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br Conclusions and perspectives br Acknowledgements This wor
2021-11-12
Conclusions and perspectives Acknowledgements This work was supported by the National Natural Science Foundation of China (Grant Nos. 21802173, 21405182 and 21773315), the Natural Science Foundation of Guangdong Province (Grant Nos. 2018A030310301, 201710010019 and 2014A030313232, 201804020025
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Thus from this preliminary study a working model
2021-11-12
Thus from this preliminary study, a working model of HIV-1 integrase was developed from which a selective inhibitor of the strand-transfer reaction displaying whole-cell activity and negligible cytotoxicity was produced. Compound 9 provides a promising scaffold for further elaboration, and current i
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br Discussion This study dedicated to histamine H and
2021-11-12
Discussion This study, dedicated to chembridge H3 and H4 receptors, was carried out on superfused tissues preincubated with 3H-choline or 3H-noradrenaline; electrical stimulation was used to elicit quasi-physiological exocytotic release of the respective transmitter. Since inhibition of transmit
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Studies conducted in our laboratory
2021-11-12
Studies conducted in our laboratory, thus far, have shown that HKDC1 is broadly expressed [28]. Using the first developed HKDC1 mouse model, we found that complete loss of HKDC1 function is embryonic lethal, similar to other HKs [29,30]. Further studies using HKDC1 heterozygous knockout mice showed
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HER genotype was determined in breast cancer tissue of breas
2021-11-12
HER2 genotype was determined in breast cancer tissue of 73 breast cancer patients. As previously reported, Ile655Val and Ala1170Pro genotypes measured in breast cancer tissues were available for 71 and 69 breast cancer patients, respectively. Briefly, 77.5% (55/71) of patients were homozygous for th
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G protein coupled receptor kinases GRKs are another group of
2021-11-12
G protein-coupled receptor kinases (GRKs) are another group of kinases whose limited substrate repertoire is associated with an extensive binding interface. GRKs phosphorylate activated G protein-coupled receptors (GPCRs) at multiple sites, promoting binding of arrestin proteins to mediate receptor
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br For some time it was known that
2021-11-11
For some time, it was known that membrane-bound guanylate cyclases (GCs) of photoreceptor AZ505 in the retina respond to changes in the [Ca]. Lolley and Racz observed that synthesis of cyclic GMP (cGMP) was stimulated at only low [Ca], concluding that Ca has an inhibitory effect on the regulatio
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br Conflict of interest statement
2021-11-11
Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). Introduction G protein-coupled receptor 55 (GPR55) has emerg
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Human GPR hGPR was originally isolated
2021-11-11
Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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In summary we have designed and optimized
2021-11-11
In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstra
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br Conclusions In summary we
2021-11-11
Conclusions In summary, we have designed an ultrasensitive electrochemical assay for hOGG1 based on a ratiometric strategy and HCR assisted amplification. The hOGG1 can specifically identify 8-oxo G site on the DNA probes modified on the electrode surface. The subsequent cleavage reaction trigger
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Molecular dynamics studies have proved an effective means of
2021-11-11
Molecular dynamics studies have proved an effective means of characterising transition state pathways between the inward- and outward-facing states, and providing the relative propensity for each state. For example, long-timescale simulations of the membrane-embedded LeuT dimer, totalling ∼21 μs, ha
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br WM astrocytes Grey matter astrocytes express a
2021-11-11
WM astrocytes Grey matter astrocytes express a variety of GluR types that have both physiological and pathophysiological significance [87]. Non-NMDA GluR are also expressed in WM astrocytes [40], although the functionality of these receptors has not been tested. The fibrous astrocytes that popula
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A main finding of this study
2021-11-11
A main finding of this study was that the impact of exogenous insulin on hippocampal memory and glucose utilization was GluT4-dependent. Although insulin was administered directly to the hippocampus, it is important to point out that such administration does indeed have physiological relevance; that
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prescription Gastric inhibitory polypeptide a hormone belong
2021-11-11
Gastric inhibitory polypeptide, a hormone belonging to the glucagon-secretin family of peptides, exhibits protection against the neurodegeneration and also stimulates neurogenesis in adult rats in a paracrine manner (Gault and Holscher, 2008, Nyberg et al., 2005, Usdin et al., 1993). The expression
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