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In conclusion phenolic hydroxyl was introduced not only to C
2023-04-21

In conclusion, phenolic hydroxyl was introduced not only to C3 side chain but also to C6 or C7 position of the quinoxalinone core, resulting in a new group of ARIs candidates exhibiting antioxidant activity. Biological activity tests suggested that compounds were not only sufficient to inhibit ALR2
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A combination of factors might however account for the low
2023-04-20

A combination of factors might, however, account for the low rate of success of drug development for neuropsychiatric disorders. First, in most neuropsychiatric disorders, the symptomatology is heterogeneous and the neurobiology remains poorly understood, making therapeutic targets difficult to iden
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At first the APC is a kDa protein divided
2023-04-20

At first, the APC is a 310kDa protein divided into three domains such as N-terminal, central core and C-terminal domain [102], plays a major role to regulate the Wnt signaling pathway in human cancer by translating β-catenin from the LDN193189 Hydrochloride to the nucleus [103]. The SIRT1 regulates
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Fencilli et al reported derivatives of PHA which demonstrate
2023-04-20

Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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In clinical studies BA has been reported
2023-04-20

In clinical studies, BA has been reported to promote dose-dependent LDL-C lowering effects of up to 30% as monotherapy, and up to an additional 24% when added in combination with stable statin therapy, or approximately 50% when combined with ezetimibe 109, 110, 111, 112. These effects were accompani
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Findings of the present study provide a molecular mechanism
2023-04-20

Findings of the present study provide a molecular mechanism for the elevated ASK1 expression in obesity and how it may be functionally linked to whole-body insulin resistance. The role our findings assign to increased E2F1 in upregulating ASK1 parallels the capacity of this transcription factor to r
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AT signaling is distinct to
2023-04-20

AT2 signaling is distinct to that of AT1 (Kaschina and Unger, 2003). As shown here, opposite to the stimulating effect of AT1 signaling, it inhibits apelin secretion. Activation of AT2 receptor, which is also G-protein coupled, is known to decrease cAMP and cGMP levels by inhibiting adenylyl cyclase
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Maynard et al demonstrated that serum
2023-04-20

Maynard et al. [54] demonstrated that serum levels of sFlt-1 were five times higher in pregnant women with PE than in normotensive women; as a consequence, VEGF and PlGF levels were found to be proportionally reduced in these women [54]. The literature confirms that there is a sharp increase in sFlt
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Women are usually at risk of sleep deprivation
2023-04-20

Women are usually at risk of sleep deprivation or restriction during pregnancy, especially in the third trimester of gestation, due to the pregnancy-associated anatomic, physiological and hormonal changes (Pien and Schwab, 2004). However, several major TRAM 39 developmental events, such as the neur
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br Conflict of interest br Introduction
2023-04-20

Conflict of interest Introduction The Piezo proteins, Piezo1/FAM38A and Piezo2/FAM38B, are multi-pass transmembrane proteins that have been identified as mechanically-activated (MA) homomultimeric, pore-forming ion channels [1,2]. Piezo1 is broadly expressed with its highest expression in blad
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br In patients with spina bifida and spinal cord injury
2023-04-19

In patients with spina bifida and spinal cord injury, fecal incontinence is a serious issue that can impair activities of daily living and patient self-esteem. To address this Malone et al. first described the Antegrade Continence Enema (ACE) procedure in 1990 [1], which achieves continence by all
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In addition to drawing attention
2023-04-18

In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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br Apelin Discovered in apelin was initially identified as
2023-04-18

Apelin Discovered in 1998, apelin was initially identified as the sole endogenous ligand for the APJ receptor (Tatemoto et al., 1998). Apelin-77 (pre-pro-apelin) is the precursor for various pharmacologically active apelin isoforms (e.g. apelin-12, -13, -17 and 36), and it shares 75–95% sequence
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br Methods and materials br Results br Discussion GPCR regul
2023-04-18

Methods and materials Results Discussion GPCR regulation in response to agonist stimulation is common to nearly all GPCRs and is essential in physiological systems to limit persistent signalling. In this study we have investigated the [Pyr1]apelin-13-induced trafficking and desensitization
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Sorafenib was the first small RTK inhibitor
2023-04-17

Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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