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Although effects of low concentrations of
2024-09-12
Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major chk1 α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-esterase-inhibiting dru
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Molecular docking simulations were carried out
2024-09-12
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic ER
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rs G allele was previously associated with
2024-09-12
rs523349 G allele was previously associated with a decrease in the conversion rate of testosterone to DHT (Beesley et al., 2007). This SRDA52 variant may have a trend towards higher testosterone availability, which according to the US Food and Drug Administration is described as a teratogen of categ
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br Studies in zebrafish vascular
2024-09-12
Studies in zebrafish: vascular and neural development and the regulation of left–right asymmetry Zebrafish embryos represent an excellent model system to examine vertebrate vascular development. Major advantages of the zebrafish system include its genetic tractability, small size, external fertil
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Although several different membrane estrogen receptors have
2024-09-12
Although several different membrane estrogen receptors have been reported (Qiu et al., 2008; Revankar et al., 2005), a large percentage of membrane-initiated steroid hormone signaling appears to be performed by a subpopulation of the same receptors that act in the nucleus. Specifically, estrogen rec
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Thymoquinone TQ is the major active compound derived
2024-09-12
Thymoquinone (TQ) is the major active N6-Methyl-dATP derived from Nigella sativa (Woo et al., 2012). Recent animal studies support the potential of TQ for the treatment of a variety of inflammatory disorders like inflammatory bowel disease (IBD), RA, and osteoarthritis (OA) (Salem, 2005, Badr et al
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5-fluorocytosine br Aromatase inhibitors The aromatase enzym
2024-09-12
Aromatase inhibitors The aromatase enzyme, P450arom, belongs to the super-family of P450 proteins which includes more than 480 members divided in 74 different families. P450arom is a unique member of family 19 [39], and is located in the endoplasmic reticulum of mammalian 5-fluorocytosine that e
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From a clinical utility standpoint
2024-09-11
From a clinical utility standpoint, this study showed that AR can be useful in the GATA3-positive tumor of unknown origin setting. Epidemiologically, in this setting, the top 2 diagnoses in the differential diagnosis are metastatic carcinoma of breast origin or urothelial origin [18]. Seven out of 1
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br MHCI peptide editing N terminal
2024-09-11
MHCI peptide editing, N-terminal extensions and the peptide loading complex Conventionally, peptide-MHCI binding is thought to require both amino- and carboxyl-termini for stable interaction (Madden, 1995; Bouvier and Wiley, 1994). Peptides with longer than optimal length (10–13 residues) have be
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AhR was proven to participate in carcinogenesis Its
2024-09-11
AhR was proven to participate in carcinogenesis. Its high expression was demonstrated in a variety of tumors, i.e. pancreatic, prostate, urinary tract, lung and papillary thyroid carcinoma (Safe et al., 2013, Mian et al., 2014). However, cell line studies showed variable AhR levels/responses. AhR kn
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Unexpectedly under pathological pain conditions inhibition o
2024-09-11
Unexpectedly, under pathological pain conditions, inhibition of spinal glutamate transporter activity can produce antinociceptive effects. For example, intrathecal injection of the transportable inhibitor trans-pyrrolidine-2,4-dicarboxylic Betaine synthesis (t-PDC) or antisense oligonucleotides red
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Adenosine receptors are proposed to play proangiogenic role
2024-09-11
Adenosine receptors are proposed to play proangiogenic role in vascular and immune 3-Bromopyruvic acid within microenvironment of hypoxic tissues to maintain tissue oxygenation in chronic ischemic condition [9]. Adenosine also stimulates the production of angiopoetin-1, VEGF and Interleukin-6 (IL6)
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Previous studies have demonstrated the presence
2024-09-11
Previous studies have demonstrated the presence of soluble NTPDases, 5′-nucleotidase and adenosine deaminase in rat blood serum as well as in human blood (Doleski et al., 2016; Oses et al., 2004; Yegutkin, 1997; Yegutkin et al., 2007). In addition, our earlier reports have shown that these membrane-
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Chlorprothixene Introduction Microdialysis is an in vivo tec
2024-09-11
Introduction Microdialysis is an in vivo-technique which allows continuous sampling of small molecular weight substances (such as neurotransmitters, metabolites and neuropeptides) from the extracellular space of different tissues or organs, e.g. brain, muscle or skin. While the implantation of the
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br Experimental procedure br Funding
2024-09-10
Experimental procedure Funding The present study was supported by the Grant Russian Foundation for basic research (project no. 16-04-01517). Introduction 5-HT, a monoaminergic neurotransmitter, is synthesised from l-tryptophan catalysed by the enzymes tryptophan hydroxylase (Tph) and aroma
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