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Besides having a remarkable progestogenic effect an
2020-11-17
Besides having a remarkable progestogenic effect, an additional characteristic of DRSP is its strong antimineralocorticoid effect and antiandrogenic action [11]. DRSP is characterized by an antimineralocorticoid effect that is stronger when compared to progesterone. The decreasing synthesis of proge
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The selective estrogen receptor modulators
2020-11-17
The selective estrogen receptor modulators (SERMs) are another type of estrogen receptor ligands. The main difference between SERMs and xenoestrogens relies on the fact that SERMs present functional duality and are able to act both as agonists and antagonists of the estrogen receptors in different t
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It has previously been shown that
2020-11-17
It has previously been shown that human melanocytes are responsive to a multiplicity of hormonal triggers [10], particularly to pituitary or ovarian hormones [11]. Studies concerning the effects of Cl-Amidine trifluoroacetate salt on human melanocytes led to inconsistent data [12], [13]. Im et al.
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The role of Epac in the
2020-11-17
The role of Epac in the regulation of intracellular Ca homeostasis and contractility is still matter of debate. In rat adult cardiomyocytes, acute Epac stimulation decreased the amplitude of Ca transients [6], [9], [10] with either no changes [6] or increments [9] in cell shortening, suggesting an e
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In mammals neutrophil elastase is a
2020-11-16
In mammals, neutrophil elastase is a trypsin-like serine protease stored in the azurophilic granules of naïve neutrophils [15], [16]. The catalytic activity of neutrophil elastase relies on a His57–Asp102–Ser195 triad (chymotrypsin numbering system) that functions by transfer of electrons from the c
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Cyclosporine NEORAL Oral Solution Novartis is an
2020-11-16
Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na
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Immunomodulation effects of certain oxysterols were previous
2020-11-16
Immunomodulation effects of certain oxysterols were previously shown to depend on activation of oxysterol-binding liver X receptors (LXRs). Recent work from our labs as well as from others has shown additional receptors linking oxysterols and immunity. For example, we found that 7α,25-dihydroxychole
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Generally glycines and other small residues such as alanine
2020-11-16
Generally, glycines (and other small residues such as alanine) present in a helical GxxxG-motif that are facing the same side of the helix form a uniform surface that enables direct contact with a second helix. Crystal structures of multipass membrane proteins have demonstrated that GxxxG-motifs are
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The Inhibitor of APoptosis IAP proteins were first identifie
2020-11-16
The Inhibitor of APoptosis (IAP) proteins were first identified as gene products of baculovirus that inhibited apoptosis of infected insect buy flumazenil synthesis (Clem et al., 1991, Crook et al., 1993). Subsequently, the mammalian IAP family was identified (Rothe et al., 1995, Uren et al., 1996)
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The first hint that GLP might not
2020-11-16
The first hint that GLP-1 might not be completely stable came from a meeting abstract in 1992, reporting that GLP-1 could be degraded in plasma incubations [16], although the enzyme(s) involved was not identified. A year later, Mentlein and colleagues [17], in a search for peptide substrates of the
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Compounds that interact with MDR
2020-11-16
Compounds that interact with MDR1 can do so by different mechanisms. Verapamil is known to modulate drug resistance by acting as a competitive MDR1 substrate [36]. Interestingly, NU7441 has similar growth inhibitory activity in the sensitive and resistant Calyculin A and there was no observed reduc
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Although both DNA DSBs and DNA PK activity
2020-11-16
Although both DNA DSBs and DNA-PK activity increase with aging in skeletal muscle (Figure 1), we cannot conclude that aging-associated increase in DNA-PK activity is solely mediated by chromosomal breaks, as DNA-PK is also activated independently of chromosomal breaks by ROS (Li et al., 2014), which
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Studies on the external dehydrogenases of N crassa
2020-11-16
Studies on the external dehydrogenases of N. crassa have shown that the NDE1 protein is a Ca2+-dependent external NADPH dehydrogenase, while NDE2 is characterized as a dehydrogenase oxidizing both cytosolic substrates (external NADH and/or NADPH) (Carneiro et al., 2004, Melo et al., 2001). All three
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br Results br Discussion The sequence
2020-11-16
Results Discussion The sequence homology-based clustering of the human kinome by Manning et al. (2002) has been extremely useful to organize kinases into Rucaparib free base by sequence relationship. Since kinases are such prominent drug targets, we expect that clustering of the kinases by th
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Despite the significant associations between TNF and TRAIL
2020-11-16
Despite the significant associations between TNF-α and TRAIL in our results, the use of a single top cytokine in predicting sPTB is limited, and the previous study using the specific candidate cytokines failed to accurately predict the risk for sPTB in asymptomatic women, with AUC ranged from 0.48 t
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