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Nowadays more than kinases have been identified of
2024-08-19
Nowadays, more than 500 kinases have been identified of human genome [2]. Imatinib (Gleevec) was the first tyrosine kinase inhibitor approved by the US Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia [3], and kinases have become an attractive target for the developme
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Matthew et al synthesized and carried out
2024-08-19
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that I-BET151 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), EC
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Here we report discovery of highly selective
2024-08-19
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Estradiol Cypionate bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interac
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YO-01027 mg The GRAVY value for a protein is calculated as
2024-08-19
The GRAVY value for a protein is calculated as the sum of hydropathy values of all the amino acids, divided by the number of residues in the sequence (Kyte and Doolittle, 1982). According to Kyte and Doolittle (1982) integral membrane proteins typically have higher GRAVY scores than do globular prot
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Although several different membrane estrogen receptors have
2024-08-19
Although several different membrane estrogen receptors have been reported (Qiu et al., 2008; Revankar et al., 2005), a large percentage of membrane-initiated steroid hormone signaling appears to be performed by a subpopulation of the same receptors that act in the nucleus. Specifically, estrogen rec
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Since obesity appears to impact
2024-08-19
Since obesity appears to impact leptin and adiponectin levels in opposite manners, several studies have suggested that the serum adiponectin/leptin ratio may be a key parameter in indicating the relative risk of postmenopausal breast cancer (Ollberding et al, 2013, Cleary et al, 2009). Therapeutic s
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Several MAP kinases are involved in the signal transduction
2024-08-19
Several MAP kinases are involved in the signal transduction pathways that lead to the upregulations of inflammatory mediators. Moreover, transcriptional activations of STATs are regulated by MAP kinases, as evidenced by reports that p38 MAPK is necessary for the S727 phosphorylation of STATs (Kovari
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MMP is the most critical
2024-08-19
MMP9 is the most critical protease which is involved in the degradation of ECM. TIMP-1 is an important regulator in the synthesis and degradation of ECM [8,9]. Hepatic TIMP-1 expression significantly increases in patients with liver fibrosis [10]. Serum level of TIMP-1 expression is positively assoc
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Recently whey products have been added
2024-08-19
Recently, whey products have been added to nutritional beverages to boost their antioxidant capacity. Supplementation of a lemon drink with 1% WP hydrolyzed by subtilisin increased the antioxidant activity of the beverage from 0.75 to 7.79 mmol of TE/L (Athira et al., 2014). In addition, a flavored
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Given that neither case is derived from
2024-08-19
Given that neither case is derived from multiplex Loxapine Succinate with affected individuals, principles of Mendelian segregation cannot be applied to implicate the T201S mutation in causing familial CJD. In addition, like many rare gene variants, it is not possible to apply practice guidelines su
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Consistent with the in vitro results memantine ameliorated
2024-08-19
Consistent with the in vitro results, memantine ameliorated Aβ-induced cytotoxicity in rat primary cortical cultures. Studies reported that memantine protected neurons against the damage caused by aggregated Aβ40 or Aβ42 oligomers in vivo[26], [27]. These results suggest that, in addition to its neu
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Dose Response Studies Against Puromycin Sensitive Aminopepti
2024-08-19
Dose–Response Studies Against Puromycin–Sensitive Aminopeptidase (PSA). PSA is a ubiquitous metallopeptidase encoded by the NPEPPS gene with subcellular distribution in the cytosol and nucleus [49]. Comprising of a 919 amino Protionamide sequence, it has a broad substrate specificity, and is respon
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br Discussion With recently improved understanding of the ro
2024-08-17
Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1)
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It is well accepted that PKA is a
2024-08-17
It is well accepted that PKA is a key enzyme activated at the beginning of the capacitation process [69]. As mentioned above phosphorylation/inactivation of cofilin in sperm is a PKA dependent process [58]. We could not see any change in cofilin phosphorylation level by adding the PKA activator 8Br-
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In this study PRP positively regulated MIIP
2024-08-17
In this study, PRP4 positively regulated MIIP levels and significantly inhibited the invasion of HCT116 cells. Further investigations elucidated that PRP4 dephosphorylated MIIP via PP1A regulation, which was confirmed by PP1A inhibition in the presence of OA. Upon dephosphorylation, MIIP possibly in
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