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The extent to which GPCR oligomerization is a regulated proc
2025-03-03

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
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Dimensions of EGFP fluorescence protein Ryoichi et al modifi
2025-03-03

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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The LO has so far only
2025-03-01

The 15-LO-1 has so far only been found in humans and rabbit reticulocytes [3], [20] and the rabbit 15-LO-1 protein demonstrate 81% identity to the human 15-LO-1. However, rabbit monocytes express an enzyme with mainly 12-LO activity [20], [21]. The high degree of sequence conservation between these
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ASK has been identified as an
2025-03-01

ASK2 has been identified as an ASK1 binding protein (Wang et al., 1998). ASK1 supports the stability and active configuration of ASK2 in the heteromeric complex, while ASK2 has been found to activate ASK1 by direct phosphorylation (Takeda et al., 2007). Unlike ASK1, which is ubiquitously expressed i
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br Leptin Adiponectin a permissive
2025-03-01

Leptin/Adiponectin: a permissive imbalance Leptin, a satiety hormone, is encoded by the obesity (ob) gene. It essentially functions as an energy sensor which is involved in the regulation of body weight by sending signals to the isx to reduce appetite (Woods and D'Alessio, 2008). Obesity results
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Atherosclerosis is a chronic lipid metabolism disorder linke
2025-03-01

Atherosclerosis is a chronic lipid metabolism disorder linked with lipid accumulation within the arterial wall and subsequent formation of foam cells and vascular disease [96], [97]. The level of apelin is decreased in human atherosclerotic coronary arteries [4], and coronary collateral formation in
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In our study S aureus activated the
2025-03-01

In our study, S. aureus activated the TLR signaling pathways of BMECs, thus inducing profibrogenic growth factor expression via NF-κB and AP-1. Since fibrosis is an important pathogenic process in both bovine and human mastitis, further studies on the molecular mechanisms of S. aureus infection are
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br Materials and methods br
2025-03-01

Materials and methods Results Discussion Diabetic kidney disease (DKD) is the most common cause of end-stage renal disease [15], [16]. The pathogenesis of DKD is not fully understood, and there is no effective treatment. Although previous studies suggested that early lesions of DKD are foun
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br Natriuretic peptides and neprilysin Left ventricular syst
2025-03-01

Natriuretic peptides and neprilysin Left ventricular systolic function, most commonly due to myocardial damage as a consequence of coronary artery disease, hypertension or both, and leading to sustained, pathological activation of the renin angiotensin SCH-900776 system (RAAS) and sympathetic ner
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Immunohistochemistry in tissue samples showed the
2025-03-01

Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of ibuprofen solubility tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator also re
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abiraterone acetate To guide our attempts at achieving AKT p
2025-03-01

To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AK
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Eltrombopag br Endocytosis of AdipoR Surface receptor
2025-03-01

Endocytosis of AdipoR1 Surface receptor activity may be shut down by endocytic uptake and subsequent lysosomal degradation of the proteins [20]. Clathrin-dependent endocytosis (CDE) has been extensively studied and internalization from the plasma membrane is mediated through clathrin-coated pits
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The present work has implications for
2025-03-01

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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Adenosine is a ubiquitous homeostatic purine nucleoside that
2025-03-01

Adenosine is a ubiquitous homeostatic purine nucleoside that accumulates extracellularly in response to metabolic stresses such as hypoxia and inflammation. Activation of either G protein-coupled adenosine receptors (ARs; A1R, A2AR, A2BR, and A3R) by extracellular adenosine can modulate cell signali
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In conclusion we have demonstrated
2025-03-01

In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi