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However at variance with the well studied
2021-09-02
However, at variance with the well-studied R form of FBP1 which is flat, the R state of FBP2 is diametrically different, with a perpendicular orientation of the upper and lower dimers (Barciszewski et al., 2016). The cruciform-like R state of FBP2 is stabilized by a unique hydrophobic motif called ‘
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The inhibitory activities of the
2021-09-02
The inhibitory activities of the compounds with the modification of the amino group against human liver FBPase are summarized in . Replacement of the amino group of with hydrophobic substituent such as a methyl group () led to a substantial loss of activity (IC=995nM). Similarly, replacement with ha
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br Acknowledgements The authors have no ethical
2021-09-02
Acknowledgements The authors have no ethical conflicts to disclose. The authors have no conflicts of interest to declare. This work was funded by the Research Council of Lithuania. Introduction This paper studies whether there is a causal influence of the risk-taking incentives provided by op
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br Introduction Thrombosis is one of
2021-09-02
Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable MRT68921 sale and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts about 1 million (
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br Introduction Addiction to opioids
2021-09-02
Introduction Addiction to opioids such as morphine is a chronic disorder that affects the mesocorticolimbic dopaminergic pathway in the brain. Activation of the pathway ultimately leads to dopamine release in the nucleus accumbens (NAc) (Di Chiara et al., 1998) and stimulation of dopamine recepto
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next week br Conclusions In this paper
2021-09-01
Conclusions In this paper we describe the recombinant expression and characterization of ParI, a C5-DNA-MTase from P. arcticus 273–4. To our knowledge, this is the first characterization of an orphan C5-DNA-MTase from a psychrophilic bacterium. The C5-DNA-MTase could not be expressed in regular E
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Several research groups have disclosed potent and
2021-09-01
Several research groups have disclosed potent and selective DGAT-1 inhibitors from several chemically-distinct series. Pre-clinical studies with these compounds have confirmed that small molecule DGAT-1 inhibitors can elicit metabolic outcomes comparable to those observed in DGAT-1−/− mice.19, 20,
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br Structure of ketosteroid dehydrogenase Overall fold High
2021-09-01
Structure of 3-ketosteroid Δ1-dehydrogenase Overall fold — High-resolution crystal structures of Δ1-KSTD are currently available for the Δ1-KSTD1 isoenzyme from R. erythropolis SQ1 [30]. The Δ1-KSTD1 molecule has an elongated shape, and consists of two domains, an FAD-binding domain and a catalyt
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Dexamethasone DEX a potent synthetic glucocorticoid drug is
2021-09-01
Dexamethasone (DEX), a potent synthetic glucocorticoid drug, is effective for treatment of a range of inflammatory and autoimmune conditions as well as the reduction of side effects associated with chemotherapy. On the Czech Republic pharmaceutical market, DEX is incorporated into eighteen drugs use
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belinostat br Materials and methods br Results br Discussion
2021-09-01
Materials and methods Results Discussion Consistent with previous reports (Barr et al., 2010, Vuong et al., 2010), the current study demonstrates that rats treated with amphetamine exhibit heightened anxiety states during withdrawal. Furthermore, icv. infusion of a CRF2 receptor antagonist
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Further studies are needed as continuation
2021-09-01
Further studies are needed as continuation of this work to explore the effects of type and position of substituents of pyridazinone ring on anti-inflammatory activity profile. Taking into consideration that the phenyl moiety at position 2 wasn't a favorable substituent, even certain studies may be r
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AICAR br Acknowledgements br Introduction In Arabidopsis tha
2021-09-01
Acknowledgements Introduction In Arabidopsis thaliana (L.) Heynh, there are at least four copies of the caseine kinase-like gene Ck1, which is involved in peptide phosphorylation in mammals [1]. These genes are distributed on AICAR 1, 2, 4, and 5. A similar number of copies for Ck1 have been
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Selective inhibitor of phosphodiesterase type PDE I is
2021-09-01
Selective inhibitor of phosphodiesterase type 5 (PDE5I) is commonly used for ED treatment. PDE5I exhibits its vasodilatory effect by inhibiting the degradation of cyclic guanosine monophosphate (cGMP), which relaxes the smooth muscle and allows increased blood flow for penile tumescence. Udenafil (D
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In the brain E can modulate
2021-09-01
In the brain, E2 can modulate the mitogen-activated protein kinases/extracellular signal-regulated kinases (MAPK/ERK) pathway, which is involved in the formation of different memory types (Atkins et al., 1998, Blum et al., 1999, Schafe et al., 2000). When the MAPK/ERK signaling pathway is activated,
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The optimization of the lead compound
2021-09-01
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic SKF 81297 hydrobromide moiety with other functional groups led to loss of functional activity against EP
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