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In this review we will present the traditional and actual
2024-07-01
In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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Here the so called alkali assay is proposed
2024-07-01
Here the so-called alkali assay [18] is proposed as a method to be applied directly on the purified recombinant enzyme sharing the same structural and functional features of the wild-type enzyme [19], [20], [21] using its physiological substrate androstenedione. The assay that was already successful
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br Materials and methods br Results br
2024-07-01
Materials and methods Results Discussion Pulmonary fibrosis is a progressive and chronic lung disease and its typical features include NS 11394 receptor proliferation, epithelial injury, chronic interstitial inflammation, increased extracellular matrix (ECM) production, and collapse of alv
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br Materials and methods br Results A first series
2024-07-01
Materials and methods Results A first series of experiments explored whether the Ampkα1 isoform is involved in the regulation of cardiac Pkcζ. To this end, HL-1 cardiomyocytes were transfected with a construct encoding constitutively active Prkaa1T183D (CAα1) or with the empty vector as contro
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The initial demonstration of the potential
2024-06-28
The initial demonstration of the potential of MALDI-TOF MS for testing antifungal susceptibility of pathogenic fungi came from a proof-of-concept study by Marinach et al. [31] who monitored the changes of the proteome of C. albicans Resiquimod australia exposed to different concentrations of flucon
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Tetracyclines constitute one of the most important antibioti
2024-06-28
Tetracyclines constitute one of the most important antibiotic groups used as veterinary and human medicine and as feed additives in the agricultural sector (Li et al., 2011a, Simon, 2005). Annual worldwide production of tetracyclines is estimated to be in the thousands of tons (Michalova et al., 200
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Clozapine br HIF Blockade in AA Therapy
2024-06-28
HIF-α Blockade in AA Therapy In lieu of the evidence supporting a central role for HIF-α signaling in tumor angiogenesis and CC pathobiology, significant efforts have focused on the discovery of small-molecule HIF-α inhibitors (for exhaustive compendia, see [28,44,45]). In brief, inhibitors vary
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Sorafenib was the first small RTK inhibitor drug to
2024-06-28
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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br AR mediated actions in cells of the vascular wall
2024-06-28
AR-mediated actions in Apatinib of the vascular wall Sex hormones may influence the size and composition of atherosclerotic lesions indirectly by modifying systemic cardiovascular risk factors such as plasma lipids profiles and insulin sensitivity; this aspect of their action is discussed elsewh
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The SMN and SMN promoters are regulated
2024-06-28
The SMN1 and SMN2 promoters are regulated by transcription factors such as E26 transformation-specific domain containing protein (ELK-1) and cAMP response element-binding protein (CREB) 58, 59. Compared with WT animals, mice with SMA exhibit increased and decreased ELK-1 and CREB phosphorylation, re
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br Introduction AMPA receptors AMPARs mediate
2024-06-28
Introduction AMPA receptors (AMPARs) mediate the majority of fast excitatory postsynaptic currents (EPSCs) in the Andarine sale (Jonas, 2000). The brevity of EPSCs and rapid deactivation of AMPARs depend upon a short lifetime of synaptically released glutamate, estimated to be about 1 ms (Clemen
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We also measured macrophage infiltration and
2024-06-28
We also measured macrophage infiltration and CLS presence in peri-gonadal AT from db/db mice and controls. CLS are morphological features within AT that are accurate indicators of adipocyte death and macrophage infiltration [56]. An earlier study showed that CLS macrophages account for >90% of the t
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The dependence of blood cell production on a limited
2024-06-28
The dependence of blood cell production on a limited number of HSC and HPC (hereafter collectively referred to as HSPC) means that protection from potential toxins is essential for maintenance of the hematologic system (see Fig. 1). For example, the generation of blood cells within the intramedullar
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br Discussion With recently improved understanding of the
2024-06-28
Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1) e
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Adiponectin also suppresses inflammatory stimuli induced NF
2024-06-28
Adiponectin also suppresses inflammatory stimuli-induced NF-kappaB activation, which may significantly contribute to the anti-diabetic and anti-atherogenic effects of adiponectin (Ouchi et al., 2000). The downstream mediators of AdipoR1 and AdipoR2, RPPAR and AMPK increase inflammatory responses by
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