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Several dehidropregnenolone derivatives functionalized at C
2023-12-12
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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br Phosphorylation of P c Initial studies In addition to
2023-12-12
Phosphorylation of P450c17 – Initial studies In addition to the molar ratio of POR to P450c17 and the allosteric action of cytochrome b5, a third factor that governs 17,20 lyase activity is the serine/threonine (Ser/Thr) phosphorylation of P450c17 itself. In a search for post-translational factor
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The resolution cocrystal structure of ACL in
2023-12-12
The 2.10Å resolution cocrystal structure of ACL in complex with citrate indicates that the carboxyl (COH) groups of citrate forms a network of H-bonds with hydrophilic residues surrounding the ACL citrate binding domain (CBD) (A). The - carboxyl group forms a salt bridge with the guanidine moiety of
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br Disclaimer Statement br Acknowledgments br Introduction
2023-12-12
Disclaimer Statement Acknowledgments Introduction Metabolic changes are a common feature of cancerous tissues. Mutations in oncogenes and tumor suppressor genes cause alterations to multiple intracellular signaling pathways that rewire tumor cell metabolism and re-engineer it to allow enhan
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br Antibiotic drug discovery approaches Traditionally novel
2023-12-12
Antibiotic drug discovery approaches Traditionally, novel Carbenicillin, Disodium Salt were largely discovered by phenotypic screening approaches of various sources of compounds, such as natural products isolated from extracts of soil microbes and semi-synthetic or fully synthetic compound libra
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br The role of LOX plays in
2023-12-12
The role of 12/15-LOX plays in autophagy Autophagy is a process by which cellular material is delivered to lysosomal to degrade the damaged organelles and proteins to facilitate nutrient recycling (Towers and Thorburn, 2016). There has been characterized three types of autophagy-macroautophagy, m
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Decrease in soluble protein content in diabetic lenses compa
2023-12-12
Decrease in soluble protein content in diabetic lenses compared with those in control lenses in present study could be due to leakage of proteins and insolubilization. T. purpurea treatment could increase the levels of soluble proteins in diabetic lenses may be by preventing cross-linking/aggregatio
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Studies on both TCDD treated mice and AhR null mice
2023-12-12
Studies on both TCDD treated mice and AhR null mice have also pointed to a role of AhR in hematopoiesis [65], [66]. Singh et al. showed that AhR is a negative regulator of HSC (hematopoietic stem cell) proliferation, while deletion of AhR leads to spleen enlargement in juvenile and adult mice [67].
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Heart failure is a chronic syndrome
2023-12-12
Heart failure is a chronic syndrome in which the heart is unable of pumping an adequate supply of blood to meet the metabolic requirements of the body or generating the required elevated ventricular filling pressures to maintain output [34]. Despite considerable advances in the treatment of heart fa
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Extracellular ATP and downstream purinergic signaling have
2023-12-12
Extracellular ATP and downstream purinergic signaling have also been proposed to contribute to dental pulp tissue healing and dentin regeneration. Mechanical and thermal stimulation of external dentin can induce ATP release in dental pulp through pannexins [13]. Cold stimulation was also reported to
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CEP-32496 Tacrine an aminoacridine derivative Fig A
2023-12-11
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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The present work has implications
2023-12-11
The present work has implications for our thinking about the effects of antidepressant (e.g. SSRIs) use on maternal care in depressed mothers which consist of approximately 10–20% of all mothers (Gjerdingen and Yawn, 2007, Susser et al., 2016), and more than 40% of depressed mothers are prescribed w
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In this paper we describe the
2023-12-11
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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We found a protective effect of the GTCC haplotype against
2023-12-11
We found a protective effect of the GTCC haplotype against ED, which is reflected by its association with increased IIEF in patients with clinical ED. Further studies are required to determine the functional implications of these genetic markers combined in specific haplotypes blocks. Indeed, we fou
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Different antioxidants were described as useful biomarkers i
2023-12-11
Different antioxidants were described as useful biomarkers in monitoring response to treatment in human and veterinary medicine [33,65,66]. In the same line, Thiol and TAC also proved to be useful biomarkers in monitoring the post-ovariohysterectomy period in queens with pyometra, since antioxidants
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