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α-Bungarotoxin Despite having potent activity and good
2022-05-18

Despite having potent activity and good solubility, showed inhibitory activities against cytochrome P450 (CYP) 2C8, 2C9, and 2C19 with an IC value of less than 10 μM. In general, the specificity of the compound to the target should improve and the off-target risk such as CYP inhibitory activity sho
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Currently ursodeoxycholic acid UDCA is the
2022-05-18

Currently, ursodeoxycholic Altretamine (UDCA) is the only recommended and widely used drug in the treatment of CFLD. However, the clinical efficacy of UDCA is controversial. The most recent Cochrane review only identified a small number of trials assessing the effectiveness of UDCA [92]. The author
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br Results and discussion br Conclusion In
2022-05-17

Results and discussion Conclusion In conclusion, twenty-one 4-monocyclic aryl-5-carbamoyl-3-isoxazolols have been synthesized and evaluated for their antagonistic activities against housefly and common cutworm GABARs expressed in Xenopus oocytes. The TEVC results indicated that etretinate seve
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br Discussion and concluding remarks FPR
2022-05-17

Discussion and concluding remarks FPR1 is considered to be a promising drug target for treating inflammatory and immunological diseases. Thus, natural compounds that could block and/or regulate FPR1 activity may be an important source of novel therapeutics for modulating inflammatory processes. H
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5-Ethynyl-2'-deoxyuridine Considering their good FAAH in
2022-05-17

Considering their good FAAH inhibitory activity, compounds and have been selected for an in vivo study in a DSS-induced colitis model. Specific Pathogen Free male 7weeks old C57/Bl6 mice received 2.5% DSS in drinking water during 8days. Concomitantly, they were administrated daily intraperitoneall
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The third group also included samples belonging to
2022-05-17

The third group also included samples belonging to subjects with undetectable viraemia, for which the negative or persistence of the indeterminate WB result in subsequent samples indicated a non-HIV infection. In this subgroup, the VITROS HIV Combo test (as well as the other two tests) was negative
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mln0128 br Concluding Remarks Given the
2022-05-17

Concluding Remarks Given the increasing global incidence of metabolic disorders, new drugs that lower body weight and improve glucose tolerance are desperately needed. While we still have a long way to go, GPR55 might be an interesting target to explore, given its expression in numerous metabolic
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GPR detection by reverse transcription polymerase
2022-05-17

GPR35 detection by reverse transcription-polymerase chain reaction (RT-PCR). Total RNA of cultured DRG neurons was extracted using the RNAqueous kit (Ambion). Complementary DNA (cDNA) was synthesized from 1μg of isolated total RNA with SuperScript III reverse transcriptase (Invitrogen). An aliquot o
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It was reported that GPR is expressed
2022-05-17

It was reported that GPR120 is expressed on macrophages in adipose tissue (Oh et al., 2010). Whether GPR120-positive everolimus in human and rat pancreas belongs to macrophages was studied. CD68 is a transmembrane glycoprotein that is highly expressed by human monocytes and tissue macrophages (Hori
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The activation of the ERK pathway
2022-05-17

The activation of the ERK pathway may participate in the sensitization of primary afferents in pain transmission (Ji et al., 2009, Lai et al., 2011); the blockade of ERK activation in the DRG can decrease mechanical and heat hypersensitivity in inflammatory pain. IL-10 can inhibit phosphorylation of
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One of the main clinical issues of ABCB together with
2022-05-16

One of the main clinical issues of ABCB1, together with its impact on intestinal absorption, concerns its location at the BBB. Indeed, ABCB1 has been identified in the luminal side of endothelial cells and in the abluminal side of astrocyte endfeet processes of the CNS microvasculature [[36], [37],
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The general synthetic routes leading to aspartate and diamin
2022-05-16

The general synthetic routes, leading to aspartate and 2,3-diaminopropionate analogs, are shown in . As outlined in , aspartic Pyrrolidinedithiocarbamate ammonium analogs – were synthesized through standard carbodiimide-mediated coupling between an amine and an appropriately protected aspartic acid.
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A key limiting factor in the semi quantitative analysis of
2022-05-16

A key limiting factor in the semi-quantitative analysis of changes in the nuclear-to-cytoplasmic distribution of glucokinase is the large intercellular heterogeneity of CGP 35348 of glucokinase in both isolated hepatocytes in vitro and also in liver in vivo[13], [23], [24], [26], [36]. This necessi
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The HH signaling has also been implicated
2022-05-16

The HH signaling has also been implicated in the regulation of cancer stem DCPIB (CSC) by promoting their self-renewal [53]. Activated HH signaling has been identified in CSCs of many solid tumors, such as glioblastoma, breast, colon, pancreatic cancer, melanoma, and hematological malignancies, inc
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GLI proteins activate or repress transcription of their
2022-05-16

GLI proteins activate or repress transcription of their target genes by binding to a similar sequence motif within a cis-regulatory module (CRM) (Hallikas and Taipale, 2006, Peterson et al., 2012). Transcriptional responses to the HH pathway can be elicited either by de-repression of GLI-R or in oth
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