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Recently considerable effort has been invested
2022-03-10

Recently, considerable effort has been invested in developing FDPS inhibitors based on alternative scaffolds (including nonbisphosphonates) that allow other tissue types and parasite-derived forms of FDPS , to be targeted. There are several limits in analyzing inhibitors of FDPS activity: the most w
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Focal adhesion kinase FAK is a
2022-03-10

Focal adhesion kinase (FAK) is a non-receptor type tyrosine kinase that can further cooperatively interact with receptor tyrosine kinase signaling to regulate adhesion, migration, survival, proliferation, polarization, and differentiation [12]. Following activation, phosphorylated extracellular regu
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There has been conflicting evidence on the possible receptor
2022-03-10

There has been conflicting evidence on the possible receptor mechanisms that mediate the neuro-immuno-modulatory effects of FAAH substrates. Evidence from in vitro studies indicates that AEA-mediated modulation of TLR4-induced neuroinflammation may be mediated by CB1/CB2 receptor dependent (Correa e
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Signaling pathways such as BMP FGF and WNT are
2022-03-10

Signaling pathways such as BMP, FGF, and WNT are strongly involved in the process of endochondral ossification and Meckel's cartilage development [20]. Interestingly, absence of BMP antagonist, Noggin, in Meckel's cartilage, resulted in a phenotype, very similar to that of Setdb1 CKO [16]. To examin
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urat1 inhibitor Our results further indicate that low expres
2022-03-10

Our results further indicate that low expression of p300/CBP in CRC is directly associated with poor clinical therapeutic outcome of 5-FU treatment, potentially providing a new set of biomarkers to predict chemo-sensitivity. Although the ability of low expression of p300/CBP to predict poor prognosi
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br Conclusion br Author contributions br Ethics
2022-03-10

Conclusion Author contributions Ethics approval Competing interests Introduction VHL is a well-known tumor suppressor and works as a target recruitment subunit of an E3 ubiquitin ligase complex that recruits hydroxylated hypoxia inducible factor α (HIF-α) for proteasomal degradation u
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br Structural studies of the cyclase catalytic domains
2022-03-10

Structural studies of the cyclase catalytic domains Structural determinants for catalytic activity The structure of the active αβGCcat structure has remained elusive. However, several studies have suggested how specific structural elements are involved in αβGCcat transitioning from the open in
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The GPR gene was included in our survey because
2022-03-09

The GPR35 gene was included in our survey because of its location immediately 3′ to CAPN10 and because it showed evidence of association with type 2 diabetes. Also, its expression in tissues including pancreatic islets and skeletal muscle is consistent with a possible role in type 2 diabetes. Our re
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br Materials and methods br Results In this study we
2022-03-09

Materials and methods Results In this study we re-examined the kinetics of ET transport and tested the ability of various suggested substrates of OCNT1 to inhibit ET uptake. Using a native ET transporter expressed in the human HeLa cell line ET was found to be taken up with a Km of 51 μM and V
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The lactam compounds including ceftriaxone CEF have
2022-03-09

The β-lactam compounds, including ceftriaxone (CEF), have shown to attenuate drug-seeking in several drugs of abuse including methamphetamine [31], cocaine [32,33], nicotine [34] and morphine [35]. Moreover, in our laboratory, we have shown that CEF can reduce chronic alcohol drinking via upregulati
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br Clinical trials testing GLP mimetics in AD or
2022-03-09

Clinical trials testing GLP-1 mimetics in AD or PD patients GIP analogues show good neuroprotective effects in animal models of AD and PD Glucose-dependent insulinotropic polypeptide (GIP) is a 42-amino PIK-75 incretin growth factor which activates pancreatic islets to enhance insulin secreti
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br Acknowledgements br Introduction Ghrelin is
2022-03-09

Acknowledgements Introduction Ghrelin is a potent orexigenic hormone and growth hormone secretagogue mainly derived from the stomach [1], [2], [3], [4], [5]. Other pleiotropic actions of the hormone include those that are glucoregulatory, food reward-enhancing, gastric motility-enhancing, and
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The effects of GHS R a blockade
2022-03-09

The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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Berberine hydrochloride receptor Similar to C lividipennis R
2022-03-09

Similar to C. lividipennis RDL (Jiang et al., 2015), we found that the intracellular loop variants of A. mellifera RDL had no effect on GABA EC50 (Table 1). Also, as with C. lividipennis, there was no significant difference in maximal GABA responses (Table 1). However, whereas the 31 amino acid inse
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An advantage of photolabeling with tritiated photoprobes fol
2022-03-09

An advantage of photolabeling with tritiated photoprobes followed by microsequencing with Edman degradation is the ability to both identify the photolabeled mgmt inhibitor and to quantify photoincorporation which enables assessment of pharmacological specificity and allosteric interactions with oth
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