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The NF B family of transcription factors is involved in
2021-10-02

The NF-κB family of transcription factors is involved in acquisition of resistance to anticancer drugs as well as to apoptosis. NF-κB-mediated mdr1 gene upregulation is part of the anti-apoptotic protection mechanism of proximal tubule (PT) aa-dutp synthesis against cadmium-induced oxidative stress
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In conclusion our results show that P C enhances
2021-10-02

In conclusion, our results show that P7C3 enhances endogenous neurogenesis by upregulating the generation of endogenous neuroblasts and neural stem/progenitor cells by increasing the expression of neuroprotective proteins (Bcl-2, ki67, DCX, adam11, adamts20, and β-tub3) by activation of the cAMP/PKA
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Despite having potent activity and good solubility showed
2021-10-02

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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guanabenz To obviate the mitogenic FGF activity several engi
2021-10-01

To obviate the mitogenic FGF19 activity, several engineered FGF19 variants have been generated aiming to maintain the metabolic activity excluding the protumorigenic ones. One variant, M70, that differs from wild-type FGF19 by 5-amino acids deletion at the N-terminus and the substitution of 3-amino
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Here we investigated on epigenetic regulatory mechanisms
2021-10-01

Here, we investigated on epigenetic regulatory mechanisms of ALX/FPR2 expression. Epigenetic changes, that include phosphorylation, acetylation, methylation and ubiquitination of DNA and histone proteins, occur in a variety of diseases [21] and are being recognized as key targets for personalized me
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On the contrary the benzhydrol
2021-10-01

On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the s equol tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compared to the unsubst
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The H R antagonist cimetidine
2021-10-01

The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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It was speculated that could affect the protein
2021-10-01

It was speculated that could affect the protein translation or processing in the HCV replication cycle. The viral protein processing was thus investigated, to establish whether the HCV inhibition was determining an increased amount of unprocessed polyprotein, due to a block in the processing, or a
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Not all metals are susceptible of being accumulated by insec
2021-10-01

Not all metals are susceptible of being accumulated by insects. Tissue concentrations of essential metals like Cu and Zn are regulated in many insects and hence cannot be used to biomonitor metal pollution (Hare, 1992). A similar behaviour could explain the observed stability of Zn and Cu relative t
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faah inhibitors Mice with GSTP knock out show
2021-10-01

Mice with GSTP1 knock out show increased risk of skin cancer when exposed to carcinogens like polycyclic aromatic hydrocarbons [23]. Most of the genetic association studies have focused on GSTP1 c.313G > A variant which results in isoleucine to valine substitution at amino faah inhibitors residue nu
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Calcium mobilization FLIPR assay CHO K cells expressing an
2021-10-01

Calcium mobilization (FLIPR) assay: CHO-K1 cells expressing an NFAT-β-lactamase reporter and the promiscuous Gα-subunit Gqi5 were stably transfected with either empty vector (pCDNA3.1, Invitrogen) or vector expressing HA-GPR81, GPR109A or GPR109B. Cells were seeded at 10,000cells/well in 384-well cu
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The intracellular signaling that mediates the adipogenesis i
2021-10-01

The intracellular signaling that mediates the adipogenesis induced by GPR120 still remains largely unknown. In the present study we showed that TUG-891 induced the activation of [Ca2+]i and ERK1/2 signaling in 3T3-L1 cells. Moreover, incubation of TUG-891 combined with BAPTA-AM or U0126 abolished TU
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GPR A a G protein coupled receptor located mainly
2021-10-01

GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic Okadaic acid [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-media
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Previous studies showed that pregnancy rate improves when ew
2021-10-01

Previous studies showed that pregnancy rate improves when ewes have a BCS that exceeds a minimum threshold [43]. The pregnancy rate is increased in sheep with BCS ≥2.5 [44] and >2 [45]. In this work, pregnancy rate was higher in the GnRH group with low BCS compared to the hCG and Control groups. Des
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AFB Fapy dG has been long recognized as
2021-10-01

AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by T7 Tag Peptide excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB1-Fapy-dG f
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