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Introduction Eicosanoid lipid prostaglandin D
2021-02-23
Introduction Eicosanoid lipid prostaglandin D2 (PGD2) is the major prostaglandin produced by activated mast Sodium Nitroprusside (Lewis and Austen, 1981). The physiological function of PGD2 is mainly mediated by two G protein-coupled receptors (GPCRs), PGD2 receptor 1 and 2 (DP1 and DP2), which sha
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The full length human CPG protein is
2021-02-23
The full-length human CPG2 protein is expressed in CNS tissue with the highest expression in the neocortex, hippocampus and striatum, consistent with mRNA localization patterns of the rat Cpg2 homolog (Cottrell et al., 2004). In the rat, the CPG2 protein localizes primarily to the postsynaptic endoc
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The aim of this study was
2021-02-23
The aim of this study was to use molecular methods to characterise C. difficile isolates circulating in the Czech Republic from 2013 to 2015. Material and methods Discussion During a three-year period (2013–2015) a total of 32 hospitals voluntarily participated in this project, but only 11 ho
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br Conclusions br Introduction Today just
2021-02-23
Conclusions Introduction Today – just as for the past 50 years – the most commonly used repellent in the world is DEET (Fradin, 1998; Pickett et al., 2008). The active ingredient, N,N-Diethyl-m-toluamide, is an oily synthetic substance applied topically to the skin in order to alter the host f
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In summary we demonstrated the high
2021-02-23
In summary, we demonstrated the high potency of fluxametamide against M. domestica, L. striatellus, and T. urticae GABACls, which leads to high acaricidal/insecticidal effects on these arthropod pests. In contrast to its high potencies against the GABACls of arthropod pests, fluxametamide exhibited
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Prenylation may turn a flavonoid from
2021-02-23
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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ERR is constitutively active in the
2021-02-23
ERRγ is constitutively active in the absence of endogenous ligand. However, several synthetic ligands that can repress or induce ERRγ function by disrupting ERRγ-coactivator interactions have been reported to date. The estrogen receptor modulators diethylstilbestrol (DES) and 4-hydroxytamoxifen (4-O
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Prostaglandin E PGE is involved in several biological proces
2021-02-23
Prostaglandin E2 (PGE2) is involved in several biological processes such as renal function, inflammation, angiogenesis, and tumor growth. The various biological effects of PGE2 are mediated by the so-called E-type prostanoid receptors (EP1 to EP4). Among these, the EP4 receptor has been well studie
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Several of the keloid like
2021-02-23
Several of the keloid-like lesions seen in these individuals were pigmented. It is of potential relevance that genetic variants in DDR1 [MIM: 600408] have been associated with vitiligo, and DDR1 activation is involved when MLN 8237 are attached to collagen-IV fibers. Because DDR1 and DDR2 are paral
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The potential off target activity of against
2021-02-23
The potential off-target activity of against other ATP-dependent enzymes, such as kinases, was also investigated. Encouragingly, there was no significant inhibition of ATP binding to 97 human kinases, when was evaluated at 10μM within a DiscoveRx scanEDGE® kinome screen (, ). All together, these d
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br Ubiquitylation of the TGF BMP pathway components Ubiquity
2021-02-23
Ubiquitylation of the TGFβ/BMP pathway components Ubiquitylation is a reversible post-translational modification that is essential in many cellular regulatory mechanisms [20], [21]. During the ubiquitylation cascade, ubiquitin is attached to target proteins through the concerted actions of an E1-
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br Concluding remarks A crucial
2021-02-23
Concluding remarks A crucial step in the microbial degradation of steroids is the 1(2)-dehydrogenation of the steroid nucleus by FAD-dependent Δ1-KSTDs. This step is required to initiate the opening of the steroid nucleus under both aerobic and anaerobic conditions. A large variety of steroid-deg
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Addition of deoxyuridine to CY cultures led to
2021-02-22
Addition of deoxyuridine to CY11 cultures led to a significant decline in the amount of uracil-DNA (Fig. 5). Deoxyuridine effectively induces the deo operon and is efficiently degraded to uracil and deoxyribose 1-phosphate by the deoA gene product, thymidine phosphorylase; a minor percentage of deox
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During the course of our
2021-02-22
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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Coumarins also known as benzopyran
2021-02-22
Coumarins also known as benzopyran-2-ones are a family of nature-occurring lactones first isolated from Tonka beans in 1820. They are an important class of oxygen containing heterocycles widely found in nature, so much so that they have been routinely employed as herbal remedies since early days. O
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