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The first rationally designed dual mPGES
2023-01-02

The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic Pridinol Methanesulfonate receptor - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted deriv
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Because of its role in tumor growth proliferation and metast
2023-01-02

Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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br Introduction Lung cancer is the leading cause
2023-01-02

Introduction Lung cancer is the leading cause of cancer death worldwide and is one of the most refractory of solid tumors along with pancreatic cancer. Since 1975 there have been notable improvements in the 5-year survival rate of patients with lung cancer [1]. This improvement in survival is tho
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br Introduction Heart failure HF is a chronically progressiv
2022-12-23

Introduction Heart failure (HF) is a chronically progressive disease and one of the most important causes of morbidity and mortality worldwide despite recent improvements in its treatment [1], [2], [3]. The mortality and morbidity benefits of angiotensin converting enzyme inhibitor (ACEI) are wel
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The association of male gender
2022-12-23

The association of male gender with increased atherosclerosis has stimulated interest in the role of androgen signalling in this condition. Androgens act (Fig. 2) by direct activation of androgen receptor (AR), a nuclear receptor that acts as a ligand-regulated transcription factor (Gao et al., 2005
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Notably AR and AR signaling
2022-12-21

Notably, β2AR and β3AR signaling can also occur via mechanisms independent from G protein [13]. Additionally, the response to GPCR stimulus can be modified by various parameters, including chronic stimulation, cell hypoxia, acidosis, and aging [14], [15], [16]. GRKs have a significant role in the r
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Human testicular peritubular cells HTPCs are
2022-12-21

Human testicular peritubular fasudil receptor (HTPCs) are also the only human testicular cell type that can be isolated, cultured and studied in vitro (Albrecht et al., 2006, Mayerhofer, 2013). Results from recent studies indicate that their roles go beyond sperm transport and include immunological
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It is important to note that stable amnesia
2022-12-21

It is important to note that stable amnesia is, apparently, a general biological phenomenon and can be found in different animal species. In studies on rats, it was found that if reconsolidation of conditioned olfactory aversion memory was impaired by the antagonist of NMDA glutamate receptors, amne
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Actin is capable of polymerizing
2022-12-21

Actin is capable of polymerizing spontaneously. However, this process is relatively slow and kinetically unfavorable in cells. Formation of NHS-SS-Biotin australia dimers and trimers, which can easily disassemble due to their instability, is a rate-determining step in actin polymerization [5], [6].
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Oxaliplatin Our published data showed that in mouse heart th
2022-12-21

Our published data showed that, in mouse heart, the protein level of WDR1 was highest during the embryonic stage, but became progressively decreased to a constant level from birth to adulthood (Yuan et al., 2014), indicating an important role of WDR1 in embryonic heart development. However, function
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Using constant potential amperometry and electrochemical enz
2022-12-21

Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of Temsirolimus release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were measured simultaneous
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BGB324 receptor In the U S surveillance
2022-12-21

In the U.S., surveillance of ACEs has garnered traction at the state level through administration of the ACE Optional Module in CDC’s Behavioral Risk Factor Surveillance System (BRFSS) (Centers for Disease Control & Prevention, 2003). Since 2009, select states have implemented the ACEs optional modu
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IGF signaling has been shown to
2022-12-17

IGF-1 signaling has been shown to induce Phorbol 12,13-dibutyrate changes via interacting with MKK-p38 signaling (Serra et al., 2007) and by perturbing Foxo3a signaling (Stitt et al., 2004), among other mechanisms. The current study demonstrates that the acetyl group itself may be limiting, since I
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We wanted to investigate the influence
2022-12-17

We wanted to investigate the influence of substituents on the pyrazole ring on the activity, but only a few substituted pyrazole-3-carboxylic acids/esters were commercially available in useful amounts at a reasonable price, for example, 4- and 5-nitro-pyrazole-3-carboxylic acid. The preparation of 4
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Earlier studies with SERMs identified that distinct chemical
2022-12-16

Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes
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