• Receptor guanylyl cyclases play essential roles in

  2022-01-29

  

  Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists

• br Conflict of Interest Both GM and BDH are shareholders

  2022-01-29

  

  Conflict of Interest Both GM and BDH are shareholders in Caldan Therapeutics, a company exploring potential novel treatments for type 2 diabetes. Acknowledgments Work described herein was supported by Biotechnology and Biological Sciences Research Council [grant BB/K019864/1)] (to GM) and [gr

• Phenyl sulfate GPR is a member of the G protein coupled

  2022-01-29

  

  GPR119 is a member of the G protein-coupled receptor family, and is highly expressed in pancreatic β-cells and intestinal endocrine cells. It has been proposed that GPR119 agonists modulate glucose homeostasis by indirectly stimulating glucose-dependent insulin release through enhancing pancreatic c

• Based on the role of NMDA

  2022-01-29

  

  Based on the role of NMDA receptors in initiation and propagation of epileptic seizures and on potentiation of NMDA function by glycine, it has been hypothesized that glycine will have proconvulsant activity (Foster and Kemp, 1989). Indeed, there is some evidence that human epileptogenic foci, remov

• Variants of NEIL were also analysed in Primary

  2022-01-29

  

  Variants of NEIL1 were also analysed in Primary sclerosing cholangitis (PSC) and cholangiocarcinoma (CCA) patients by Forsbring et al. to identify effect of variants on these diseases. Four variants were identified i.e., one earlier validated (G83D) and three novel (E181K, H275, R339W). E181K was fo

• Ethanol decreased the value of desensitization

  2022-01-29

  

  Ethanol decreased the τ-value of desensitization for GluR-Di. Coexpression of stargazin or γ4 further increased the effect of ethanol on desensitization (Fig. 3A, B). The highest ethanol concentration tested (200mM) reduced the τ-value by 16.5±4.9% (n=5) in the control receptors and by 29.3±9.3% (n=

• Sequences of hexokinases were initially

  2022-01-29

  

  Sequences of hexokinases were initially deduced and predicted based on cDNA clones (Andreone et al., 1989, Schwab and Wilson, 1989, Schwab and Wilson, 1991, Griffin et al., 1991, Thelen and Wilson, 1991). Analysis of genome sequence data identified, in NCT-502 to the 4 expected known hexokinase enz

• Human Glucocorticoid Receptor hGR was first cloned in Hollen

  2022-01-29

  

  Human Glucocorticoid Receptor (hGR) was first cloned in 1985 (Hollenburg et al., 1985). It is a modular protein comprised of an N-terminal trans-activating domain (NTD), a C-terminal ligand-binding domain (LBD) and a central DNA- binding domain (DBD). The DBD is highly conserved and has two zinc fin

• A group of small molecule with a more promising

  2022-01-29

  

  A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-si

• Seizures in turn selectively modulate

  2022-01-29

  

  Seizures, in turn, selectively modulate the brucine receptor of GalR in the hippocampus. Thus, pilocarpine-induced SE led to a 30% downregulation of GalR2 without affecting GalR1 (personal communication with T. Bartfai, Scripps Research Institute). Therefore, despite the fact that GalR2 could have b

• Prior models suggest that the

  2022-01-28

  

  Prior models suggest that the terminal ends of the endocrine FGFs individually determine FGFR and KLB recognition, with little or no cross-talk. Our results confirm that short C-terminal sequences are necessary and sufficient to bind KLB and, supportive of a common mechanism, the underlying structur

• We have expanded these studies by doing EEG recording

  2022-01-28

  

  We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA A-803467 or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagonist o

• The present study was therefore conducted with three

  2022-01-28

  

  The present study was therefore conducted with three aims; (1) we tested the effect of IRL-1620, a selective ETB receptor agonist, on the analgesic tolerance to morphine and oxycodone in mice; (2) we determined the expression of ETA receptors and ETB receptors in the Pirfenidone of morphine and oxyc

• Wolf et al then proceed to interrogate the mechanism by

  2022-01-28

  

  Wolf et al. (2016) then proceed to interrogate the mechanism by which NAG activates the NLRP3 inflammasome. When examining potential triggers previously implicated in NLRP3 activation, they found that both PGN and NAG trigger appearance of mitochondrial DNA (mtDNA) in the cytosol, which led them to

• Epidermal Growth Factor (EGF), human recombinant mg G protei

  2022-01-28

  

  G protein-coupled receptor kinases (GRKs) are another group of kinases whose limited substrate repertoire is associated with an extensive binding interface. GRKs phosphorylate activated G protein-coupled receptors (GPCRs) at multiple sites, promoting binding of arrestin proteins to mediate receptor

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