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Since the cloning of ARs
2024-04-01
Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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We have expressed the ECDs of
2024-04-01
We have expressed the ECDs of the human α1, β1, γ and ɛ AChR subunits in the past using the methylotropic yeast Pichia pastoris as soluble glycosylated proteins [15], [16]. Further work with the γ subunit ECD revealed a marked improvement of the solubility and yield following the mutation of hydroph
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The role of DHT in
2024-04-01
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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In conclusion we have produced some highly potent inhibitors
2024-04-01
In conclusion, we have produced some highly potent inhibitors of P450 in comparison to the standard RN 1734 mg KTZ. Also, due to the limited specificity of these compounds against lyase in comparison to the 17α-OHase component, these compounds would be expected to have a major impact on corticoster
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br Autophagy inducers Macroautophagy is often
2024-04-01
Autophagy inducers Macroautophagy is often seen as a cellular process capable of increasing the fitness of GPCR Compound Library and overcome resistance to several forms of stress [9], [10]. As discussed above, it has been proposed by several authors that an effective strategy for enhancing sens
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In this paper we described
2024-04-01
In this paper, we described synthesis, biological evaluation and docking study of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives 4a–o as 15-lipoxygenase inhibitors. Results and discussion Conclusion We designed and synthesized a novel of thiourea derivatives containing phenylsulfonamide mo
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Exposure to cisplatin with ATR inhibitor resulted in an incr
2024-04-01
Exposure to cisplatin with ATR inhibitor resulted in an increase in cisplatin-DNA adducts, especially in cells with ATM deficiency. This finding indicates that suppressing ATR-Chk1 signaling with VE-822 enhances cisplatin activity by enabling the drug to form DNA adducts. Therefore, VE-822 may incre
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In recent years the higher lipophilicity thus better perform
2024-03-30
In recent years, the ‘higher lipophilicity’-thus-‘better performance’ tenet, derived from the polar paradox theory applied to micro-structured media, was challenged by novel and unexpected experimental results. In particular, the synthesis of many complete series of fatty adenosine deaminase esters
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GW9508 Later on Wayner Burton Ingold Barclay and Locke
2024-03-30
Later on, Wayner, Burton, Ingold, Barclay, and Locke (1987) modified the method by using lipid to examine the ability of an antioxidant GW9508 protect against lipid peroxidation generated by azo-compound. It was later improved using β-phycoerythrin (β-PE) as a fluorescent probe, and the ability of
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stavudine australia br Introduction Active oxygen radicals i
2024-03-30
Introduction Active oxygen radicals in the human body have a strong effect of inducing lipid peroxidation, which in turn induces oxidative imbalance and causes various diseases. Natural polysaccharides are substances with certain antioxidant activity. They are used as antioxidants and have advant
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AR Vs are truncated AR proteins lacking
2024-03-30
AR-Vs are truncated AR proteins lacking the AR ligand-binding domain (AR-LBD) [6]. While AR-Vs have frequently been detected in CRPC, their expression and functional role in benign prostate tissues and primary prostate cancers is not readily apparent. Structural rearrangements in the AR gene and alt
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PHA-665752 Here we found that AMPK directly
2024-03-30
Here we found that AMPK directly phosphorylates EZH2 at Thr311 to disrupt its interaction with SUZ12 and to inhibit PRC2 enzymatic activity, which is supported by the increased expression of PRC2-repressed genes. Furthermore, the T311E-EZH2 mutant that mimics AMPK-mediated phosphorylation status sup
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Terazosin br AMPK as a druggable target AMPK
2024-03-30
AMPK as a druggable target AMPK signaling has attracted considerable attention within the past decades, owing to the capacity of pharmacological compounds (e.g., 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside [AICAR] and metformin) or natural compounds (e.g., resveratrol) to activate AMPK in
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Interestingly our transgenic mouse model with macrophages ex
2024-03-30
Interestingly, our transgenic mouse model with macrophages expressing AdipoR1 showed not only improved insulin sensitivity and inflammation in skeletal muscle and adipose tissues, but fat mass, macrophage and plasma lipid accumulation and foam cell formation was also favorably reduced resulting from
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A c and CD are expressed
2024-03-30
A2c and CD73 are expressed in a small population of OSNs with pear-shaped morphology. In spite of the expression of molecular markers of ciliated OSNs such as Golf, ACIII, and OMP [1, 17], these OSNs have an extremely short dendrite and are located in the superficial layer of OE. In addition to the
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