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Based on structure activity relationship of several SARM
2023-08-23

Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo
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Introduction Aldose reductase ALR is the
2023-08-22

Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr
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br Liver specific AHR deficiency and energy balance In contr
2023-08-22

Liver-specific AHR deficiency and energy balance In contrast to the amelioration of hepatic steatosis by global AHR deficiency, targeted knockout of Ahr in hepatocytes exacerbated it in B6 mice fed on a high-fat diet, without interfering with body weight gain [21]. This appeared to result from au
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490 mg br Results br Discussion Members of the PfkB family o
2023-08-22

Results Discussion Members of the PfkB family of proteins, which exhibit AK activity, have only been found in the eukaryotic organisms in the past. Hence, the report of a PfkB family protein in MTub that exhibited AK activity was of much interest, and it necessitated closer examination of its
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hydroxydopamine OHDA is a selective catecholaminergic neurot
2023-08-22

6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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br Autophagy in the central nervous system The autophagic
2023-08-22

Autophagy in the central nervous system The autophagic process appears to be very important for the cells of the central nervous system, as it allows to maintain the functional integrity of the nervous tissue. Indeed macroautophagy is involved in the regulation of homeostasis of the CNS, playing
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THZ2 Inactivation of autophagy can also impact
2023-08-22

Inactivation of autophagy can also impact the surface internalization of MHC I molecules, leading to increased antigen presentation. Inactivation of autophagy factors Atg5 and Atg7 in DCs causes elevation of MHC I surface levels by decreasing endocytosis due to a poor recruitment of adaptor-associat
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ABC super family proteins are found in all forms of
2023-08-22

ABC super family proteins are found in all forms of life and ABC-F subfamily of proteins are involved in cellular processes such as translational control and antibiotic resistance by ribosomal protection [3], [5]. The Mtb ABC proteins that do not contain transmembrane domains have not been studied [
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ras inhibitor The tumor suppressor function of LOX in normal
2023-08-22

The tumor-suppressor function of 15-LOX-2 in normal prostate epithelial cells may be explained by the induction of replicative senescence [14,15]. Thus, 15-LOX-2 is overexpressed in age-dependent prostatic hyperplasia, but cell senescence may hinder progression to malignant transformation. Notwithst
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Arginase deficiency is a rare urea cycle disorder with hyper
2023-08-22

Arginase deficiency is a rare urea cycle disorder with hyperargininemia and profound neurological impairment as hallmark features. Arginase-1-deficient mouse models have been created, and they exhibit a profound lethal phenotype approximately 2 weeks after birth in the global knockout (KO) mice or a
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br Materials and methods br Results In order to eval
2023-08-22

Materials and methods Results In order to evaluate changes in the amount of PKC-θ expressed by MEL cells at different stages of the cell cycle, we measured the level of the kinase in cells collected from cultures containing 90% of cells in the interphase or 80% cells synchronized at the metaph
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HMP Linker mg Dual acting RAAS blockade and neprilysin inhib
2023-08-22

Dual-acting RAAS blockade and neprilysin inhibition has been evaluated in several clinical HF trials. In PARADIGM-HF [6,7], LCZ696 was superior to enalapril in reducing mortality and HF hospitalizations in symptomatic patients with HF with reduced EF. Augmented benefits on maladaptive cardiac remode
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Brefeldin A Immunohistochemistry in tissue samples showed th
2023-08-22

Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of Brefeldin A tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator also resulted in
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Herein we employ an adapted targeted quantitative proteomic
2023-08-21

Herein we employ an adapted targeted quantitative proteomic isotope dilution method, developed in our laboratory [[18], [19], [20], [21]], to quantify membrane transporters in fresh lung from five donors, in four immortalized human lung cell lines and in three control cell lines. We quantify twelve
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The anorexic effect observed when AR is
2023-08-21

The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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