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In conclusion we have demonstrated that diaryl
2024-03-21
In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi
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br Conclusions Triptans are HT B D F receptors agonists
2024-03-21
Conclusions Triptans are 5-HT1B/1D/(1F) receptors agonists and are considered as the gold standard for acute migraine treatment that have been proven effective. Unfortunately, they are contraindicated in patients with cardiovascular diseases due to their vasoconstrictor (side) effects (MaassenVan
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Here we report discovery of highly selective pan Aurora
2024-03-21
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of antisedan mg bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction.
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br Acknowledgments br Introduction Cancer is a deadly
2024-03-21
Acknowledgments Introduction Cancer is a deadly disease of uncontrolled cell division and has the potential to invade or spread to other parts of the body and affects normal functioning of the vital organs. Nowadays cancer is considered as leading cause of human death in all over the world and
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Another possible explanation of the
2024-03-21
Another possible explanation of the increased BOP levels might be excess cement. In the present study, cement-retained fixed restorations were used. Cementation of the implant-supported restorations may cause the insufficient removal of excess cement from the peri-implant sulcus. Also, the placement
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For the derivatives a c another likely
2024-03-21
For the derivatives 3a–3c, another likely explanation for antifungal properties is that polymers bearing primary amine groups and secondary phosphoryl groups formed, enhancing complexation with the phosphate groups, and the complexes are amphiphilic (Palermo, Lee, Ramamoorthy, & Kuroda, 2011). The a
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br Brain Angiotensin II receptors
2024-03-20
Brain Angiotensin II receptors The information above leaves Angiotensin II receptors as the only RAAS components for which localization, regulation of expression and function in the straight from the source has been convincingly demonstrated, with the use of quantitative film and emulsion autora
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br Conflict of interest statement br Introduction Tanshinone
2024-03-20
Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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Recent results suggest that TARPs are not the
2024-03-20
Recent results suggest that TARPs are not the only auxiliary AMPAR subunits. Using a proteomic strategy (affinity purification of native AMPAR complexes followed by mass-spectrometric analysis), cornichon-related proteins (CNIHs) have been recently identified as components of the AMPAR protein micro
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br COX and LOX in
2024-03-20
COX and 5-LOX in post-mortem AD brain Minghetti (2004) reviewed the findings on COX-2 mRNA levels in AD brains, pointing out that the available evidence demonstrated either decreased or increased levels, possibly because of the short half-life of COX-2 transcripts or individual variability. Histo
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We have recently reported a regulatory effect of quercetin o
2024-03-20
We have recently reported a regulatory effect of quercetin on the AChE activity in the brainstem during the demyelination and remyelination process [17]. It has also been observed that there is a protective effect on lipid peroxidation and worsening of motor functions caused by loss of myelin in the
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Activated MAP kinases transform the
2024-03-19
Activated MAP kinases transform the stimulus into the pathophysiological responses by phosphorylating downstream substrates, including transcription factors, cytoskeletal proteins involved in mRNA translation (Li et al., 2015). Among the numerous effectors that intervene in the TNF-α action is an ac
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At the outset of targeting the two Gln side chain
2024-03-19
At the outset of targeting the two Gln756 side-chain rotamers, it was unclear which rotational isomer would lead to more potent ASK1 inhibitors. While such a preference might have been anticipated, the cohort of ASK1 inhibitors in Table 3 did not provide any guidance regarding which of the Gln756 am
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The most likely explanation for
2024-03-19
The most likely explanation for the species differences in aromatase distribution and the unique DAPI hydrochloride distribution in humans is the unique location, size and highly elaborate organization of the human aromatase gene (e.g. Bulun et al., 2003). The human Cyp19 is a large gene located on
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br Experimental procedures br Results br Discussion Although
2024-03-19
Experimental procedures Results Discussion Although previous studies have indicated that astrocyte aromatase plays a role in nociceptive processes (O'Brien et al., 2015, Smeester et al., 2016), the mechanisms responsible for the regulation of aromatase and its involvement in nociception rem
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