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Thirty six of the analogs synthesized showed ATX inhibition
2024-12-21
Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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KJ Pyr 9 Although TP status has been shown to
2024-12-21
Although TP53 status has been shown to play a role in ATR inhibition and platinum resistance [7], [27], [38], in inhibition of ATM and sensitivity to IR [39], and in the activation of Chk1 and Chk2 [3], [4], ATM and ATR signaling can occur through the p38MAPK/MK2 pathway in p53-deficient KJ Pyr 9 [
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br Material and methods br Results
2024-12-20
Material and methods Results Discussion T2D is a substantial threat to global human health [31]. Obesity-associated chronic low-grade inflammation promotes insulin resistance and T2D [32]. In obese individuals, the production of numerous inflammatory molecules including IL-6 and TNF-a is up
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br Antioxidant polymers conjugates Natural antioxidants are
2024-12-20
Antioxidant-polymers conjugates Natural antioxidants are usually used as a substitute for synthetics but some degradation phenomena could influence their applications. For example, ascorbic Sulfo-NHS-LC-Biotin as a natural antioxidant undergoes yellowish coloration as a result of oxidation [29].
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Our previous study showed that TRIM could
2024-12-20
Our previous study showed that TRIM31 could target TSC1-TSC2 complex and contributed to the clinical cancer progression [6]. In this study, we showed that TRIM31 could directly target p53 for ubiquitous degradation and further mediated anoikis-resistance of HCC cells. To further clarify the role of
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br Introduction The traditional Chinese medicine TCM Ganoder
2024-12-20
Introduction The traditional Chinese medicine (TCM), Ganoderma (G.) lucidum Karst is a well-known mushroom which has been used clinically in some Asian countries. It is termed “Lingzhi” in China, “Reishi” in Japan and “Yeongji” in Korea. It has long been used in TCM for the promotion of longevity
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dabigatran etexilate br Materials and methods br Results
2024-12-20
Materials and methods Results and discussion First, we examined whether hypothalamic Akt-mediated signaling pathways are regulated postprandially in chickens. Refeeding significantly (P dabigatran etexilate concentrations significantly increased in chicks after 1 h of refeeding (958 ± 245% of
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P2Y-purinoceptor agonist Human testicular peritubular cells
2024-12-20
Human testicular peritubular P2Y-purinoceptor agonist (HTPCs) are also the only human testicular cell type that can be isolated, cultured and studied in vitro (Albrecht et al., 2006, Mayerhofer, 2013). Results from recent studies indicate that their roles go beyond sperm transport and include immuno
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AdK as an important upstream regulator
2024-12-20
AdK as an important upstream regulator of adenosine-based homeostasis represents a promising drug target since it leads to an increase in adenosine concentrations. Taking into account that the adenosine formation is only increased in affected tissues under stress with high adenosine levels, AdK inhi
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In this study an in vitro
2024-12-19
In this study, an in vitro AChE inhibition assay combined with UF-HPLC-ESI-Q-TOF/MS method was developed for rapid screening and identification of AChEI from the roots of C. chinensis Franch. Five compounds was found with AChE inhibitory activity and identified by the on-line DAD-ESI-Q-TOF/MS compar
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Taniyama et al reported a
2024-12-19
Taniyama et al. reported a female with infertility who had a homozygous T-to-A transversion at nucleotide position g.2472 in exon 3 of the CYP17A1 gene (mutation Y201N) and decreased 17-hydroxylase and 17,20-lyase activities of IVF Phos-tag was initiated using dexamethasone to control adrenal P pro
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The mechanism by which Gas prevents inflammation has been
2024-12-19
The mechanism by which Gas6 prevents inflammation has been reported to be via inhibition of Toll-Like receptors (TLRs) signaling (Cui et al., 2016). After injury, TLRs become stimulated, leading to downstream activation of TRAF3 and TRAF6 and translocation of several transcription factors, such as I
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Imatinib is a well known anticancer drug used in
2024-12-19
Imatinib is a well-known anticancer drug used in Chronic Myeloid Leukemia (CML) against the altered expression/activity of tyrosine kinase resulting from the fusion of BCR-ABL in leukemic blasts. It has been demonstrated that Imatinib can induce autophagy in BCR-ABL expressing Cell cycle arrest Stau
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RK-33 Activated MAP kinases transform the stimulus into the
2024-12-19
Activated MAP kinases transform the stimulus into the pathophysiological responses by phosphorylating downstream substrates, including transcription factors, cytoskeletal proteins involved in mRNA translation (Li et al., 2015). Among the numerous effectors that intervene in the TNF-α action is an ac
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This progressive behaviour is summarized in Fig which depict
2024-12-19
This progressive behaviour is summarized in Fig. 4, which depicts the variation in convexity of the obtained cut-off patterns for the series of six antioxidants. The form and degree of convexity of the obtained cut-off curves should in principle correlate with the AOs hydrophobicities, and therefor
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