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We also explored various nitrogen substituents
2021-12-29
We also explored various nitrogen substituents with an aim toward modulating sterics and basicity within the ABH series. No glycine uptake inhibition was detected with non-basic bicycles (data not shown). Isopropyl was the best compromise between desired on-target effect and clearance, however, eff
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br Methods br Results br Discussion
2021-12-29
Methods Results Discussion Significant alterations in the expression of genes related to the glutamatergic system have been shown in several experimental models of epilepsy; however, in most studies focused on acute changes or modifications in expression, these were investigated during the
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The main aim of our study was to identify
2021-12-29
The main aim of our study was to identify whether glucokinase and Irs2 were required for beta cell replication induced by short-term HF diet feeding. Glucokinase plays a critical role in regulating blood glucose levels by catalysing the rate-limiting biochemical reaction of glycolysis [26,27]. In pa
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Multiple mechanisms have been suggested by which glucagon
2021-12-29
Multiple mechanisms have been suggested by which glucagon can increase energy expenditure although none have been conclusively proven to be responsible. Both enhanced gluconeogenesis and enhanced protein turnover secondary to hyperglucagonaemia have been suggested as the reason for the increased met
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However protection against kainic acid induced injury was
2021-12-28
However, protection against kainic acid-induced injury was not found by Lin et al. (2003) in the rats with AAV-GAL vector-mediated galanin overexpression, even though these animals, as mentioned earlier, exhibited attenuated of seizure severity. Although the reason for the controversy between the st
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br Results br Discussion The inflammasome consists
2021-12-28
Results Discussion The inflammasome consists of the sensor molecule nucleotide oligomerization domain (NOD)-like receptors (NLRs), the adaptor protein ASC, and the nsc library molecule CASP1 (Guo et al., 2015). Among the different types of inflammasome, the NLRP3 inflammasome requires a primi
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The C terminal regions in both
2021-12-28
The C-terminal regions in both FGF19 and FGF21 define their KLB interaction [15], [16], [23], [25]. However, less than 40% identity in comparative alignment of C-terminal sequences for these two proteins (Table 1) suggests that their interaction with KLB may require higher-order association with oth
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The exact mechanism by which N
2021-12-28
The exact mechanism by which N-BPs inhibit FPPS remains unclear. Computer modeling [10] suggests that N-BPs mimic the structure of the enzyme’s natural isoprenoid pyrophosphate substrates, geranyl pyrophosphate (GPP)/dimethylallyl pyrophosphate (DMAPP) or act as carbocation transition state analogs
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In order to establish proper
2021-12-28
In order to establish proper folding and enzymatic activity, G9a and GLP methyltransferases each contain four structural zinc ions. Both Aripiprazole contain two distinguishable types of zinc fingers; three Zn(II) ions are chelated in a triangular cluster by 9 cysteines (b, top left), whereas one Zn
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Relative to the impact of
2021-12-28
Relative to the impact of moderate PAE on markers of histaminergic neurotransmission, there were four salient observations from the studies reported here. First, it does not appear that moderate PAE affects the number of HDC-positive neurons in the tuberomammillary nucleus of the ventral hypothalamu
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The inhibition of HDAC increases the level of histone
2021-12-28
The inhibition of HDAC increases the level of histone acetylation and consequently turns the chromatin to be loose and active, allowing multiple transcription factors to access to promoters of diverse genes including tumor suppressor genes []. As compound possessed potent HDAC inhibitory activity an
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A repertoire of cytotoxic payloads is increasing
2021-12-28
A repertoire of cytotoxic payloads is increasing; among those, MMAE has been utilized for the highly effective ADC brentuximab vedotin. However, the ADCs which utilized MMAE to target GCC in solid tumors have shown a poor efficacy suggesting that various tumor types respond differently to a given to
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br Introduction The discovery that the nitric oxide NO
2021-12-28
Introduction The discovery that the nitric oxide (NO), soluble guanylate cyclase (sGC), and cyclic guanosine monophosphate (cGMP) pathway mediates erection has led to the use of phosphodiesterase type 5 (PDE-5) inhibitors as the gold standard for treating erectile dysfunction (ED) through the inh
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br Materials and methods br Results br Discussion Recently
2021-12-28
Materials and methods Results Discussion Recently, we characterized the interaction of the PH domains of various Lbc family RhoGEFs with the activated small GTPase, RhoA, and demonstrated that this could serve as a positive feedback mechanism for robust activation of RhoA (Medina et al., 20
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Originally identified as a GPCR upregulated on Burkitt lymph
2021-12-28
Originally identified as a GPCR upregulated on Burkitt lymphoma cells upon Epstein-Barr virus infection (Birkenbach et al., 1993), Ebi2 was later found to play critical roles in immunity by regulating the migration of activated DAPI hydrochloride synthesis to extrafollicular sites for early plasmabl
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