• As a part of our continuing efforts towards discovery of

  2022-10-09

  

  As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here

• ICH induced striatal lesion produced a

  2022-10-09

  

  ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino Tacalcitol transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia

• ICH induced striatal lesion produced a

  2022-10-09

  

  ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino Tacalcitol transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia

• ICH induced striatal lesion produced a

  2022-10-09

  

  ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino Tacalcitol transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia

• Genetic disruption or pharmacologic inhibition of the hepati

  2022-10-09

  

  Genetic disruption or pharmacologic inhibition of the hepatic glucagon pathway has invariably been shown to increase pancreatic α cell mass. This has been observed in glucagon receptor (GCGR) knockout (Gcgr−/−) mice (Gelling et al., 2003), glucagon knockout mice (Hayashi et al., 2009), prohormone co

• br Calcium permeability pathway It has been demonstrated tha

  2022-10-09

  

  Calcium permeability pathway It has been demonstrated that physiological shear stress in the circulation causes a reversible increase in Ca2+ permeability [29], [30], [31], [32], [33] and electrophysiological evidence has been recently reported for transient activation of the Ca2+-sensitive K+ ch

• There is increasing evidence that Cxs

  2022-10-09

  

  There is increasing evidence that Cxs in astrocytes may play a role in several models of brain pathologies. Interestingly their roles are at the moment more considered through their hemichannel function (Bennett et al., 2012; Bosch and Kielian, 2014; Davidson et al., 2013; Orellana et al., 2016; Kim

• The feasibility of using the Fas Fas

  2022-10-08

  

  The feasibility of using the Fas/Fas ligand (FasL) system to target vascular progenitor apoptosis contributing to intimal hyperplasia has been shown in many studies [[18], [19], [20], [21], [22], [23], [24]]. Fas receptor, a member of tissue necrosis factor family, is a death receptor that initiates

• Spindle positioning is governed by

  2022-10-04

  

  Spindle positioning is governed by the actin cytoskeleton. After a transient metaphase arrest, cells lacking haspin exhibit a misdistribution of actin, which accumulates within the bud. Actin dynamics is modulated by an intricate network including septins, the polarisome complex, and formins. We sho

• Over the last years numerous studies gave insights

  2022-10-04

  

  Over the last 15 years, numerous studies gave insights into sGC activation and binding of activators: Photoaffinity labelling studies with cinaciguat suggested the N-terminus of the β1 subunit as target region for this new drug [17]. Schmidt et al. identified the amino acids tyrosine 135, serine 137

• br Introduction The discovery that

  2022-10-04

  

  Introduction The discovery that the nitric oxide (NO), soluble guanylate cyclase (sGC), and cyclic guanosine monophosphate (cGMP) pathway mediates erection has led to the use of phosphodiesterase type 5 (PDE-5) inhibitors as the gold standard for treating erectile dysfunction (ED) through the inh

• GSK can function in regulating

  2022-10-04

  

  GSK-3 can function in regulating insulin signaling and glucose metabolism. Inactivation of GSK-3 activity results in dephosphorylation and activation of GS that leads to improved glucose tolerance. However, there are additional mechanisms that can lead to increases in GS activity and improve insulin

• To apply the recently developed GPR ligands to

  2022-10-04

  

  To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the rock inhibitor and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To this end,

• GPR agonistic activity was evaluated for the human GPR recep

  2022-10-04

  

  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 (defin

• br Author contributions br Acknowledgements The

  2022-10-04

  

  Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa

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