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Since natural and recombinant glycoprotein
2024-11-26
Since natural and recombinant glycoprotein hormones exhibit some differences in their carbohydrate structures, we checked whether this could affect the permissive effect on FSK-induced cyclic AMP response in MLTC-1 cells. Fig. 6 shows that the same sensitizing effect to FSK is observed with pituitar
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Phosphodiesterase inhibition increases the intracellular lev
2024-11-26
Phosphodiesterase inhibition increases the intracellular levels of cAMP to restore spontaneous contraction (Essayan, 2001, Qi and Kwan, 1996), acting downstream of adenylyl cyclase. Therefore, cardiac arrest induced by decreased intracellular cAMP levels could be reversed by phosphodiesterase inhibi
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The exact etiology of BPH is not completely
2024-11-26
The exact etiology of BPH is not completely understood, however this pathology has been associated with elevated ABT 724 trihydrochloride mg levels of the androgen DHT (10). Thus, a valuable strategy in BHP treatment is the reduction of DHT (10) levels, by inhibiting its biosynthetic production [6]
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Aurora A or B selective
2024-11-26
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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Preliminary results of studies sponsored by the manufacturer
2024-11-26
Preliminary results of studies sponsored by the manufacturer of ETC-1002 have also shown positive results for monotherapy in statin-intolerant patients and for the combined use of the ACL inhibitor plus other cholesterol-reducing agents. In patients with a documented history of intolerance to statin
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As previously mentioned when hypoxia treated cells become re
2024-11-26
As previously mentioned when hypoxia-treated cells become re-oxygenated they sustain a significant amount of DNA damage which has been attributed to the formation of reactive oxygen species . This finding represents more than just an interesting in vitro phenomenon as within a tumor, cells have been
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The structural analysis of the ASK activation
2024-11-25
The structural analysis of the ASK1 activation segment, which was not phosphorylated in the crystal structure, showed interactions mimicking those found in activated kinases. In addition, the isolated unphosphorylated ASK1-CD is active and able to autophosphorylate itself at three sites, Thr813, Thr
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Crystal structures were obtained of
2024-11-25
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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Inflammations lead to the perturbation of aromatase
2024-11-25
Inflammations lead to the perturbation of aromatase enzyme [112], which normally is responsible for a broad array of critical functions. Chemotherapy targets this enzyme, so this treatment option is never side-effect-free and not fully-effective. Therefore, the mankind should be careful so as not to
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Cy5 NHS ester (non-sulfonated) Angiogenesis refers to the fo
2024-11-25
Angiogenesis refers to the formation of new blood vessels from pre-existing vasculature [1]. Physiological angiogenesis is necessary for key processes such as wound healing, tissue regeneration and repair. In pathological conditions, including cardiovascular diseases, diabetes, cancer, and other pat
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This evidence suggests the strong
2024-11-25
This evidence suggests the strong clinical relevance of the identification of acquired resistance mechanisms for a proper therapeutic decision in patients with ALK-rearranged NSCLC. When the tissue is not available, the analysis of circulating tumor DNA (cfDNA) can be a valid alternative for the det
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Although several studies indicate that ALDH protects
2024-11-25
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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Gratifyingly compound also demonstrated improved physicochem
2024-11-25
Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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In this study we obtained the
2024-11-25
In this study, we obtained the absorbance and photoluminescence (PL) of ω-Agatoxin TK sale polymerized with various types of actin-binding proteins in order to probe the actin structures in situ without labeling. Both optical measurements have been useful in examining biomaterials such as DNA and pr
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Molecular docking simulations were carried out for ligands i
2024-11-25
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic Pr
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