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br Conclusions Triptans are HT B D F receptors agonists
2022-11-08

Conclusions Triptans are 5-HT1B/1D/(1F) receptors agonists and are considered as the gold standard for acute migraine treatment that have been proven effective. Unfortunately, they are contraindicated in patients with cardiovascular diseases due to their vasoconstrictor (side) effects (MaassenVan
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phosphodiesterase inhibitors br Introduction Adenosine deami
2022-11-08

Introduction Adenosine deaminase (ADA), also known as adenosine aminohydrolase, is a key enzyme involved in the purine metabolism that converts adenosine to inosine irreversibly (Lupidi et al., 1997). It is a zinc containing metalloenzyme present in both prokaryotes and eukaryotes. In humans ADA
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Compounds were profiled for their inhibitory
2022-11-08

Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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Overexpression of SMAD and SMAD strongly enhanced
2022-11-08

Overexpression of SMAD3 and SMAD4 strongly enhanced luciferase activity of the new pN10 reporter gene construct which was further reinforced by addition of TGFβ. Serial mutations of SBE-1 and SBE-2 led to a slight loss in 5-LO promoter inducibility. The data demonstrate that the two SBEs within the
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br Patients and Methods br Results br
2022-11-08

Patients and Methods Results Discussion Gjerdrum et al showed that Axl bet bromodomain is required to maintain the mesenchymal-like invasiveness of metastatic breast carcinoma cells, but Axl knockdown has no effect on the cell proliferation of MDA-MB-231 cells. Mackiewicz et al also showed
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Matthew et al synthesized and carried out SAR studies
2022-11-08

Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that capmatinib 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3),
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Introduction An association of elevated
2022-11-08

Introduction An association of elevated branched-chain mitotane (BCAA—Leu, Val, Ile) with obesity and insulin resistance was first reported nearly 50 years ago (Felig et al., 1969). With the advent of metabolomics technologies, it has since become apparent that the association of BCAA and related
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Asiatic acid Chromatin proteins play important roles in gene
2022-11-08

Chromatin proteins play important roles in gene expression and DNA repair. The importance of chromatin composition on gene expression is exemplified by X-inactivation, where one of the two X chromosomes in female mammalian Asiatic acid is transcriptionally silenced by heterochromatin , , , . In the
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The incremental reduction albeit not statistically
2022-11-07

The incremental reduction, albeit not statistically significant, in collagen I with LCZ696 compared to perindopril treated animals, may therefore be related to a more compliant ventricle in LCZ696-treated animals. This is not so surprising given the incremental anti-fibrotic effect of the active met
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As noted above yeasts particularly S cerevisiae
2022-11-07

As noted above, yeasts, particularly S. cerevisiae (Frey and Röhm 1978; Trumbly and Bradley 1983), produce APs, but these are intracellular enzymes located in the vacuolar compartment, with the exception of aminopeptidase II. About 40% of aminopeptidase II activity is detected as external enzyme, li
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Recently two distinct small molecule
2022-11-07

Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Cy3-UTP sale with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the gr
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In large biopsies series from ALK
2022-11-07

In large biopsies series from ALK+ NSCLC treated patients, the number of detected mutations increased after second generation ALKi (Gainor et al., 2016) and in one study were present in 56% of the entire cohort (Shaw et al., 2013b). For example, the rate of G1202R mutations increases from 2% in post
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br Translational Considerations Targeting the AHR Pathway
2022-11-07

Translational Considerations Targeting the AHR Pathway Modulating AHR function offers exciting therapeutic potential in host immunity and inflammation. However, the emerging concept of AHR function in a cell type-specific manner, combined with differences between AHR activation in cell culture in
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A highly attenuated B pertussis strain named
2022-11-07

A highly attenuated B. pertussis strain, named BPZE1, has recently been described [10]. It produces enzymatically inactive pertussis toxin (PT), no dermonecrotic toxin and only trace amounts of tracheal cytotoxin. Markedly reduced lung pathology was observed in mice intranasally (i.n.) infected with
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Metformin s pluripotent roles are alluded to in terms
2022-11-07

Metformin's pluripotent roles are alluded to in terms of its antitumorigenic, glucose-lowering, and cardioprotective effects, which are due in part to its upregulation of AMPK activity [39,40]. Metformin's glucose-lowering effect is a result of reduced hepatic gluconeogenesis, whereas improved insul
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