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The extent to which GPCR oligomerization is
2024-10-11
The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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br Materials and methods br Results
2024-10-11
Materials and methods Results The clinical characteristics of the two selected groups are shown in Table 1. As shown in Table 1, the enzyme activity of ATX in CSF of MS patients (59.90±3.09nmol/min/ml±SEM) was significantly higher (p Discussion Numerous studies have so far shown that ATX tak
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Ryoichi et al modified potent clinical candidate VX with cya
2024-10-11
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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Previous studies have demonstrated ATR inhibition is
2024-10-10
Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia excitation emission cy5 to enhance chemotherapy sensitivity [[16], [17], [18],[20], [
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Fmoc-Asp-OAll mg br Materials and methods br Results br Disc
2024-10-10
Materials and methods Results Discussion In the present study, we found that SSTR2, SSTR5, and DA2R proteins are expressed in ACTH-positive Fmoc-Asp-OAll mg in healthy canine pituitary glands, with particularly high positive cell ratios in the intermediate lobes. Somatostatin has been repo
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br Conclusion br Acknowledgements br Introduction Synapses a
2024-10-10
Conclusion Acknowledgements Introduction Synapses are the fundamental elements of neuronal networks that enable the processing, encoding, and retrieval of information in the brain, and pathological disruptions in synapse structure are broadly held to underlie the development of neurological
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Methylpiperidino pyrazole Several structural classes of ASK
2024-10-10
Several structural Methylpiperidino pyrazole of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck
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Therefore the rational design of target compounds
2024-10-10
Therefore, the rational design of target compounds is based on the hybrid of attractive phenotypic bis-indole (5, Fig. 1) and sulfonamide moieties, in which the indole core might anticipate in hydrophobic interaction, and the functionality of sulfonamide group may involve in H-bonding with the site
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Chlorogenic acid an abundant polyphenol found in
2024-10-10
Chlorogenic mth1 pathway (7), an abundant polyphenol found in coffee and the human diet, has various biological activities including antioxidant and anticancer effects [54]. Jiang et al. reported that compound 7 had a selective cytotoxic activity on human oral tumor cells (HSG, HSC-2) as compared wi
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br Acknowledgements This work is sponsored by the National
2024-10-10
Acknowledgements This work is sponsored by the National Natural Science Foundation of China (grant no. 31201963) and Youth Backbone Teachers Project in Henan Province Department of Education, China (grant no. 2016GGJS-061). Introduction Acute lymphoblastic leukemia (ALL) is a malignant disord
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CORT induced hippocampal damage has been implicated in depre
2024-10-10
CORT-induced hippocampal damage has been implicated in depression, aging and long-term glucocorticoid therapy. Therefore, finding a drug that can protect hippocampal neurons from the adverse effects of CORT could have significant clinical benefits. In this regard, we tested the potential protective
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The functional similarity between GPR and APLNR ie both
2024-10-10
The functional similarity between GPR25 and APLNR, ie both can be activated by Apelin and Apela and are coupled to Gi-cAMP signaling pathway (Fig. 2, Fig. 3, Fig. 4), strongly suggests that GPR25 signaling may play important physiological and pathological roles in vertebrates more or less similar to
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br Conclusions and perspectives In view of the evidences sup
2024-10-10
Conclusions and perspectives In view of the evidences supporting that autophagy pathway MAS receptors mediate the effects of AT1 antagonists (Iwai et al., 2012, Ohshima et al., 2014, Pernomian et al., 2015, Schuchard et al., 2015), the prime targets from the perspectives on future directions in
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br Functional repercussions of each
2024-10-10
Functional repercussions of each trimming pathway A main difference between the two pathways presented in Fig. 1 lies in enzyme kinetics and selectivity. In pathway #1, the substrate for ERAP1 is free peptide, and so both kinetics and selectivity are determined by interactions between the peptide
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Another important finding of our study is the observation
2024-10-10
Another important finding of our study is the observation that high glucose per se does not affect TER in mature HREC monolayers; but at the same time it does upregulate ICAM-1 directly and activates HRECs to leukocyte adhesion. This would imply that high glucose affects TER in mature HREC monolayer
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