• br Glucose metabolism and diet Glucokinase is

  2022-01-14

  

  Glucose metabolism and diet Glucokinase is essential for sensing blood glucose levels, thus controls metabolism (Iynedjian, 1993, Iynedjian, 2009, Postic et al., 2001, Agius, 2008). Loss of glucokinase activity in humans and mice leads to diabetes (Printz et al., 1993b, Postic et al., 2001, Agius

• LbGlcK crystallized as a ligandless dimer in

  2022-01-14

  

  LbGlcK crystallized as a ligandless dimer in the asymmetric unit of space group P21 (Fig. 1a) with two identical subunits stabilized by a large contact surface area of 2295 Å2 (13% of the total surface area) as determined by the Protein Interfaces, Surfaces, and Assemblies (PISA) server [18]. Each m

• AKR D is very highly expressed

  2022-01-14

  

  AKR1D1 is very highly expressed in human liver and based upon the observations outlined above, with respect to other steroid hormone pre-receptor metabolising enzymes, it is entirely plausible that AKR1D1 could represent a critical regulatory step in the control of metabolic phenotype within the liv

• br Competing interests br Acknowledgements br Introduction

  2022-01-14

  

  Competing interests Acknowledgements Introduction - Factors Regulating Glucose Tolerance Strictly speaking, the incretin effect refers to the amplification of insulin secretion, which occurs when Torin1 synthesis is taken in orally as compared to infused intravenously [1]. Normally, the in

• MK cyclobutylpiperidin yl oxyphenyl methyl trifluoromethyl q

  2022-01-13

  

  MK-3134 (3-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methyl-5-(trifluoromethyl)quinazolin-4-one) was synthesized by Merck, as the structurally constrained analogue of MK-0249 (Nagase et al., 2008). This H3R inverse agonist has MW 457.49, seven HBA, and MLogP 4.58, with one violation in terms of dr

• br Conclusion br Acknowledgments This research

  2022-01-13

  

  Conclusion Acknowledgments This research was funded by Tianjin Health Institution Key Projects, grant number 15KG148” and “Tianjin Medical University General Hospital Youth Incubation Fund, grant number ZYYFY2017029”. I would like to express my heartfelt gratitude to Professor Hongtao Zhang fo

• Another interesting approach is to

  2022-01-13

  

  Another interesting approach is to use partial agonists as starting point to develop specific antagonists like done in earlier decades [64], [65]. Possible indications for an attenuation of the NO/sGC signalling pathway might be specific neuronal disorders: an involvement in the aetiology of migrain

• It is well known that O

  2022-01-13

  

  It is well known that 12-O-tetradecanoylphorbol-13-acetate (TPA) is a tumor promoting agent of skin carcinogenesis in rodents [12]. TPA stimulates a variety of cellular functions in cancer cells, including cell motile activity [13], [14]. In our recent study, when liver epithelial cells were treated

• br Experimental br Acknowledgments This research

  2022-01-13

  

  Experimental Acknowledgments This research was supported by the Korea Research Foundation (2013R1A1A2007509). The authors thank to Dr. Moon Ho Son (Dong-A Pharm. Co. Ltd) for hGPR119 agonist activity assay. We also thank to Pharmacal Research Institute and Central Laboratory of Kangwon Nationa

• Several investigators including ourselves have previously

  2022-01-13

  

  Several investigators including ourselves have previously shown, that allogeneic HLA-DPB1 class II-alleles are powerful leukemia rejection Spectinomycin hydrochloride hydrate for CD4 T-cell therapy following allogeneic hematopoietic stem cell transplantation (Herr et al., 2017, Rutten et al., 2008,

• BIBW2992 Introduction The brain contains abundant fatty acid

  2022-01-13

  

  Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in dev

• d-cycloserine GK allosteric activators validate the

  2022-01-12

  

  GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of many

• Various strategies have been pursued in

  2022-01-12

  

  Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino Dimethyl Fumarate synthesis substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modificatio

• Calcitriol Introduction br Alzheimer pathology A and Tau

  2022-01-12

  

  Introduction Alzheimer pathology: Aβ and Tau Amyloid β protein (Aβ) plays an important role in AD pathogenesis. At the molecular level, senile amyloid plaques and neurofibrillary tangles (NFT) are two neuropathological hallmarks of AD [1]. Mutations in genes encoding amyloid precursor protein (A

• It is well known that

  2022-01-12

  

  It is well known that TLR4-induced inflammation is associated with behavioural alterations including fever, hypolocomotion, altered appetite, anxiety and anhedonia (Dantzer, 2006, Dantzer et al., 2008). The current data demonstrate that while PF3845 potently attenuates TLR4-induced cytokines in the

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