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Previous reports indicate that the expression
2024-07-25
Previous reports indicate that the expression of AChRs and their clustering on myotubes are critical factors required to induce contacts on muscle fibers in a natural biological system [14], [15], [16], [17], [18], [19]. For instance, in NMJ development in the mouse, AChRs are pre-patterned at sites
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Both subcutaneous s c and mucosal administration of s
2024-07-25
Both subcutaneous (s.c.) and mucosal administration of short synthetic peptide derivatives of AChR prevent the onset of EAMG, but do not treat ongoing EAMG [80], [81], [82], [83], [84], [85]. The selection of peptides for treatment is mainly based on the identification of immunodominant T- and B-cel
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Based on the observation that antipsychotic drugs increase H
2024-07-25
Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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The exact etiology of BPH is not completely
2024-07-25
The exact etiology of BPH is not completely understood, however this pathology has been associated with elevated AZD6482 levels of the androgen DHT (10). Thus, a valuable strategy in BHP treatment is the reduction of DHT (10) levels, by inhibiting its biosynthetic production [6], [8]. An important
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We used the lead compound C to demonstrate
2024-07-25
We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system. E
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Chromatin proteins play important roles in gene expression
2024-07-25
Chromatin proteins play important roles in gene expression and DNA repair. The importance of chromatin composition on gene expression is exemplified by X-inactivation, where one of the two X chromosomes in female mammalian iCRT 14 is transcriptionally silenced by heterochromatin , , , . In the ATR
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br Nanoparticle Conjugated Topoisomerase Inhibitors The safe
2024-07-25
Nanoparticle-Conjugated Topoisomerase Inhibitors The safety and efficacy of topotecan administered as LDM or MTD have been evaluated in several preclinical studies and a few clinical trials whose results showed that there can be significant adverse effects likely precluding its use in patients [5
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The evidence points toward a
2024-07-24
The evidence points toward a role for 12/15-LO activity in WAT in modulating chronic local inflammation and subsequent systemic metabolic decline in the obese state. However, little is known as to the role of 12- and 15-LOs in BAT. Indeed, in addition to WAT, platelet- and leukocyte-type 12-LO are e
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The subdivision of HT receptors started
2024-07-24
The subdivision of 5-HT receptors started in the 1950s by Gaddum and colleagues, when they realised that in the guinea pig ileum, the effects of 5-HT could be blocked in part by morphine (M), and in part by dibenzyline (D). Gaddum and Picarelli proposed two receptor classes, 5-HT M and 5-HT D (1957)
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In the late s Solvay Pharmaceuticals discontinued the Phase
2024-07-24
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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br Funding br Introduction The interest in the effects
2024-07-24
Funding Introduction The interest in the effects of endocrine disrupting chemicals (EDCs) in the aquatic environment continues to increase over the past decade, specifically those that act on steroidogenic pathways. EDCs that include synthetic androgenic and estrogenic compounds can severely a
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The compounds containing beryllium act as
2024-07-24
The compounds containing beryllium act as strong Lewis acids because of electron deficiency of the Be trovafloxacin synthesis []. Interactions of X-Be-Y compounds with different Lewis bases have been studied by Yanez and co-workers [], extensively. Recently, they proposed a class of extremely stron
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Functional implications notwithstanding the intermolecular c
2024-07-24
Functional implications notwithstanding, the intermolecular contact appears to shield the Y361 side chain (Fig. 3) from being accessible for regulation by phosphorylation/dephosphorylation as has been proposed [18,19]. It is, therefore, likely that Src kinase and PTP1B phosphatase bind to an AROM mo
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br Concluding Remarks and Future Perspectives Fluorescent an
2024-07-23
Concluding Remarks and Future Perspectives Fluorescent Y-27632 receptor have helped researchers to elucidate antibiotic MOA and off-target interactions, to screen for new antibiotics, to detect antibiotics in the environment, to track antibiotic uptake throughout cells and organisms, and to dete
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Since primitive societies plants herbs and seeds rich in phy
2024-07-23
Since primitive societies, plants, herbs and seeds, rich in phytochemicals, were used due to their benefits in human health. These molecules were shown to present a diverse array of action mechanisms, including antioxidant activity, enzyme stimulation, hormones mimicking and by interfering with DNA
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