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Epiandrosterone synthesis In Rainey et al published the resu
2024-01-22
In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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Protein phosphorylation is an important posttranslational
2024-01-22
Protein phosphorylation is an important posttranslational mechanism for the regulation of distribution, trafficking, and function of modified proteins (Wang et al., 2014). GluA1 phosphorylation at S845 also has functional consequences (Lu and Roche, 2012). For instance, S845 phosphorylation drove tr
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Crystal structures were obtained of sulfonamide and amide as
2024-01-22
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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Although the exact mechanisms are not fully understood IGF
2024-01-22
Although the exact mechanisms are not fully understood, IGF-1 is tightly linked with ER and estrogen actions and a crosstalk occurs between these two systems in breast cancer. To illustrate this close relationship, studies have identified a synergy between IGF-1 and estrogen in Ranitidine synthesis
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Based on its kinetic parameters and quaternary structure R
2024-01-22
Based on its kinetic parameters and quaternary structure, R. pycnus arginase is a typical ureotelic L-arginase [2]. The Km value of the enzyme was lower than other arginases from other organisms (Table 2), including S. cerevisiae (15.7mM), B. anthracis (10mM), B. caldovelox (3.4mM), human liver (2.3
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MiR has already been implicated in
2024-01-22
MiR-21 has already been implicated in the protective effects of Res on lung fibrosis, but the molecular mechanisms are underexplored. Our results showed a clear increase of activation protein 1 (AP-1) activity after TGF-β treatment, which was suppressed by Res in a dose-dependent manner, suggesting
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Since the beginning of s
2024-01-22
Since the beginning of 1990s, more than 17,000 papers about physiological relevance of antioxidants have been published according to data from web of science. Based on the available literature, it seems that assessing the antioxidant potential of food by means of in vitro assays or solely epidemiolo
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Protein arrays provide a new approach for
2024-01-22
Protein arrays provide a new approach for the identification of substrates for several protein-modifying enzymes. For example, protein kinase substrate identification, which constitutes an important aspect of pathway mapping because of the prevalence of these substrates in biological pathways. MacBe
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Given that the FST protocol for mice does not
2024-01-22
Given that the FST protocol for mice does not engage the exposure to a previous stressful session, posits that Agtr1a levels could be kept higher by basal glutamatergic transmission rather than by stressful stimuli as postulated before. To address this possibility, we used the EMBL-EBI Expression At
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br Prostate cancer and resistance to AR
2024-01-22
Prostate cancer and resistance to AR targeting treatment The AR plays a pivotal role in the development, differentiation, homeostasis and secretory function of the normal prostate (Wilson, 2011). The AR is also a key player in many phases of prostate carcinogenesis (Huggins et al., 1941, Scher an
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It has been reported that trehalose shows beneficial
2024-01-22
It has been reported that trehalose shows beneficial effects in a mouse model of several neurodegenerative diseases [21], [22], [23]. There are also reports showing that trehalose can improve the impaired cognitive and learning ability and reduced Aβ deposit in hippocampus of APP/PS1 transgenic mice
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The AHR potentially enhances IDO expression possibly
2024-01-19
The AHR potentially enhances IDO-expression, possibly via crosstalk with several inflammatory signaling pathways (shown by now for IL6 and ‘signal transducer and activator of transcription’ (STAT) 3, and for NFκB, toll like receptor-pathways) [56,59,60]. IDO metabolizes Trp to kynurenines, which are
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Since natural and recombinant glycoprotein hormones exhibit
2024-01-19
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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LO is a soluble kDa enzyme composed of an
2024-01-19
5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracell
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AT9283 The benzimidazole group seems to be a key
2024-01-19
The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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