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GSK is inhibited by serine phosphorylation at a
2022-03-28
GSK-3 is inhibited by serine Ro 48-8071 at a residue its N-terminus (Ser 9 in GSK-3β and Ser 21 in GSK-3α) [52], [53], [54]. This raised the possibility that the N-terminal tail may function as a pseudo-substrate by mimicking the pre-phosphorylated substrate. The interaction mode of the pseudo-subs
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We have previously established the pharmacokinetic profile a
2022-03-28
We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in hcv virus and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The compound
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We have previously established the pharmacokinetic profile a
2022-03-28
We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in SB 239063 sale and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The com
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siRNA construction and transfection For small
2022-03-28
siRNA construction and transfection. For small interfering RNA (siRNA) experiments, we used Stealth™ select RNAi oligonucleotides targeted against GPR120 (Gibco/Invitrogen). The target sequence of siGPR120 used were; sense 5′-AAGUGGGUGCGAUUGACUUGGUCCA-3′ and antisense 5′-UGGACCAAGUCAAUCGCACCCACUU-3′
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The top concern for the clinical use of
2022-03-28
The top concern for the clinical use of CRISPR-Cas9 technology is safety. Off-target alterations must be avoided to ensure genome integrity and proper cellular function. WGS found no off-target effects among the top 49 predicted off-target sites. WGS did find 4,658 indels and 1,891 SNVs in sgRNA1/2-
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Diabetes induced damage results in
2022-03-28
Diabetes-induced damage results in peripheral nerve pathology that d-glucose correlates with clinical signs and symptoms. Nerve injury that results in structural changes can be measured through clinical neurological assessment, quantitative sensory testing, nerve conduction studies, and peripheral
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Depending upon the varied habitats e
2022-03-28
Depending upon the varied habitats (e.g. soil, water, animal digestive tracts, etc.), microbes possess a diverse range of carbohydrate ABC transporters and metabolic pathways (Rodionov et al., 2013; Bräsen et al., 2014). Thermus thermophilus HB8, a thermophilic gram-negative bacterium dwelling in ho
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Tamoxifen Due to its unusually long pre
2022-03-26
Due to its unusually long pre-implantation period [20,21], the horse conceptus is entirely dependent on histotrophic nutrition for the first 40 days of gestation [22]. During the pre-implantation period, glucose transporters in the endometrium and conceptus membranes must deliver the glucose require
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The structural similarity software vROCS OpenEye has been ut
2022-03-26
The structural similarity software vROCS (OpenEye) [45] has been utilized by Musumeci et al. [46] to screen the Maybridge [47] HitFinder database (∼14,400 compounds) using Distamycin A (Fig. 3B) as a query. Using the Tanimoto coefficient (Section 6.4) and vROCS's colour scoring (atom/feature similar
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In early a collaborative effort between the group that
2022-03-26
In early 2017, a collaborative effort between the group that pioneered the above described evidence of platinum-induced PUFA chemotherapy resistance and a group that has contributed to much of the known molecular pharmacology of FFA4, revealed that the molecular target of 16:4(n-3), which affords ch
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Here we investigated on epigenetic regulatory mechanisms of
2022-03-26
Here, we investigated on epigenetic regulatory mechanisms of ALX/FPR2 expression. Epigenetic changes, that include phosphorylation, acetylation, methylation and ubiquitination of DNA and histone proteins, occur in a variety of diseases [21] and are being recognized as key targets for personalized me
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The PK and the tissue distribution profiles of
2022-03-26
The PK and the tissue distribution profiles of 15k, 15j, 14d and 2 (Table 8) in male ICR mice were assessed. 15k, 15j, 14d all exhibited prolonged half-lives and improved plasma exposure. 15k achieved the highest concentration (15.45 μg/mL) in plasma among four compounds. The observation that 15j (S
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Our results are consistent with the hypothesis that
2022-03-26
Our results are consistent with the hypothesis that reduced Fas-mediated apoptosis in maternally activated T-lymphocytes could result in insufficient trophoblast invasion of the spiral MMP-2 Inhibitor I mg as the activated T-lymphocytes become able to enhance the destruction of the cytotrophoblasts
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The exact mechanism by which N BPs inhibit FPPS remains
2022-03-26
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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br Development of calibrators and controls for DiXaIs br Met
2022-03-26
Development of calibrators and controls for DiXaIs Method validation and comparison with reference technique (LC:MS) At this stage, anti-Factor Xa bioassays can be established for reliably measuring DiXaI concentrations in plasma, with the available appropriate drug specific calibrators and co
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