• br Mutagenesis and Receptor Modeling Studies br Signal Trans

  2022-08-19

  

  Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio

• GPR has been implicated in neuropathic and inflammatory

  2022-08-19

  

  GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow

• biotin-LC-LC-tyramide The intracellular signaling that media

  2022-08-19

  

  The intracellular signaling that mediates the adipogenesis induced by GPR120 still remains largely unknown. In the present study we showed that TUG-891 induced the activation of [Ca2+]i and ERK1/2 signaling in 3T3-L1 cells. Moreover, incubation of TUG-891 combined with BAPTA-AM or U0126 abolished TU

• br Materials and methods br Results br Discussion Heart

  2022-08-18

  

  Materials and methods Results Discussion Heart hypertrophy is initially physiological to compensate for the loss of heart functions. However, sustained stresses lead to a pathological status, in which myocardium becomes stiffened by interstitial fibrosis and thereby diastolic dysfunction in

• br Excitatory amino acid transporter mediated glutamate

  2022-08-18

  

  Excitatory amino mtor inhibitor transporter-mediated glutamate transport Early studies detailing the presence of uptake systems capable of transporting glutamate and aspartate into neurons and glia represented a critical step in the overall task of demonstrating that l-glutamate was indeed an en

• Ionotropic glutamate receptors GluRs are

  2022-08-18

  

  Ionotropic glutamate receptors (GluRs) are ligand-gated ion channels that mediate information processing at the majority of excitatory synapses in the brain and participate in such physiological processes as learning and memory, development and maintenance of cellular connections, and pain perceptio

• cAMP is a key secondary messenger which transduces extracell

  2022-08-18

  

  cAMP is a key secondary messenger which transduces extracellular signals at glucagon receptors to intracellular effector molecules. cAMP-protein kinase A (PKA) pathway increases the gene expression of enzymes including phosphoenolpyruvate carboxykinase (PEPCK) and glucose 6-phosphatase (G6Pase) whic

• Consistent with recent independent studies we confirm

  2022-08-18

  

  Consistent with recent independent studies, we confirm that the GCG-induced increase in oxygen consumption is only partially blunted in Fgf21−/− mice [32], implicating additional GCGR-dependent mechanisms contributing to the acute GCG-dependent enhancement of energy expenditure. Notably, glucagon ad

• Despite a robust impact on

  2022-08-18

  

  Despite a robust impact on learned, social feeding behaviors, we observed no differences in body weight or food intake when the control or vHP GHSR-1A KD animals were maintained on either a normal chow diet or a Western diet high in fat and sugar. This is interesting in light of our previous work sh

• br Conflict of interest br Transparency document

  2022-08-18

  

  Conflict of interest Transparency document Acknowledgements We acknowledge our funding sources from the American Heart Association (13EIA4480016) and the National Institute of Health/National Heart, Lung, and Blood Institute (RO1 HL094414). We are very grateful to Dr. Shaohua Xiao and Dr. S

• The present in vitro experiments confirm previous suppositio

  2022-08-18

  

  The present in vitro experiments confirm previous suppositions (Ciosek, Gałecka, 2011, Izdebska, Ciosek, 2010) that Gal modulates AVP and OT release by acting at every level of the hypothalamo-neurohypophysial system. In fact, both 10−10 M and 10−8 M Gal diminished basal release of AVP and OT from t

• br Fipronil resistance associated with

  2022-08-18

  

  Fipronil resistance associated with A2′S and A2′G mutations Fipronil is a second-generation NCA (Fig. 1), and A2′S and A2′G mutations provide a low level of cross-resistance to fipronil (Cole et al., 1995, Gao et al., 2007). As shown in Table 1, the A2′S Mouse iPSC Chemical Reprogramming Cocktail

• Photoincorporation of pTFDBzox AP occurred

  2022-08-18

  

  Photoincorporation of 21-pTFDBzox-AP occurred predominantly in the β3 subunit, very modestly in the α1 subunit and not at all in the γ2 subunit. These observations taken together with the sensitivity of 21-pTFDBzox-AP enhancement of GABA currents to the α1 M1 mutation Q242 W4 suggest that the 21-pTF

• Natural products are a diverse and interesting source

  2022-08-18

  

  Natural products are a diverse and interesting source for the discovery of new lead structures (Newman and Cragg, 2016). After a successful era of natural product research, many pharmaceutical companies stopped their investment in natural product-driven drug discovery in the 1990s. The reason behind

• Recently Bristol Myers Squibb and Merck reported their GPR a

  2022-08-18

  

  Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic brucine derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agonists wit

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