding diabetes market is one of the driving forces for the development of new antidiabetes drugs. Diabetes mellitus influenced an estimated 371 million humans during 2012 worldwide, and this figure is projected to increase in every country. According to International Di

• br Conflict of interest br Acknowledgment This work

  2022-04-26

  

  Conflict of interest Acknowledgment This work was supported by National Program on Key Basic Research Project of China (No. 2013CB127305); The National Natural Science Foundation of China (No. 314020785); Hubei Provincial Creative Team Project of Agricultural Science and Technology (No. 2007-6

• As natural ligands of GPR several long chain

  2022-04-26

  

  As natural ligands of GPR120, several long chain polyunsaturated fatty acids (Lc-PUFAs) have been demonstrated to modulate the 3T3-L1 adipogenic differentiation. However, the effects of the Lc-PUFAs are inconclusive. DHA is shown to inhibit, promote or even not affect the differentiation of preadipo

• In order to investigate whether this

  2022-04-26

  

  In order to investigate whether this off-target activity was related to a particular structural feature of this thz1 or was characteristic of the series, compounds , and were selected as being matched pairs with compound but with structural variation in terms of the R, R and R groups, respective

• The compounds described in this paper

  2022-04-26

  

  The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m

• br GPR is a class

  2022-04-26

  

  GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine SAR 405 which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell sign

• We hypothesized that modulating redox stress

  2022-04-26

  

  We hypothesized that modulating redox stress by altering endogenous antioxidant content (overexpression of catalase) and/or via dietary intervention will improve energy metabolism, adipose tissue function, and overall glucose and lipid homeostasis. To better understand the interplay between redox re

• In addition to redox stress nutritional intake plays

  2022-04-26

  

  In addition to redox stress, nutritional intake plays a key role in modulating energy metabolism. DIO animal models are commonly used to study altered metabolic changes consequential to fat storage within various fat pads. In general, diets containing >40% high-fat lard, milk, and butter promote exc

• The pharmacokinetics of was obtained

  2022-04-26

  

  The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indi

• Fmoc-Phe-OPfp br Next we explored the SAR

  2022-04-26

  

  Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic Fmoc-Phe-OPfp sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo did no

• br Conclusion br Acknowledgements This

  2022-04-26

  

  Conclusion Acknowledgements This work was supported by a Grant-in-Aid for challenging Exploratory Research (15K12715) and was a partly supported by Suzuken Memorial Foundation (2014). The authors would like to thank Enago (www.enago.jp) for the English language review. G protein-coupled rec

• br Materials and methods br

  2022-04-26

  

  Materials and methods Results Discussion Previously, it is well known that methionine and choline deficient (MCDD) or choline-deficient, L-amino acid-defined (CDAA) models are widely accepted in NASH research. MCDD or CDAA dietary model has been mimic human NASH in rodents by sequentially p

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