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We have previously established the pharmacokinetic profile a
2022-05-10
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 Enalapril Maleate receptor and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [
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Generally replacement of the aryl group was well tolerated
2022-05-10
Generally, replacement of the aryl group was well tolerated, with tetrahydropyran () and hydroxyl () functionality providing potency equivalent to and . These substitutions had no effect on selectivity versus GlyT2 and taurine transporter (TauT)—no activity was observed at micromolar concentrations.
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br Inclusion exclusion criteria br Quality assessment All
2022-05-10
Inclusion/exclusion criteria Quality assessment All studies included in the qualitative synthesis were evaluated using the Quality Assessment Tool for Quantitative Studies (QATQS), which allows to determine their methodological quality. QATQS assesses 8 sections: selection bias, study design,
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Because AM had limited efficacy on rodent GPR
2022-05-10
Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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GIPR genes were not found in any of
2022-05-09
GIPR genes were not found in any of the available bird genome as well as the genomes of several species of fish (Tables S3 and S4). The genomic neighborhoods surrounding the GIPR genes in species that have them was generally conserved (see Fig. 8), and like GLP2R, those fish that did have a Gipr gen
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With rare exceptions the biological role of secretase cleava
2022-05-09
With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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br Concluding remarks In this
2022-05-09
Concluding remarks In this small material of thirteen pituitary tumors of various kinds, we could not run statistical analysis. However, with a follow-up period of up to five years, we show that Disclosure Statement Acknowledgments Introduction Galanin is a 29/30-residue neuropeptide fo
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cddo br Experimental section br Acknowledgements This
2022-05-09
Experimental section Acknowledgements This study was supported by grants from the National Natural Science Foundation of China (Grants 81673299 and 81273376). Introduction Free fatty acids (FFAs) are important metabolic fuels and those that are polyunsaturated are essential components of t
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Piroxicam belongs to the oxicam family of NSAIDs
2022-05-09
Piroxicam belongs to the oxicam family of NSAIDs and a special attention has been drawn to this drug because of its multifunctional potential [5], [27], [28]. Chemically, piroxicam (4-hydroxy-2-methyl-N-2-pyrimidyl-2H-1,2-benzothiazine-3-carboxyamide) is an enolic Ropivacaine HCl mg with a size com
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br Acute host defense Inflammation
2022-05-09
Acute host defense Inflammation, the host response to infection and tissue injury, is crucial for survival and restoration of tissue structure and function. This acute response is mediated and governed by a variety of pro-inflammatory circuits to ensure recognition of invading pathogens, coordina
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The inhibitory activities of the compounds with
2022-05-09
The inhibitory activities of the compounds with the modification of the amino group against human liver FBPase are summarized in . Replacement of the amino group of with hydrophobic substituent such as a methyl group () led to a substantial loss of activity (IC=995nM). Similarly, replacement with h
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br Acknowledgments We apologize for the omission
2022-05-09
Acknowledgments We apologize for the omission of primary citations owing to space limitations. This work was supported by grants from National Natural Science Foundation of China (81772801 and 81472455 to C.D.), the Key Program of Zhejiang Provincial Natural Science Foundation (LZ17H160002 to C.D
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Rhapontigenin Consistent with our result Camacho Barquero
2022-05-09
Consistent with our result, Camacho-Barquero and coworkers showed that curcumin reduced phospho-P38 MAPK. P-38 MAPK is a key effector of several downstream factors that eventually modulate the homing of monocytic cells during the onset of intestine inflammation (Camacho-Barquero et al., 2007). Along
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br Results br Discussion In this
2022-05-09
Results Discussion In this study, six new T30695 variants were synthesized with the acyclic R or S glycerol linker instead of PF-543 unit at 4, 8 or 12 T residue. Based on our previous studies on TBA-GQ, this type of modification should provoke local changes in GQ conformations in the final T
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More recently the JmjC domain histone H K
2022-05-09
More recently, the JmjC domain histone H3K36 di-demethylase KDM2B/FBXL10 has also been shown to play an important role in definitive hematopoiesis [17]. Kdm2b is highly expressed in the HE, and its deletion (Tie2) caused embryonic lethality due to a precipitous drop in the number of hemogenic endoth
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