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NPC L expression is both tissue and species specific
2021-03-29
NPC1L1 expression is both tissue- and species-specific. Consistent with its function, NPC1L1 is mainly localized to the brush border membrane of enterocytes and the canalicular membrane of hepatocytes. NPC1L1, which is expressed in the liver of humans and rats but not mice, mediates cholesterol PF-5
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As expected the nortestosterone derived progestins tested we
2021-03-29
As expected, the 19-nortestosterone-derived progestins tested were moderate agonists of hAR (C), with EC50s ranging from 2 to 10nM, however all were less potent than the endogenous ligand DHT by at least a factor of 6, with relative potencies ranging from 0.0301 to 0.164. This is in agreement with p
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br Author contributions br Funding M E B
2021-03-29
Author contributions Funding M.E.B. was supported by Research Fund #3096. Competing interests Introduction Lung cancer has become one of the most common death causes in both male and female malignant tumors (Jemal et al., 2011). Air pollution, smoking and estrogen level are known risk f
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One possible pitfall of using EPAC activators in the treatme
2021-03-29
One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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Our study found a significant association between the degree
2021-03-29
Our study found a significant association between the degree of primary tumor lobulation and EGFR mutations status (P 1661010 synthesis status. However, only a small portion of these previous studies included the evaluation of lobulation, and almost all of them reported no association between EGFR
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Introduction Protein ubiquitination is a posttranslational
2021-03-27
Introduction Protein ubiquitination is a posttranslational modification that plays a major role in almost all cellular processes in eukaryotes (Hochstrasser, 2009; Komander & Rape, 2012). It involves the covalent attachment of ubiquitin (Ub) via its C-terminal glycine carboxylate to a primary amine
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br Conclusion The role of
2021-03-27
Conclusion The role of DNA-PK target in DNA DSB repair renders this Seratrodast kinase of great medicinal interest in cancer chemotherapy especially the cancer types of linked to DNA defects. Due to the absence of 3D DNA-PK target structure, different ligand-based methods were applied for design
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We also discovered important clues
2021-03-27
We also discovered important clues to domain ARCA Cy3 EGFP synthesis of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding r
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Indeed the alkyl group is not seen
2021-03-27
Indeed, the -alkyl group is not seen in the original crystallographic electron density omit map prior to positioning either inhibitor in DHODH, nor can it be found in the final maps. Rather, the electron density maps are consistent with hydrolysis of the amide to the acid. Once the scaffold was clea
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This hydrophobic biphenyl tail gave good binding
2021-03-27
This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC gap27 was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding interactions which were resp
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br Results and discussion br Conclusions
2021-03-27
Results and discussion Conclusions An optimization study of the dipeptidyl enoates was performed by chemical structure modifications (Fig. 5). Compound FGA50 displaying R configuration at C-3 was more active than its epimer FGA40. Two modifications of the chemical structure of FGA50 were done:
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The most important finding in the present study is
2021-03-27
The most important finding in the present study is that the EKR1/2-Egr-1 signaling pathway might be involve in the mechanisms underlying CysLT2 receptor-mediated IL-8 production. The signaling profile can be described by the following sequential processes: the agonists (LTC4 and LTD4) activates CysL
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In conclusion our work led
2021-03-27
In conclusion, our work led to the characterization of some signalling events of the CysLT1 receptor variants, at several levels, and showed that a punctual serine mutation could alter the response of receptors to cysLTs. Although atopy is a complex phenotype implicating different cell types, mediat
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In vivo study showed that the CYP A activity
2021-03-27
In vivo study showed that the CYP3A activity was increased, when morroniside (10, 30 and 90 mg/kg, i.g.) was daily for seven consecutive days. Further, RT-PCR analysis showed that the induction of mRNA Anisodamine by morroniside (10, 30 and 90 mg/kg, i.g.) was 1.13-, 1.43- and 1.79-fold higher, resp
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Coumarins also known as benzopyran ones are a family of
2021-03-27
Coumarins also known as benzopyran-2-ones are a family of nature-occurring lactones first isolated from Tonka beans in 1820. They are an important class of oxygen containing heterocycles widely found in nature, so much so that they have been routinely employed as herbal remedies since early days. Ov
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