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As one of the two receptors for
2019-07-12
As one of the two receptors for the primordial chemokine CXCL12, ACKR3 exists in jawless fish (Bajoghli, 2013, Nomiyama et al., 2011, Venkatesh et al., 2014). The sea lamprey genome contains two copies of the ACKR3 gene (Ensembl Acc. Nos.: ENSPMAP00000011187 and ENSPMAP00000011401) (Table 1), both e
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While several C terminal peptides have been
2019-07-12
While several C-terminal peptides have been reported to have modest (astressin) or substantial (astressin2-B, antisauvagine-30) subtype selectivity for the CRF2 receptor (), [125I]YP20 is the first reported small analog of the C-terminus of CRF exhibiting subtype selectivity for the CRF1 receptor vs
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Our recent discovery M P H R A S
2019-07-12
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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Estrogen receptor related receptor ERR like other members of
2019-07-12
Estrogen receptor-related receptor γ (ERRγ), like other members of the ERR subfamily, is a constitutively active orphan nuclear receptor, though unlike ERRα and β, it is more selectively expressed in metabolically active and highly vascularized tissues such as heart, kidney, brain, and skeletal musc
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br Disclaimer Statement br Introduction The erythropoietin p
2019-07-12
Disclaimer Statement Introduction The erythropoietin-producing hepatoma (Eph) receptors represent the largest class of receptor tyrosine kinases (RTKs). They are type I transmembrane proteins that interact with their membrane-bound ligands the ephrins and facilitate cell-to-cell contacts resul
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Cynomolgus HGF / Hepatocyte Growth Factor Protein Next our
2019-07-11
Next, our exploration shifted to modifications at the lateral chain of the benzoquinone nucleus (SAR 2). Considering that the CK2 inhibitory activity is favoured by the presence of the -Ph-4-NO2 (SAR 1), the subsequent analogues were investigated with this moiety retained. The influence of the side
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br Results and discussion br Conclusion br Experimental sect
2019-07-11
Results and discussion Conclusion Experimental section Pharmacological studies Introduction Survival analysis is a set of statistical methods that aim at modeling the relationship between a set of predictor variables and an outcome variable and, in particular, prediction of the time w
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Mesoridazine Besylate weight The action of pt PGE as an EP r
2019-07-11
The action of 17-pt-PGE2 as an EP1 receptor agonist [34] was demonstrated in several experimental settings, including cancer, neurons, vascular system, kidney and was confirmed by application of EP1 receptor selective antagonists [35], [36], [37], [38], [39], [40], [41]. Receptor binding studies in
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Almorexant Accumulating evidence suggests that certain abnor
2019-07-11
Accumulating evidence suggests that certain abnormal emotional traits, such as impulsive aggression and cluster B personality, are associated with suicidal behaviors (Currier and Mann, 2008, Mann et al., 2009, Rujescu et al., 2007, Turecki, 2005). Impulsive aggression appeared to be associated with
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mitotic inhibitor Glycolysis is important to maintain the vi
2019-07-11
Glycolysis is important to maintain the vital functions of T. gondi. Extracellular T. gondii shift its mitotic inhibitor metabolism towards glycolysis, based on the observation that a relocation of glycolytic enzymes from the cytosol to the pellicle occurs at the time when tachyzoites egress from h
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Several studies on the collagen receptor
2019-07-11
Several studies on the collagen receptor DDR1 have revealed a defined collagen signaling pathway that causes cell scattering and cadherin switching. As mentioned earlier, DDR CPI-203 on collagens are distinct from integrin binding sites; therefore, the same collagen protein can bind to DDR and inte
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GLP signaling mediates important renal
2019-07-11
GLP-1 signaling mediates important renal functions [101], as suggested by the expression of both DPP-4 and GLP-1R in the kidney of several species, including humans [102]. However, controversial data exists on the specific expression pattern of these proteins, based on the specificity and sensitivit
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A set of small molecule LigI inhibitors were identified
2019-07-11
A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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br Material and methods br Discussion First we
2019-07-11
Material and methods Discussion First, we investigated cannabis use, and results showed that the lifetime prevalence of cannabis use in our sample was 29.63%, with a significant difference between males (73.8% of the abusers) and females (26.2%). Moreover, the mean age and age at onset were si
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br Dienogest DNG Dienogest is a nortestosterone derivative w
2019-07-11
Dienogest (DNG) Dienogest is a 19-nortestosterone derivative with two special structural changes [Fig. 1a]: [a] At the cabon-17 position there is a cyanomethyl group instead of an ethinyl group; [b] A double bond is present between carbons 9 and 10. DNG is the only progestogen that combines prope
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