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Among prostaglandins PG PGD remained
2021-02-25
Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso
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ACAT may act as a dimer of dimer Within each
2021-02-25
ACAT1 may act as a dimer of dimer [38]. Within each dimer, it may contain two identical sterol substrate sites (designated as site S), and one or two sterol activator site(s) (designated as site A). Site S preferentially binds pregnenolone (PREG); it can also bind a variety of sterols that contain 3
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In the current study cocaine did
2021-02-25
In the current study, cocaine did not significantly increase negative subjective effects and nepicastat did not increase these responses. This outcome is somewhat surprising given that the most commonly reported effect to date has been to increase the aversive properties of cocaine such as anxiety,
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Although the implication of DA and glutamate signaling
2021-02-25
Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
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br Application of the screening system for ITP
2021-02-24
Application of the screening system for ITP-binding proteins Inosine is a nucleoside with hypoxanthine as a base. Inosine nucleotides are relatively abundant in human Lomustine because inosine monophosphate (IMP) is a general precursor molecule for the de novo synthesis of AMP and GMP or a produc
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Mycophenolic acid Patients with a tumor of cm or greater
2021-02-24
Patients with a tumor of 4 cm or greater were more likely to have lymph node or tumor metastasis (Fisher’s test p = 0.0001 and 0.0003, respectively). In this smaller patient group a significant correlation between higher DAPK-1 mRNA Mycophenolic acid in tumor and normal tissue in tumor-free patient
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832 582 4016 Recent studies investigating the effects of
2021-02-24
Recent studies investigating the effects of mesenchymal stem cell (MSC) therapy in rodent models including chronic renal failure and glomerulonephritis have demonstrated that MSC therapy can result in beneficial effects [57], [58]. In cats, autologous intra-renal injections of either adipose tissue-
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Adding MPA or NETA we found no impact
2021-02-24
Adding MPA or NETA we found no impact on the estradiol-induced downregulation of serum-stimulated endothelin synthesis in vitro [40]. Progesterone was also able to inhibit the angiotensin II-induced increase in endothelin production [41]. Several clinical studies on the effect of oral or transdermal
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Prenylation may turn a flavonoid
2021-02-24
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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sglt-2 In the literature we can find two different
2021-02-24
In the literature, we can find two different modes of action for estrogens: Firstly there is the commonly accepted genomic pathway. Estrogens pass the cell membrane due to their lipophilic character via diffusion and bind to estrogen receptors (ERs) in the cytoplasm. After binding a dimerization of
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An important role for the precursor molecule of the
2021-02-24
An important role for the precursor molecule of the main EBI2 ligand, 25-OHC, in the inhibition of inflammation was recently shown. 25-OHC was demonstrated to inhibit inflammasome induction in mouse macrophages [28]. Inflammasome assemblies are the sites of caspase 1 activation and lead to the gener
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br Multi subunit RINGs There are RING
2021-02-24
Multi-subunit RINGs There are RING-type E3s that exist as multi-subunit assemblies (see Fig. 3B). A striking example is the Cullin RING Ligase (CRL) superfamily [35], which exhibits enormous plasticity in substrate specificity. Each CRL subfamily is characterized by a cullin protein (Cul-1, 2, 3,
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br Conclusion In the last year significant advances
2021-02-24
Conclusion In the last year, significant advances in our understanding of ubiquitin transfer by IAPs and related E3 ligases have been made. The three crystal structures of the RING-bound E2~Ub show that the conjugate is bound by the RING domain in the closed conformation, where the I44-centered f
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The differences between ground and transition state properti
2021-02-24
The differences between ground and transition state properties are exemplified by a comparison of our human–yeast results with those of a structural study of possible differences in ubiquitin-Uba-1 binding in yeast (known structure) with human (simulated in [12]). Their discussion focuses on Ubiquit
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br Discussion Several DPP inhibitors are currently
2021-02-24
Discussion Several DPP-4 inhibitors are currently available for use in the treatment of type 2 diabetes mellitus. Due to the different chemical structures there are marked differences both in the binding kinetics on the target enzyme [10] and also different pathways of elimination [13] exist. In
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