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Cystatins are potent inhibitors of cysteine proteases from t
2020-11-26
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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The sequence identity of CYP A with CYP A
2020-11-26
The sequence identity of CYP3A163 with CYP3A sequences from other species is maximum in reptiles ranging (75-91)%, gradually decreasing from anatoxin a (63-71)% to mammals 62% to downwards based on evolutionary distances. The high level of homology with CYP3A77 in Alligator mississippiensis suggest
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Another breakthrough towards the understanding
2020-11-26
Another breakthrough towards the understanding of the mechanisms responsible for stress-induced relapse to drug seeking behaviour is the evidence published by the group of Wise [34] in which they show that the activation of VTA CRF2 and not CRF1 receptors is responsible for stress-mediated relapse t
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Based on the finding described
2020-11-26
Based on the finding described above, the present study was designed to investigate the effects of specific CRF receptors, CRF1 and CRF2, in the BLA and CeA on the duration of TI in guinea pigs (Cavia porcellus). To this end, we evaluated whether administration of the CRF1 AP 18 antagonist CP-37639
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This study evaluated the role
2020-11-26
This study evaluated the role of SERT in classical fear conditioning using a SERT knockout rat model. We found a clear disruption of cue-conditioned fear in SERT−/− rats, as measured with the fear-potentiated startle. This disruption was due to a deficit in fear acquisition and was accompanied by de
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Furthermore positioning the naphthalene nucleus
2020-11-26
Furthermore, positioning the naphthalene nucleus in 3d within the main active site and forming one hydrogen bond with Tyr385 in addition to many hydrophobic interactions with Val349, Leu352, Gly526, Ala527 and Leu531 residues, correlates well with the position and hydrophobic interactions of the tri
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Application of the CPH model
2020-11-26
Application of the CPH model relies on the assumption that the hazard ratio of two observations is constant over time [2]. This enables us to infer the rate of risk of the treatment. For example, in the study of patients with pulmonary arterial hypertension (PAH) [5], the hazard ratio of a group of
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Sensory gating describes a filter
2020-11-26
‘Sensory gating’ describes a filter mechanism protecting the central nervous system from sensory overload by inhibiting behaviorally irrelevant input (Boutros et al., 2004, 2008). This permits Mirin to a changing contextual environment (Fruhstorfer et al., 1970; Grunwald et al., 2003). Auditory gat
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It should be noted that the
2020-11-26
It should be noted that the long-lifetime binding-responsive luminescence of ARC-1528 and ARC-1530 becomes evident only upon illumination with radiation at near-UV range where the excitation of ATB or ASB moiety is possible. At higher wavelength range (visible light), the fluorophore (5-TAMRA) can b
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br Results and discussion br Conclusion In
2020-11-26
Results and discussion Conclusion In this investigation, pharmacophore models of CK1 inhibitors were developed using a pharmacophore modeling protocol proposed by us. The optimal pharmacophore hypothesis, Hypo2, was adopted to retrieve potential CK1 inhibitors from the commercial chemical data
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In most cases the ligand affinity between subtypes is
2020-11-26
In most cases, the ligand affinity between subtypes is similar, but their tissue distribution is different. In the case of the estrogen receptors (ER), two subtypes (ERα and ERβ) exist (Kuiper et al., 1996) and ERβ has several isoforms, designated ERβ1–5 (Moore et al., 1998) or ERβcx (Ogawa et al.,
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MoAbs targeting the tumourigenic pathways such as IGF
2020-11-26
MoAbs targeting the tumourigenic pathways, such as IGF-1R may theoretically have a dual working mechanism. On the one hand they block pathways having an anti-tumour working mechanism, and on the other hand they may also stimulate an immunological response inducing a reaction of the patients own imm
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Dual inhibition of ACE and NEP as a strategy for
2020-11-25
Dual inhibition of ACE and NEP as a strategy for treating hypertension has been extensively investigated, including contributions from these laboratories through the discovery of Sampatrilat . Given that both targets are related zinc metalloproteinases, dual enzyme inhibition can be achieved within
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In terms of its protease
2020-11-25
In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other often line up to buy of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target and degrade t
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As in our earlier observations the PTPN SNP affected
2020-11-25
As in our earlier observations, the PTPN22 SNP affected the appearance of β-cell autoimmunity, but in contrast to our earlier report, only a borderline effect of the PTPN22 SNP on the progression to clinical disease was observed in the current analysis [22], [27]. The finding of an effect of the PTP
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