• br ABCA is a sterol

  2023-12-13

  

  ABCA2 is a sterol-responsive gene The first evidence to demonstrate that ABCA2 expression responded to sterol loading was provided in an experiment involving monocyte to macrophage differentiation in vitro. Upon sterol loading with enzymatically degraded LDL (eLDL), ABCA2 expression increased onl

• Bexarotene The importance of insulin in controlling

  2023-12-13

  

  The importance of insulin in controlling lipolysis and fat mass is further emphasized by mouse models with alterations in the insulin signaling pathway of adipocytes. For example, mice with a tamoxifen-inducible knockout of the insulin receptor in mature adipocytes reveal a substantial decrease of a

• Fig A shows a schematic representation of

  2023-12-13

  

  Fig. 2A shows a schematic representation of histological results according to the Franklin and Paxinos Mouse Brain Atlas (2001). The black circles represent the sites of drug infusion that were on-target within the amygdala. Gray circles represent the animals that had infusion locations outside the

• Previous studies have demonstrated the presence

  2023-12-13

  

  Previous studies have demonstrated the presence of soluble NTPDases, 5′-nucleotidase and adenosine deaminase in rat blood serum as well as in human blood (Doleski et al., 2016; Oses et al., 2004; Yegutkin, 1997; Yegutkin et al., 2007). In addition, our earlier reports have shown that these membrane-

• MTT The extent to which GPCR

  2023-12-12

  

  The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or

• Over the past decade extensive research has

  2023-12-12

  

  Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F

• MLN another selective Aurora A

  2023-12-12

  

  MLN8237, another selective Aurora-A inhibitor is said to be more potent than MLN8054 and to cause less benzodiazepine-like side effects based on structure modulation by the addition of a methoxy group to either end of the MLN8054 molecule. It was studied [62] in a once daily (QD) schedule for 7 days

• The acidification of endocytic compartments

  2023-12-12

  

  The acidification of endocytic compartments is closely related to endocytic activity, although the mechanism linking acidification and membrane dynamics is largely unknown. In a recent RNA interference (RNAi)-based screen, V-ATPase depletion blocked the formation of clathrin-coated vesicles, an effe

• The LOX hydroxide metabolites are converted to secondary lip

  2023-12-12

  

  The 15-LOX hydroxide metabolites are converted to secondary lipid mediators such as lipoxin A4 from 15-HETE and protectin D1/resolvin D1 from 17-HDoHE [45] (Fig. S3). Importantly, all of these secondary lipid mediators have anti-inflammatory and pro-resolving properties [46], [47], [48]. Lipoxin A4

• From an historical perspective ligands for GPCRs adrenaline

  2023-12-12

  

  From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Bay 11-7085 or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands wer

• Our research is the first to report that administration of

  2023-12-12

  

  Our research is the first to report that administration of HMW-HA is an effective strategy to defend against PM2.5-induced disruption of pulmonary epithelial barrier and lung injury, and addresses that HMW-HA restricts PM2.5-induced epithelial apoptosis through reducing oxidative stress and followin

• Several alterations have been or can be associated to the

  2023-12-12

  

  Several alterations have been or can be associated to the decreased tolerance of steatotic liver to I/R injury. Previous studies demonstrated that upregulation of the mitochondrial uncoupling protein-2 (UP2) is strictly related to the increase of I/R injury in steatotic liver [4]. UPR induction is c

• Hypoxia of the adipose tissue is a key step in

  2023-12-12

  

  Hypoxia of the adipose tissue is a key step in the inflammatory response linked to obesity and contributes to accelerated tumor progression in the obese population (Rosenow et al., 2013). Intermittent hypoxia exposure induces a 2.2-fold increase in the infiltration of tumor-associated macrophages an

• Esomeprazole Sodium Many naphthoquinone derivatives have bee

  2023-12-12

  

  Many naphthoquinone derivatives have been previously obtained from fungi in the genus Fusarium isolated from various sources, F. oxysporum from the root of citrus (Nagia and El-Mohamedy, 2007), Fusarium sp. (No. b77) from the mangrove plant (Shao et al., 2010), F. solani and F. oxysporum from fibrou

• Based on structure activity relationship of several

  2023-12-12

  

  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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