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In terms of the ring B C position while C
2023-11-16
In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge
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Given these findings above we hypothesized that hypernocicep
2023-11-15
Given these findings above, we hypothesized that hypernociception produced by intra-amygdala 8-OH-DPAT is result of hyperpolarization in this area. This neuronal inhibition of the amygdaloid complex might result in an inactivation of crucial neurotransmitter systems of the descending inhibitory pain
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Interestingly this situation might be changed
2023-11-15
Interestingly, this situation might be changed by the immunological context, in particular by the cytokines encountered during differentiation or activation. LPS-activation of bone marrow-derived DCs differentiated in GM-CSF decreases autophagy, CP2, and subsequent activation of CD4+ T cells (Fig. 2
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Aurora kinases were initially identified as
2023-11-15
Aurora kinases were initially identified as protein kinases essential for error-free chromosome segregation during mitosis and meiosis. Aurora A appears to control premetaphase events, such as bipolar spindle assembly 3, 4, with Aurora B and C directing metaphase and postmetaphase events, including
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Aurora A the polar kinase is located at the centrosome
2023-11-15
Aurora A the ’polar kinase’ is located at the centrosome and is required for its maturation, division, for the mitotic spindle assembly and entry into mitosis., Mutation or transcriptional silencing of Aurora A impairs centrosome maturation and separation, leads to mono/multipolar spindles, to dela
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ProteOrange The co crystal structure of blebbistatin bound t
2023-11-15
The co-crystal structure of ()-blebbistatin ()- bound to myosin II (PDB: ) was used to scout for possible favorable interactions with the residues lining the binding pocket. Looking at A, we hypothesized that -oriented hydrophilic moieties (e.g. hydroxymethyl) on C of the blebbistatin scaffold migh
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In addition to drawing attention to Ser of
2023-11-15
In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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AT signaling is distinct to that of AT
2023-11-15
AT2 signaling is distinct to that of AT1 (Kaschina and Unger, 2003). As shown here, opposite to the stimulating effect of AT1 signaling, it inhibits apelin secretion. Activation of AT2 receptor, which is also G-protein coupled, is known to decrease cAMP and cGMP levels by inhibiting adenylyl cyclase
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AP activity is increased by MAP kinase
2023-11-15
AP-1 activity is increased by MAP kinase stimulation in different cell types (Whitmarsh and Davis, 1996), while MKP-1, the enzyme that catalyzes the dephosphorylation and inactivation of MAP kinases in the nucleus, inhibits AP-1 (Rössler et al., 2008, Rössler and Thiel, 2009, Mayer et al., 2011, Thi
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Limitations of this study include the use
2023-11-15
Limitations of this study include the use of HL-1 cardiomyocytes, which show different characteristics than primary cardiomyocytes [56]. Furthermore, sustained TAC in Ampkα1-deficient mice did not favorably influence cardiac function [33]. It must be kept in mind that global Ampkα1-deficiency may af
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In Pham et al employed the microsphere
2023-11-15
In 2014, Pham et al. [22] employed the microsphere-based technology to create a Luminex probe-based assay for the rapid identification of single nucleotide polymorphisms that are known to confer resistance to one or more echinocandins in C. glabrata. The targets for the FKS probes were generated usi
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For the first series we decided to verify
2023-11-15
For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives
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Since the cloning of ARs in
2023-11-15
Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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br Results br Discussion The actin cytoskeleton is
2023-11-14
Results Discussion The Probenecid cytoskeleton is a highly attractive target for many bacterial toxins, owing to its role in activation and locomotion of immune cells, secretion of humoral response factors, and maintenance of protective barriers at the cellular (sub-membrane cytoskeleton) and
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The GRAVY value for a protein is
2023-11-14
The GRAVY value for a protein is calculated as the sum of hydropathy values of all the amino acids, divided by the number of residues in the sequence (Kyte and Doolittle, 1982). According to Kyte and Doolittle (1982) integral membrane proteins typically have higher GRAVY scores than do globular prot
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