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Two excellent GSMs with clear
2021-10-02
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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br Medium to long chain fatty acids Medium to long
2021-10-01
Medium- to long-chain fatty acids Medium- to long-chain fatty acids impart a wide range of physiological effects. Medium-chain and long-chain fatty acids have 6–12 carbons and >12 carbons, respectively. As the energy source, these fatty acids are supplied primarily by food intake, biosynthesis, a
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Recently they reported an enyne
2021-10-01
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral Adenine sulfate (tmax=15min) and a decent pharmacokinetic profile
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DLS only provides a Z average size
2021-10-01
DLS only provides a Z-average size based on spherical model, hence the size of nanorods was determined as 300 nm by DLS measurement. However, the size of length is nearly 400 nm while width is about 100 nm, which was clearly observed by transmission electron microscopy (TEM) (D). Meanwhile, the TEM
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Initial evidence that cell contact
2021-10-01
Initial evidence that cell-contact-mediated transmission of HIV-1 is relevant for the generation of latently infected SP 600125 mg was suggested in the context of transmission from dendritic cells to resting CD4+ T cells (Evans et al., 2013, Kumar et al., 2015). As dendritic cells probe for antigen
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fty720 receptor Although we showed that RBL
2021-10-01
Although we showed that RBL-2H3 Sc98 fty720 receptor took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, includin
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br Acknowledgments br Introduction Postmenopausal osteoporos
2021-10-01
Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by chemical m receptor deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approximate
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Recently unimolecular multi functional peptides that combine
2021-10-01
Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with prostaglandin e2 and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and
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br To explore further the
2021-09-30
To explore further the functional impact of the similarity of the UTY and KDM6A proteins, the FANTOM5 human dataset was analysed to determine whether or not the genes were expressed at the same time in the same tissues (which would suggest that they are controlled by the same regulators) or with o
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Acknowledgement This work was supported
2021-09-30
Acknowledgement This work was supported by grants from the National Natural Science Foundation of China (No.81802749), Shenzhen Healthcare Research Project (No.SZBC2017029), the Science and Technology Foundation of Shenzhen (JCYJ20170412155231633, JSGG20170414104216477), National Key Research and D
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br Hedgehog pathway The Hedgehog pathway Fig derives
2021-09-30
Hedgehog pathway The Hedgehog pathway (Fig. 1) derives its name from Hh gene mutant Drosophila, which presents a spiked phenotype resembling the animal “hedgehog” [13]. The Hh proteins control embryonic development in vertebrates, where the signaling mechanisms mediated by the proteins are multip
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In the course of studies leading to the discovery
2021-09-30
In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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Here we report the genomic structure and the phylogenetic
2021-09-30
Here we report the genomic structure and the phylogenetic analysis of testis-specific Ser/Thr kinase haspin gene. Materials and methods Results Discussion The isolation and analysis of haspin genomic DNA showed that haspin was an intron-less gene and localized in an intron of integrin αM29
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Efficiency of methylated process was assessed by calculating
2021-09-30
Efficiency of methylated process was assessed by calculating PMI and SMI. On average, PMI was 0.9 and ranged from 0.1 to 3.8 while SMI was 4.9 and ranged from 0.3 to 21.3. The observed differences in the arsenic methylation can be associated with the inter-individual variations caused by a genetic p
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Finally our data found that
2021-09-30
Finally, our data found that the EBV dUTPase protein modulates tryptophan, serotonin, and DA metabolism and use in vitro and in vivo. The EBV dUTPase may alter kynurenine catabolism in microglia in vitro, suggesting that there is an increase synthesis of quinolinic acid. Quinolinic acid, an agonist
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