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We have shown that an extensive region
2024-12-26
We have shown that an extensive region in SERBP1 (amino acids 354 to 474, using co-ordinates based on the full-length isoform, Figs. 1a and 2) is necessary for it to interact with RACK1; since this region has substantial homology to the corresponding region of HABP1 (Fig. 3) it is a reasonable hypot
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Our research group has been involved by
2024-12-25
Our research group has been involved by many years in the synthesis of new 2,3-benzodiazepin-4-ones (e.g. 1, Fig. 1) and in the characterization of their mechanism of action.15, 16, 17 Within the development of these compounds, we demonstrated that an improvement of AMPAR antagonism by 2,3-benzodiaz
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It remains to elucidate whether proteolytic activity is the
2024-12-25
It remains to elucidate whether proteolytic activity is the cause or the consequence of changing levels of peptidergic substrates. In fact, in some cases, the expression of the enzyme does not necessarily parallel with its activity [26], [55], [57] and other factors such as a definite biochemical en
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MAFP AKT has been shown to be important for G S
2024-12-25
AKT1 has been shown to be important for G1-S checkpoint transition and proliferation, whereas AKT2 regulates cell-cycle exit through its interaction with p21 (Héron-Milhavet et al., 2006). In a recent study in triple negative breast cancer, AKT3, rather than AKT1 activity was most important for cell
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br Material and methods br Results br Discussion GRK
2024-12-25
Material and methods Results Discussion GRK2 activity has increasingly been shown to contribute to the progression of numerous diseases and organ dysfunction [5], [6]. For instance, a large body of work over the last two decades has identified GRK2 as a major regulator of cardiac dysfunctio
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It is important to note that stable amnesia
2024-12-25
It is important to note that stable amnesia is, apparently, a general biological phenomenon and can be found in different animal species. In studies on rats, it was found that if reconsolidation of conditioned olfactory aversion memory was impaired by the antagonist of NMDA glutamate receptors, amne
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quadrol In brief serotonin can interact with classes of rece
2024-12-25
In brief, serotonin can interact with 7 classes of receptors are differentiated into 14 subtypes (Barnes and Sharp, 1999). Specifically, 5-HT1A and 5-HT2C receptors have been the most widely studied in the modulation of anxiety responses (Deakin et al., 1992; Millan, 2003). However, the studies that
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br Concluding remarks ROP is a
2024-12-25
Concluding remarks ROP is a major cause of childhood blindness in the world. Current pharmacological therapy focus on anti-VEGF strategy, but this strategy is associated with the unintended effects on delayed eye growth and retinal vasculature development of preterm infants. Preclinical studies u
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During the course of our ACK inhibitor program a
2024-12-25
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident
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To date more than different mutations
2024-12-25
To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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Based on the observation that antipsychotic drugs increase
2024-12-25
Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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br Research perspective In vitro and in vivo studies
2024-12-25
Research perspective In vitro and in vivo studies have demonstrated that increased LPA/ATX signaling contributes to cancer initiation and progression. Recent findings on the role of non-tumoral ATX in cancer progression and metastasis highlighted a new functional contribution for the microenviron
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Celecoxib IC values were obtained for
2024-12-25
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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Then Autodock was employed for
2024-12-24
Then, Autodock4.2 was employed for site directed docking on AD with the ligands of the cluster(s) having high binding affinities in VS II experiment (Morris et al., 2009). Docking protocols were followed as per our earlier report with 200 GA (genetic algorithm) run (Kalani et al., 2015). Likewise, l
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In this study we showed that TRIM promotes ASK activation
2024-12-24
In this study, we showed that TRIM48 promotes ASK1 activation through ubiquitination-dependent degradation of a negative regulator of ASK1 activation, protein arginine methyltransferase 1 (PRMT1). Knocking down TRIM48 suppressed oxidative-stress-induced cell death mediated by ASK1, and the additiona
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