• Finally we investigated if calpain truncation affects GlyT t

  2022-07-21

  

  Finally, we investigated if calpain truncation affects GlyT1 turnover and trafficking. To simulate calpain cleavage at the T602/T603 and G626/S627 sites we constructed GlyT1 transporters missing the last 12 and 36 amino acids. Since the 36 amino Riboflavin truncation also removes all C-terminal ant

• It is well known that GPCR responsiveness desensitizes after

  2022-07-21

  

  It is well known that GPCR responsiveness desensitizes after prolonged exposure to agonists through several mechanisms such as receptor phosphorylation, arrestin binding and internalization (Dhami and Ferguson, 2006). Therefore, in the present work we decided to study whether group I-mGluR signaling

• The dorsal horn of the

  2022-07-21

  

  The dorsal horn of the spinal cord shows a high density of Ca2+-permeable AMPA receptors, particularly in the superficial spinal laminae (laminae I and II), where primary afferents carrying nociceptive and thermoreceptive inputs terminate and synapse on spinal second-order neurons (Engelman et al.,

• Malotilate receptor The energy required to drive the functio

  2022-07-21

  

  The energy required to drive the functional process to actively maintain lens transparency is primarily derived from the metabolism of glucose. Since the lens is avascular and exists in an environment of low oxygen tension, glucose is primarily metabolized by Malotilate receptor glycolysis (Kinoshi

• The eradication of agonist activity in compound

  2022-07-21

  

  The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary Ac-DEVD-AFC as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagonize

• Furthermore our results are the first to demonstrate that

  2022-07-21

  

  Furthermore, our results are the first to demonstrate that the stimulating effect of GALP on AVP release in rats is independent of galanin receptors. The same stimulatory GALP influence on AVP secretion has been also observed in the presence of galantide, an antagonist of Gal receptors in the incuba

• D appears to be important

  2022-07-21

  

  D83 appears to be important for receptor function as a mutation to an alanine produced a non-functional channel. Interestingly, maintaining the charge as in D83E produced only a small reduction in GABA sensitivity. Other mutations at this position which included residues capable of hydrogen bonding

• The effect of on the conformational of G quadruplexes was

  2022-07-21

  

  The effect of on the conformational of G-quadruplexes was investigated with circular dichroism (CD) spectroscopy. In the absence of , the CD spectra of parallel G-quadruplex exhibited a characteristic positive peak at about 265 nm, and a negative peak at about 240 nm; antiparallel G-quadruplex sh

• The physicochemical properties of the prodrugs

  2022-07-21

  

  The physicochemical properties of the prodrugs provided important clues for understanding a broad range of inhibitory activities in the cell assays (Table 2). Some physicochemical properties are useful in predicting drug absorption. Considering Lipinski’s rules and the polar surface area (PSA),l-ala

• br Acknowledgements We thank Dr Bhushan Nagar and Dr Albert

  2022-07-21

  

  Acknowledgements We thank Dr. Bhushan Nagar and Dr. Albert Berghuis for access to the X-ray diffraction machine at McGill University. We also thank Dr. Manon Couture and Dr. Steve Charette at Université Laval for access to scientific equipment. Funding for this research was provided by Discovery

• Trifluoromethyl ketones and fluorophosphates were the first

  2022-07-21

  

  Trifluoromethyl ketones and fluorophosphates were the first generation FAAH inhibitors identified. They showed good in vitro FAAH inhibition potency, but most of them exhibited poor selectivity for FAAH over other serine hydrolases (such as the triacylglycerol hydrolase and the membrane-associated h

• In a preliminary communication we showed that AT and

  2022-07-20

  

  In a preliminary communication, we showed that AT and ETB receptors colocalize and coimmunoprecipitate in renal proximal tubule cells, and stimulation of the AT receptor increases ETB receptor expression in Wistar-Kyoto (WKY) rats [abstract; Zeng C,, 26:80A, 2003]. We hypothesize that the ETB recept

• The Hippo pathway is a

  2022-07-20

  

  The Hippo pathway is a growth control signaling cascade that has been demonstrated to play an important role in regulating cell proliferation and differentiation [5,6]. The core signaling pathway consists of a group of kinases which negatively regulate the expression of transcriptional co-activators

• Multiple studies from our laboratory and

  2022-07-19

  

  Multiple studies from our laboratory and others, which have used stoichiometric kinetic analyses of ANP/NPRA, have provided strong evidence that bound ligand-receptor complexes are internalized and processed intracellularly, and that degraded products are released into the culture medium of various

• On the basis of the foregoing

  2022-07-19

  

  On the basis of the foregoing set of considerations, L1 could exert three possible actions on sGC determining its deactivation, schematically depicted in Fig. 6: i) oxidation of Fe2+ to Fe3+; ii) coordination to sGC, conjecturably, via the pyridyl nitrogen of the canthin-6-one; iii) coordinating and

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