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The inflammatory cytokine IL is an
2023-10-11
The inflammatory cytokine IL-6 is an additional factor that has been hypothesized to contribute to epinephrine-mediated repression of drug detoxifying proteins such as CYP3A4 (Aninat et al., 2008). Indeed, this CYP is well-known to be repressed by IL-6 (Dickmann et al., 2011) and epinephrine has pre
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APPL is highly expressed in pancreatic cells
2023-10-11
APPL1 is highly expressed in pancreatic β cells, but its levels are significantly decreased in several mouse models of obesity and diabetes, including HFD-induced obese mice and db/db mice [6], [73], suggesting that the dysregulation of APPL1 may be associated with malfunction of the pancreas in obe
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Taken together BRP represents a novel chemotype of LT
2023-10-10
Taken together, BRP-187 represents a novel chemotype of LT biosynthesis inhibitors with outstanding potency in human PMNL and monocytes activated under pathophysiological relevant conditions and with effectiveness in vivo. Using the PLA that visualizes the in situ interaction between 5-LO and FLAP i
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Many ruthenium complexes were tested as
2023-10-10
Many ruthenium complexes were tested as potential anticancer agents and two complexes, namely NAMI-A (trans-[imH] [RuCl4(dmso-S)(im)]; im, imidazole) and KP1019 (trans-[indH][RuCl4(ind)2]; ind, indazole) have successfully entered clinical trials [27], [28]. NAMI-A is selectively active against meta
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The interaction of ATR ATRIP with
2023-10-10
The interaction of ATR-ATRIP with RPA-coated ssDNA is sufficient for ATR-ATRIP recruitment to DNA lesions, but it is not sufficient to fully activate ATR. In response to DNA damage, the heterotrimeric ring-shaped complex 9-1-1 (RAD9-RAD1-HUS1 in humans; Ddc1-Rad17-Mec3 in S. cerevisiae) is loaded at
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Because R gene is positively
2023-10-10
Because 5α-R2 gene is positively regulated by T and in the prostate gland (Torres et al., 2003), and our BPA-treated rats showed decreased circulating T and probably intraprostatic androgen levels, it might be responsible for the decrease of 5α-R2 expression. However, in a previous work using castra
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Two major categories of arginase inhibitors
2023-10-10
Two major categories of arginase inhibitors have been distinguished (Fig. 3): the first category comprises synthetic arginase inhibitors, which have been developed from the substrate l-arginine [35]; and the second category includes inhibitors derived from natural products [36]. The category of synt
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br Implications for cancer ROS have a long
2023-10-10
Implications for cancer ROS have a long history of being involved in the development and progression of cancer and increased ROS level is considered as a hallmark of many tumors [76], [77]. Initially, it was thought that ROS would serve as chemical mutagens that would indiscriminately damage cell
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Introduction It has long been recognized that
2023-10-10
Introduction It has long been recognized that angiogenesis is critical to the growth, progression, and metastasis of many solid tumor types [1], and thus, drugs targeting the angiogenic pathway have been a topic of clinical investigation in the oncology community for many years. Angiogenesis is reg
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corticosterone mg In addition AMPK reduces protein synthesis
2023-10-10
In addition, AMPK reduces protein synthesis and stimulates apoptotic and autophagic pathways through the inhibition of the mechanistic target of rapamycin (mTOR), which regulates cellular metabolic homeostasis, insulin secretion, insulin resistance, autophagy and apoptosis (Maiese, 2016). mTOR is th
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br MHCI peptide editing N
2023-10-10
MHCI peptide editing, N-terminal extensions and the peptide loading complex Conventionally, peptide-MHCI binding is thought to require both amino- and carboxyl-termini for stable interaction (Madden, 1995; Bouvier and Wiley, 1994). Peptides with longer than optimal length (10–13 residues) have be
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The ORR obtained with crizotinib
2023-10-10
The ORR obtained with crizotinib on our cohort was low compared to other studies, such as the prospective studies of A. Shaw et al. (ORR = 65% in second line), B. Solomon et al. (ORR = 74% in first line) and the more comparable large retrospective study of M. Duruisseaux et al. on the French CLINALK
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A straightforward synthetic pathway was
2023-10-10
A straightforward synthetic pathway was adopted to synthesize the target compounds as outlined in . The starting chloromethylquinazolinones (–) were synthesized from anthranilic Balaglitazone in two steps following reported procedures., , , The first step involves chloroacetylation of anthranilic
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AdipoRon acts on the anti diabetic effects
2023-10-10
AdipoRon acts on the anti-diabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively [23]. AdipoR activation is a promising treatment for diabetes, nonalcoholic fatty liver disease, and cardiovascular disease, demons
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As noted earlier the PfkB family
2023-10-09
As noted earlier, the PfkB family of carbohydrate kinases can phosphorylate the hydroxymethyl group of a wide variety of sugar moieties [1], [3]. Recent searches of the Swiss-Prot database with the two conserved sequence motifs found in these proteins (Accession nos. PS00583 and PS00584) identified
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