• The absolute requirement for substrate

  2022-05-21

  

  The absolute requirement for substrate prephosphorylation raised the possibility that short phosphorylated peptides might serve as selective substrate competitive inhibitors. A set of phosphorylated peptides patterned after known GSK-3 substrates was generated and shown to inhibit GSK-3 in vitro in

• GPR agonistic activity was evaluated for the human GPR

  2022-05-21

  

  GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defi

• To investigate if such an effect is

  2022-05-21

  

  To investigate if such an effect is observed in native GlyT1, we introduced S605D and S605A mutations into GlyT1 and transfected these DNA constructs into N2a cells. For an internal control of calpain cleavage, we also introduced the first 100 amino-acids of the rat GlyT2N terminus upstream of the m

• Studies of human and mouse GPR as ascertained by

  2022-05-21

  

  Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infla

• The typical pharmacophore for GPR agonists contains four par

  2022-05-21

  

  The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors

• Accordingly a bioassay guided approach was been used

  2022-05-21

  

  Accordingly, a bioassay-guided approach was been used to study the bioactive compounds in VAS contribute to the α-glucosidase inhibitory and antioxidant activity. The 95% ethanol extraction of VAS was successively partitioned with petroleum ether, ethyl acetate and n-butanol. Ethyl acetate fraction

• br Acknowledgements The authors are grateful for

  2022-05-21

  

  Acknowledgements The authors are grateful for funding provided by the Health Research Council of New Zealand. Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, fa

• br Acknowledgments br The authors would like to acknowledge

  2022-05-21

  

  Acknowledgments The authors would like to acknowledge the technical assistance of J. Lee. This work was supported by the U.S. National Institute of Health grant HL111206 (to R.A.H.) the Italian Ministry for University and Research (MIUR 2010329EKE). Introduction The liver plays a vital role

• LIMKi 3 The vast majority of clinical studies have shown

  2022-05-21

  

  The vast majority of clinical studies have shown that chronic administration of GLP-1R agonists frequently lowers SBP/DBP in diabetic humans, which is consistent with preclinical studies, though the reported reductions are not as potent as those observed in their animal counterparts. In contrast, ac

• Gli signaling pathways play critical

  2022-05-21

  

  Gli signaling pathways play critical roles in embryonic and postnatal lung development [22]. Many reports suggest that wound healing and fibrotic diseases involve activation of pathways used during development [23]. In the adult lung, Gli signaling activity measured by Gli1 expression is restricted

• AICAR phosphate synthesis Further our data demonstrate a rol

  2022-05-21

  

  Further, our data demonstrate a role for mitochondrial AIF in oxidative cell death induced by RSL3. We found that AIF knockdown using siRNA completely protected the AICAR phosphate synthesis against RSL3 induced oxidative stress. Similar to other pathways of caspase-independent programmed cell death

• br Role of funding source br

  2022-05-20

  

  Role of funding source Conflict of interest Acknowledgements We thank F. Blaskovits and P. Kesner for technical assistance. This project was supported by operating grants from the Canadian Institutes of Health Research (CIHR) to X. Zhang (MOP123249) and the National Natural Science Foundati

• This study appears to provide an

  2022-05-20

  

  This study appears to provide an additional example, albeit an unanticipated one, of the importance of renal ETB receptor function in the normal control of blood pressure and salt and water homeostasis. ETB receptor-deficient rats, collecting duct-specific ETB receptor knockout mice, and rats chroni

• With the aim to identify potential novel targets in

  2022-05-20

  

  With the aim to identify potential novel targets in CVD, we applied proteome analyses on vascular tissue of these frequently used mouse models of atherosclerotic disease in the presence and/or absence of diabetes. Potential targets for intervention identified with this approach were validated in hum

• At baseline Hdc KO mice have alterations in the

  2022-05-20

  

  At baseline, Hdc-KO mice have alterations in the examined signaling cascades that resemble those seen in WT mice after RAMH challenge. Specifically, gaba inhibitor of MSK1 at T581 and of rpS6 ad S235/236 are elevated in dMSNs to a similar extent after saline in KO mice and after RAMH challenge in W

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