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Molecular docking study of compound was performed using the
2020-06-28
Molecular docking study of Cobimetinib was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and the cyano-hyd
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EP is the major receptor to mediate
2020-06-28
EP4 is the major receptor to mediate PGE2-induced inflammatory pain. EP4 is upregulated by JNJ-10198409 australia in DRG neurons [16]. Intrathecal injection of the EP4 agonist produced pain responses [25]. Either systemic or local injection of EP4 antagonists relieves inflammatory pain [3], [16], [
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wst-1 assay Since the number of peptides hydrolized by
2020-06-28
Since the number of peptides hydrolized by PEP is quite large, it is not easy to relate the increase of enzymatic activity with the altered changes of a concrete peptide. However, it is noticeable that imbalances of several natural substrates of PEP [6], such as angiotensins, bradykinin, vasopressin
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Metal ions are known not to be necessary for catalytic
2020-06-28
Metal ions are known not to be necessary for catalytic activity of serine proteinases. Nevertheless, Co2+ and Ca2+ ions were found to stabilize glutamyl endopeptidase molecule [1], [7], [19]. In our previous study, we have described significant stimulating effect of Ca2+, Mg2+, and Co2+ on biosynthe
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br Ubiquitylation of the TGF BMP pathway components Ubiquity
2020-06-28
Ubiquitylation of the TGFβ/BMP pathway components Ubiquitylation is a reversible post-translational modification that is essential in many cellular regulatory mechanisms [20], [21]. During the ubiquitylation cascade, ubiquitin is attached to target proteins through the concerted actions of an E1-
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Hydrocortisone Electroencephalographs at onset ranged from h
2020-06-24
Electroencephalographs at onset ranged from hypsarrhythmia to mild abnormalities but more abnormalities in background rhythms and epileptiform activity develop over time.15, 17, 19, 48, 52, 54, 55 Early mild abnormalities that sometimes precede a diffuse encephalopathy included focal delta slowing i
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br Conclusions CK inhibition protects young and
2020-06-24
Conclusions CK2 inhibition protects young and aging WM function against an ischemic episode by preserving oligodendrocytes and axonal structure by maintaining mitochondrial integrity. CK2 recruits CDK5 and AKT/GSK3ß signaling to mediate WM ischemic injury in a differential spatiotemporal manner s
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Nimodipine is an L type calcium channel antagonist that
2020-06-24
Nimodipine is an L-type calcium channel antagonist that reduces excessive calcium influx during pathological conditions, contributing to its neuroprotective properties (Zornow and Prough, 1996; Kobayashi and Mori, 1998). Autophagy can be induced by increased [Ca2+] (Rami et al., 2008). Nimodipine si
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br Conflicts of interest br Introduction
2020-06-24
Conflicts of interest Introduction G protein-coupled receptors (GPCRs), form the largest human membrane protein family, with 800 members overall. Many druggable targets for treatment of common diseases involve GPCRs that mediate therapeutic effects of 34% of all marketed drugs (Hauser, Attwood
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Industrial fermentation aims to produce valuable products fr
2020-06-24
Industrial fermentation aims to produce valuable products from cheap feedstocks by utilizing diverse microbial functions through aerobic or anaerobic fermentation [[8], [9], [10]]. During anaerobic fermentation, the reducing power is mostly directed to product synthesis rather than being oxidized, r
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There have been two reports
2020-06-24
There have been two reports of tumor shrinkage in response to dasatinib treatment in lung SCC patients harboring the DDR2 kinase domain S768R mutation., In the first case described by Hammerman et al. a combination of erlotinib (an epithelial growth factor receptor inhibitor) and dasatinib was admin
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In a previous study we reported that
2020-06-24
In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in Asiaticoside reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present experiments was to inv
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Regarding the effects of CRF on
2020-06-24
Regarding the effects of CRF on anxiety, Sahuque et al. (2006) have demonstrated that this neuropeptide also enhances anxiety when injected into the bed nucleus of the stria terminalis (BNST), a Puromycin aminonucleoside structure that has also been related to defensive behavior (Casada and Dafny,
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Among the other mediators which have been reported to
2020-06-24
Among the other mediators which have been reported to play a role in erection are prostaglandins (PGs). Several studies have reported that alprostadil- synthetic PGE1- showed high efficacy in management of erectile dysfunction as it induces corpus cavernosal relaxation. Alprostadil has been first de
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One architecture termed closed has
2020-06-23
One architecture, termed closed, has been visualized at near-atomic resolution in cryo-EM maps of recombinant complexes that superimpose with earlier lower-resolution EM data obtained for APC/CCDC20–MCC purified from HeLa VTX-2337 receptor arrested during the mitotic checkpoint (Figure 4E) 38, 48,
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