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We have previously established the pharmacokinetic profile a
2022-06-16
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 Calpeptin and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The compound
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br Material and methods br Results The
2022-06-16
Material and methods Results The search for proteins selectively expressed in pancreatic islet Vialinin A in the Human Protein Atlas (HPA) yielded 27 hits, including well-known islet cell markers such as insulin, glucagon and pancreatic polypeptide (Table 1). The search algorithm excluded isl
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G protein coupled receptor GPCR ligands
2022-06-16
G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa
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Experiments conducted on the human parasite Leishmania major
2022-06-16
Experiments conducted on the human parasite Leishmania major has shown that specific parasitic antigens are involved in steering the immune responses to “protective” as opposed to “disease” state (Reiner et al., 1993; Reiner and Locksley, 1995; and Sjölander et al., 1998) and that antigenic composit
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To confirm the in vitro findings atorvastatin or pravastatin
2022-06-16
To confirm the in vitro findings, atorvastatin or pravastatin was given to C57BL6/J mice fed with high fat diet. Doses of atorvastatin were set to be 6 mg/kg and 12 mg/kg, which were within clinical therapeutic doses. The results revealed that treatment of atorvastatin but not pravastatin impaired g
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In the course of our synthetic studies we also
2022-06-16
In the course of our synthetic studies, we also discovered an unprecedented application of Burgess reagent. Instead of generating an olefin by an intramolecular syn-elimination, the product resulting from the treatment of spirocyclic alcohols 11 and 12 with Burgess reagent led to the expansion of th
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While ghrelin s role in addictive
2022-06-15
While ghrelin's role in addictive behaviors has been most extensively explored with alcohol, ghrelin has also been implicated in biobehavioral substrates of other drugs of abuse. For example, preclinical experiments suggest that GHS-R1a blockade may improve nicotine [155,156], opioids [[157], [158],
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Two excellent GSMs with clear
2022-06-15
Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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The effect of GC on Fgf was not
2022-06-15
The effect of GC on Fgf21 was not directly dependent on ileal Fgf15 because basal Fgf21 Indacaterol Maleate sale was similar in Fgf15+/+ and Fgf15−/− mice. Moreover, GC treatment induced similar Fgf21 up-regulation in both strains. Fxr activation has been reported to increase Fgf21 expression and se
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LPCs have been previously described as potential anti diabet
2022-06-15
LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al
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The exact mechanism by which N BPs inhibit FPPS
2022-06-15
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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The iAs mainly metabolized in the liver to generate
2022-06-15
The iAs mainly metabolized in the liver to generate MMA and DMA. DMA, MMA and iAs were excreted through the urine (Khaleghian et al., 2014; Wei et al., 2017a). Pearson correlation coefficient was used to explore associations between concentrations of three arsenic species in urine and gene expressio
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Data are expressed as means SE
2022-06-15
Data are expressed as means±SE. Statistical significance was determined by the Student's -test or ANOVA with post hoc Bonferroni test. A value of MK 571 synthesis expressing human FPPS. Western blot analysis showed a clear band, which indicated the overexpression of FPPS, in U87MG cells (A, insert)
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br Challenges and open questions
2022-06-15
Challenges and open questions Deepening our understanding of PKC’s role in GSIS will require harnessing recently developed techniques and developing new tools. Here we describe three challenges remaining in the field and offer suggestions on experimental approaches to address them. PKC plays an
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Valinomycin Despite the two models for the HIV IN
2022-06-15
Despite the two models for the HIV-1 IN-aptamer complexes appeared to be comparable, disintegration assays revealed that 93-del inhibited C– or N-terminally truncated enzyme at the same extent, [18] whereas, T30695 required N-terminal domain (NTD) of the enzyme to exert its integrase inhibitory acti
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