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br Molecular modeling simulation study Molecular
2021-04-28

Molecular modeling simulation study Molecular modeling study was performed through docking of the test compounds into the binding site of hDHFR enzyme using Discovery Studio 2.5 software. Computational docking is an algorithm designed to determine the suitable position and the orientation of the
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Substituents at the C position An oxygen containing
2021-04-28

Substituents at the C11 position — An oxygen-containing substituent at the C11 position also affects the catalytic activity of Δ1-KSTDs. The Δ1-KSTDs from the Gram-positive bacteria R. equi [29], N. simplex ATCC 6946 and IFO 12069 [48,49,52], and R. rhodochrous IFO 3338 [27] were able to 1(2)-dehydr
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Cystatins are potent inhibitors of
2021-04-27

Cystatins are potent inhibitors of cysteine proteases from the C1A family. These inhibitors primarily reduce the activities of cathepsin L-like proteases, although high concentration of barley cystatin hampers the degradation of storage proteins caused by cathepsin F-like protein (HvPap-1) (Cambra e
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Conversely to the reduction in restraint evoked HR increase
2021-04-27

Conversely to the reduction in restraint-evoked HR increase following the blockade of CRF receptors, Nijsen et al. [28] demonstrated that BNST treatment with a nonselective CRF BIX 01294 antagonist enhanced the tachycardia evoked by contextual fear conditioning. Taken together, these results indica
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panx Magnified regions of the upregulated
2021-04-27

Magnified regions of the upregulated proteins identified by MALDI-TOF are shown in Fig. 2. The identified proteins were phosphoglycerate kinase, fructose-bisphosphate aldolase class II, alcohol dehydrogenase, phosphoglyceromutase, 6-phosphogluconolactonase, malate dehydrogenase, alkyl hydroperoxide
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br Criteria for ER targeted fluorescent probes br Survey
2021-04-27

Criteria for ER-targeted fluorescent probes Survey of fluorescent probes Proposed approach to high affinity fluorescent steroidal ER probes Our proposed approach to the development of a new generation of fluorescent estrogen receptor imaging agents employs many of the elements present in th
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ROS generation is crucial for NETs release upon both
2021-04-27

ROS generation is crucial for NETs release upon both physiological or pathogenic stimuli [16,30]. In our study, we further verified this conclusion by demonstrating that SRA stimulation by Poly I enhanced intracellular ROS levels while scavenging of ROS by anti-oxidant agents effectively abolished t
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br Conflict of interest br Acknowledgements This work
2021-04-27

Conflict of interest Acknowledgements This work was supported by the Basic Science Research Program through the National Research Foundation (NRF) funded by the Ministry of Science, ICT & Future Planning (2013R1A1A1076117) and also by the Priority Research Centers Program through the NRF funde
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Regarding eicosanoid production iPLA VIA
2021-04-27

Regarding eicosanoid production, iPLA2-VIA appears, in general terms, not to play a major role in mediating this response in innate immunity and inflammation, as evidenced by the large number of studies highlighting the lack of effect of selective inhibition of the enzyme in stimulus-induced AA rele
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Collectively the results presented here provide new insights
2021-04-27

Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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In all available E E structures the RING
2021-04-27

In all available E2:E3 structures, the RING-type domain binds the E2 on a surface that is remote from the active site Cys (and therefore from the ubiquitin thioester) (Fig. 2). The non-contiguous E3-binding and active sites on the E2 imply that the role played by a RING to facilitate ubiquitin trans
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Similarly synthetic analogs of Alogliptin by replacing
2021-04-26

Similarly synthetic analogs of Alogliptin by replacing the cyanobenzyl group with the butynyl group have been synthesized and tested as selective DPP-4 inhibitors [7], [8]. Additionally, quinazolines [9], [10], pyridopyrimidinediones [11], pyrazolopyrimidinones [12] and pyrimidines [13] as DPP-IV in
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br Application of D receptor
2021-04-26

Application of D1-receptor PET in psychiatric disorders Discussion Compared to other markers of the DA system, only a limited number of studies have investigated D1-R in psychiatric disorders. In schizophrenia, which is the most studied condition with a total of 83 identified unique patients,
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cGAS has a central role in
2021-04-26

cGAS has a central role in STING activation after DNA sensing, but it is unknown if most of the DNA sensors act independently or in cooperation with the cGAS-cGAMP pathway. This was addressed for IFI16 (Almine et al., 2017, Jønsson et al., 2017) and PQBP1 (Yoh et al., 2015) but remains to be tested
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br Materials and methods br Results
2021-04-26

Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy
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