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Recently two distinct small molecule inhibitors of PHGDH wer
2024-09-25
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 (R)-PFI 2 hydrochloride with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, redu
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Introduction Increasing environmental pollution caused
2024-09-25
Introduction Increasing environmental pollution caused by heavy metals, originating mainly from industrial processes and urban activities, as well as the widespread application of pesticides, fertilizers, manure and sewage sludge, has posed a serious problem for safe food production and become a po
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It is also possible that adrenoceptor activation may
2024-09-25
It is also possible that α2-adrenoceptor activation may inhibit glutamate accumulation by upregulating the glutamate-buffering activity of Müller 2-Deoxycytidine through EAAT1 or adjusting EAAT2 in bipolar cells, as well as the NMDA receptor. Therefore, we investigated whether topical administration
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HT receptors are distributed throughout the
2024-09-25
5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and Triphosphate structure and function (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes
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Although the role of mossy fiber sprouting in epileptogenesi
2024-09-25
Although the role of mossy fiber sprouting in epileptogenesis has been challenged (Elmer et al., 1997, Nissinen et al., 2001), in addition to astrogliosis, mossy fiber sprouting is one of the characteristic histopathological findings in TLE (Kharatishvili et al., 2006, Pitkanen et al., 2007, Represa
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br There is evidence to
2024-09-25
There is evidence to suggest that GMF activities are regulated in vivo by post-translational modification. indeed, there is strong precedent for ADF-homology family proteins being regulated in this manner. Cofilin is inhibited by phosphorylation of a serine residue at its N terminus. This residue
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GYKI 52466 dihydrochloride Caffeic acid dihydroxycinnamic ac
2024-09-24
Caffeic GYKI 52466 dihydrochloride (3,4-dihydroxycinnamic acid) is a natural compound that inhibits 5-LO and exerts potent anti-inflammatory and antioxidant properties. Recently, Takeda et al. reported that caffeic acid provided neuroprotective and anti-depressive activities [23]. Sertraline, a sel
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Thus one possible target for CRPC treatment is
2024-09-24
Thus one possible target for CRPC treatment is the enzyme 17,20-lyase, which plays a crucial role in androgen biosynthesis. This is because inhibition of 17,20-lyase would be expected to decrease serum androgen levels secreted not only by the testes but also by the adrenal glands.7, 8, 9 In recent
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MLN another selective Aurora A inhibitor
2024-09-24
MLN8237, another selective Aurora-A inhibitor is said to be more potent than MLN8054 and to cause less benzodiazepine-like side effects based on structure modulation by the addition of a methoxy group to either end of the MLN8054 molecule. It was studied [62] in a once daily (QD) schedule for 7 days
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In addition to drawing attention to Ser of ACL
2024-09-24
In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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br Interaction between ASK and
2024-09-24
Interaction between ASK1 and TRX Thioredoxins are small (∼12kDa) dithiol oxidoreductases ubiquitously expressed in species ranging from plants to archaea and mammals. They perform various biological functions, such as reducing protein disulfide bonds, supplying reducing equivalents to redox tyram
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br Author contribution br Acknowledgement br Introduction Si
2024-09-24
Author contribution Acknowledgement Introduction Since the initial finding of Gould et al. [1], showing the loss of dendritic spines in the hippocampus after ovariectomy and its rescue after treatment of the animals with estradiol, a tremendous number of studies have demonstrated a role of
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To investigate if WP increased CAT activity in cells
2024-09-24
To investigate if WP increased CAT activity in cells, C2C12 muscle 4 mu mg were treated with 0.1 to 0.4 mg/mL of WP (80.05% protein) for 24 h and then stressed with 0.75 mM H2O2 for 1 h (Xu et al., 2011). The CAT activity was significantly enhanced from 15.1 ± 0.7 to 23.7 ± 1.3 U/mg of total cellul
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br Small molecule homoisoflavonoid in combination with anti
2024-09-24
Small molecule homoisoflavonoid in combination with anti-VEGF therapy Basavarajappa et al. [11] reported a new synthetic homoisoflavonoid compound, SH-11037 by modifying the structure of naturally occurring homoisoflavonoid cremastranone. SH-11037 exhibited promising inhibition of human retinal m
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br Acknowledgements This work was supported by
2024-09-23
Acknowledgements This work was supported by Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), Fundação de Amparo à Pesquisa do Estado do Rio Grande do Sul (FAPERGS) FINEP research grant “Rede Instituto Brasil
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