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Since the localization of LO depends
2024-08-30
Since the localization of 5-LO depends on phosphorylation, we also analyzed the phosphorylation profile of 5-LO-WT and all isoforms by Western blot using specific beta-Nicotinamide mononucleotide against the phosphorylation sites S271 and S523. Whereas phosphorylation at S271 activates the 5-LO, in
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GS-7340 mg In this paper we describe the formation of a stru
2024-08-30
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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br Acknowledgement This work was funded by NIH NINDS
2024-08-30
Acknowledgement This work was funded by NIH/NINDS grant number NS080967 to C. Waites. Introduction Macro-autophagy also called autophagy is a conserved pathway for the lysosomal degradation and recycling of intracellular materials. It is instrumental for the homeostasis of cells and tissues a
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SB 225002 Compound was docked into the active site of Aurora
2024-08-30
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the
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The compounds containing beryllium act as strong
2024-08-29
The compounds containing beryllium act as strong Lewis acids because of electron deficiency of the Be GSK-LSD1 hydrochloride []. Interactions of X-Be-Y compounds with different Lewis bases have been studied by Yanez and co-workers [], extensively. Recently, they proposed a class of extremely strong
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However most of these SBVS studies
2024-08-29
However, most of these SBVS studies were focused on the target(s) for which crystal structures were available or have a similar template in PDB for comparative modeling. Besides, these were limited to SBVS only which relies on the rigid binding pocket, therefore, it may result in high false positive
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ionomycin br Current limitations and future directions
2024-08-29
Current limitations and future directions There are several limitations associated with PET imaging of aromatase using carbon-11 labeled aromatase inhibitors. Due to the very short half-life of carbon 11 (20min), PET studies with currently available, validated tracers can only be performed in med
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Since immunoassays cannot specifically quantify
2024-08-29
Since immunoassays cannot specifically quantify each apelin peptide, a more reliable approach, mass spectrometry (MS) has been used recently to quantify and characterize apelin fragments in plasma. Using this technology, Zhen et al. showed that [Pyr-1]-apelin-13 was the major apelin form present in
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Sorafenib was the first small RTK
2024-08-29
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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The Irbesartan Diabetic Nephropathy Trial
2024-08-29
The Irbesartan Diabetic Nephropathy Trial enrolled patients with type 2 diabetes, proteinuria of at least 0.9 g/24 h, BP >135/85 mmHg and moderate kidney impairment (creatinine 88 to 265 µmol/L in women or 106 to 265 µmol/L in men). Patients were randomized to receive irbesartan (titrated from 75 to
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br Guava tea leaves inhibit leukocyte type lipoxygenase
2024-08-29
Guava tea leaves inhibit leukocyte-type 12-lipoxygenase activity Guava tea that is extracted from guava leaves contains a number of polyphenols, and is commonly taken as a dietary supplement. The extracts show a variety of beneficial effects such as antioxidative, anti-inflammatory and antiprolif
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The binding of TQ to hsALDH changes the characteristic absor
2024-08-29
The binding of TQ to hsALDH changes the characteristic LJI308 spectrum of the enzyme. Therefore, TQ forms a complex with hsALDH and changes its absorption properties [39]. Ksv and Kb values indicate that the binding of TQ to hsALDH is very strong and of the order of static binding (complex formation
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br Introduction Psychostimulant abuse and addiction remain a
2024-08-29
Introduction Psychostimulant abuse and addiction remain a societal problem in the United States. The latest statistics from the National Survey on Drug Use and Health indicate that slightly less than one million people over the age of 12 report having a cocaine use disorder (NSDUH, 2016). Additio
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Extracellular ATP and downstream purinergic signaling have a
2024-08-29
Extracellular ATP and downstream purinergic signaling have also been proposed to contribute to dental pulp tissue healing and dentin regeneration. Mechanical and thermal stimulation of external dentin can induce ATP release in dental pulp through pannexins [13]. Cold stimulation was also reported to
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Glucose permeability studies demonstrated a high glucose flu
2024-08-29
Glucose permeability studies demonstrated a high glucose flux through the SF films used in the present work. Recent diffusion studies, including small molecular drugs and oxygen permeation through SF membranes [32], further support the quality of SF and its possible application as a material for bio
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