• It is important to note that the GC

  2022-06-15

  

  It is important to note that the GC-C expression is retained in colon tumours, and therefore GC-C expression can be used as a marker to diagnose metastatic colon cancer [42]. However, expression of uroguanylin and guanylin is often lost in colorectal cancer progression [43]. Therefore, the anti-prol

• SC 79 A nitric oxide donor glyceryl trinitrite and the

  2022-06-15

  

  A nitric oxide donor, glyceryl-trinitrite, and the substrate for nitric oxide, l-arginine, have been used to treat preterm labor. However, these studies are preliminary. The beneficial effect of nitric oxide donors needs to be confirmed by more controlled studies. The probable pitfall of using nitri

• Having identified initial leads and further lead

  2022-06-15

  

  Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic phosphocholine derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl,

• Initially the synthesized compounds from were evaluated for

  2022-06-15

  

  Initially, the synthesized compounds from were evaluated for human GSNOR potency before generating additional SAR in order to understand scaffold feasibility and required functionality as illustrated in . Commercially available 4′-hydroxy-[1,1′-biphenyl]-4-carboxylic CTX0294885 having similar termin

• On the other hand it is quite possible that

  2022-06-14

  

  On the other hand, it is quite possible that strychnine-sensitive glycine sites are responsible for mediating the anticonvulsant effects of GlyT1 inhibitors. Strychnine, which acts as an antagonist at these sites, is a well-known as a convulsant drug, and elevation of endogenous glycine levels at th

• We first investigated the influence of the acyl

  2022-06-14

  

  We first investigated the influence of the -acyl group of the glycine amide side chain and found that shorter linkers lead to better activities (–); simple -benzoyl substituents were always superior to the 3-arylpropanoyl group present in the high-throughput hit (). Electron withdrawing substituents

• Ironically another series of studies examining the role of

  2022-06-14

  

  Ironically, another series of studies examining the role of EAATs in CNS injury and disease suggest that under some pathological conditions, the operation of the EAATs is not protective, but actually contributes to the excitotoxic process (Rossi et al., 2000). The transporters do so by serving as th

• Further explorations at the ortho and meta positions of the

  2022-06-14

  

  Further explorations at the ortho- and meta-positions of the phenyl in the tail proceeded on the basis of the preliminary results. First, we investigated the fluorine group at the meta- (13p) and ortho-positions (13q) of the phenyl group, with both compounds being slightly less potent than 13o. Surp

• br Redox regulation in the brain Reactive

  2022-06-14

  

  Redox regulation in the brain Reactive oxygen species are generated in bryostatin by the mitochondrial respiratory chain, which occurs on the inner mitochondrial membrane (Murphy, 2009, Jensen, 1966, Dickinson and Chang, 2011). Interestingly, although most cancer cells are thought to primarily r

• In this present study the availability of commercial

  2022-06-14

  

  In this present study, the availability of commercial GLUT and SGLT EDTA receptor directed against different epitopes, enabled us to screen for members of the SGLT family and compare the expression patterns of GLUTs and SGLTs in the different regions of the rat lens. Based on these regional and subc

• Our data suggest that Slc a is

  2022-06-14

  

  Our data suggest that Slc38a5 is important for amino-acid-induced α cell proliferation and expansion of α cell mass following GCGR inhibition, but not for formation and maintenance of α cell mass. This is supported by the finding that Slc38a5−/− mice have normal α cell mass. This is interesting sinc

• More recently NMR techniques have been used to monitor

  2022-06-14

  

  More recently, NMR techniques have been used to monitor K+ () fluxes in isolated rat hearts. These reveal an increased rate of passive efflux of from Langendorff-perfused hearts at 20°C compared to 36°C or 10°C (Gruwel, Kuzio, Xiang, Deslauriers, & Kupriyanov, 1998). Similar experiments assessed th

• br Materials and methods br Transparency

  2022-06-14

  

  Materials and methods Transparency document Acknowledgments Introduction Hearing loss is the most common congenital sensory deficit. About 1–3 in 1000 children are affected at birth or during early childhood by severe hearing loss, which is defined as prelingual deafness, with at least h

• Despite their undisputed importance however FPR receptors

  2022-06-14

  

  Despite their undisputed importance, however, FPR receptors are not in the limelight of GPCR-related research (for review [12] and references therein). We, therefore, draw attention to this GPCR receptor family, in order to re-initiate FPR-related research, particularly in the light of biased agonis

• br Materials and methods br

  2022-06-13

  

  Materials and methods Results Discussion In the absence of vascularization phenomena, endothelial cells (ECs) are among the most quiescent cells of the body [27]. ECs proliferation is significant during embryogenesis, as the vasculature is being formed, while in the adult life takes place o

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