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As aforementioned this study aimed to design synthesize and
2025-01-06
As aforementioned, this study aimed to design, synthesize and investigate aromatase inhibitory and anti-breast cancer activities of N,N′-disubstituted thiourea derivatives. Based on the attractive phenotypic molecule 1, the synthetic N,N′-disubstituted thioureas have been designed including monothio
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Once apoptosis has been initiated
2025-01-06
Once apoptosis has been initiated the HMGA proteins themselves undergo marked changes in both the types and extent of their post-translational modifications (PTMs; review in [149,175]), some of which are likely correlated with alterations in chromatin structure. For example, the early stages of apop
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Complementing the effects of ARB and
2025-01-06
Complementing the effects of ARB and ACEI on HDL capacity to elicit cholesterol efflux, HDL of ARB- and ACEI-treated groups significantly lessened macrophage production of superoxide (Fig 2). As with efflux, there was no difference in this effect between the ARB and ACEI groups. These data are inter
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Intracellular Signaling Cascades From ligand sensitization t
2025-01-06
Intracellular Signaling Cascades. From ligand sensitization to translation of genes, all cellular processes are dependent on the intracellular levels and activity of partners involved in the signaling pathway. These signaling events lead to critical post-translational modifications including phospho
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br Conclusion We have identified three non
2025-01-06
Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina
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Aldose reductase AR is an NADPH dependent aldo keto
2025-01-06
Aldose reductase (AR), is an NADPH-dependent aldo-keto reductase very well studied as a catalyst of glucose conversion to sorbitol in the polyol pathway [11], [12]. In the diabetic lens characterized by chronically high levels of glucose, AR is responsible for production of high levels of sorbitol a
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Although several studies indicate that ALDH protects the
2025-01-06
Although several studies indicate that ALDH2 protects the heart from injury and maladaptive remodeling (reviewed in [11], [12], [13]), accumulating evidence indicates that deficiency of the enzyme could be protective as well. For example, mice expressing the defective Aldh2*2 mutation show lower ald
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THZ1 Hydrochloride The most widely recognized effects of ade
2025-01-04
The most widely recognized effects of adenosine are operated through inhibiting A1R, one of the most abundant G protein-coupled receptors in THZ1 Hydrochloride tissue [53]. A1R are located presynaptically, postsynaptically and nonsynaptically [54]. Effect of adenosine in neuronal circuits of adult m
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br Conclusion br Conflicts of interest br Introduction RNA i
2025-01-04
Conclusion Conflicts of interest Introduction RNA interference is a specific post-transcriptional gene silencing mechanism within a cell via the transfection of microRNAs (miRNA), exogenous small interfering RNAs (siRNA) or small hairpin RNAs (shRNA) [1–3]. Transfection of shRNA can be don
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The srd a isoforms showed
2025-01-04
The srd5a isoforms showed unique expression profiles in early FHM development (Fig. 2). Similar to amphibian embryos, there was a high abundance of both srd5a1 and srd5a3 at 1dpf in FHMs, suggesting that mRNA for these enzymes may be maternally deposited and that these enzymes may play a key role in
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Several approved and or experimental drugs together with nat
2025-01-04
Several approved and/or experimental drugs, together with natural compounds, have been reported to induce autophagy in different cancer types [70], [71], [72] (Table 1). In the next paragraphs, we will review more in detail a group of these agents selected in relation to their promising future outco
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Our conclusion was confirmed by two experiments The
2025-01-03
Our conclusion was confirmed by two experiments. The addition of aminopeptidase-specific inhibitors at high concentrations allowed us to exclude the possibility of substrate hydrolysis by other proteases present in the samples, for example, endoproteases. After the application of inhibitors, we were
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All desired compounds with a carboxylic acid substituent at
2025-01-03
All desired compounds with a carboxylic Tanshinone I substituent at N1 position of the quinoxalinone scaffold and a variety of aromatic substituents at C3 position were obtained by the syntheses starting from methoxy-substituted 3-chloro-quinoxalin-2(1)-ones () prepared as previously. As shown in ,
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The cavity volume of the binding pocket may
2025-01-03
The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino sodium butyrate molecular weight substitution within a binding pocket may result in a change in the cavity volume. T
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The mechanisms that control Ahr
2025-01-03
The mechanisms that control Ahr transcription are poorly understood, especially when considering cell type-specific regulation. A recent report suggested that the Ahr transcription might be directly promoted by RORγt [retinoic Oleandrin receptor (RAR)-related orphan receptor γt] based on ChIP-Seq a
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