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br Material and methods br Results The
2022-03-16
Material and methods Results The search for proteins selectively expressed in pancreatic islet L-741,626 mg 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 i
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Firstly the impact on activity and selectivity was
2022-03-16
Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)
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Pregnancy per AI results at days post TAI tended to
2022-03-16
Pregnancy per AI results at 32 days post TAI tended to differ among GnRH products and was greater for FER and CYS than FAC according to the Tukey-grouping analysis statistical approach (Table 1). In addition, P/AI was greater for cows treated with gonadorelin diacetate products than for cows treated
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br GR Is a Transcriptional Activator How GR
2022-03-16
GR Is a Transcriptional Activator How GR activates some genes while repressing others remains unsettled after decades of study. While significant controversy exists regarding GR-mediated repression, a consensus model for transcriptional activation has emerged: GR activates transcription through s
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br Summary br Acknowledgement br GR A Nuclear Receptor with
2022-03-16
Summary Acknowledgement GR: A Nuclear Receptor with Widespread Physiological Impact GR, or NR3C1 (see Glossary), is a transcription factor (TF) that regulates gene expression in nearly every cell of the body. A member of the nuclear receptor (NR) superfamily, its ligand-binding domain confe
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For another the N terminal sequence of native glucagon is
2022-03-16
For another, the N-terminal sequence of native glucagon is highly conserved, and positions 8, 9, 16 and 18 are noteworthy in maintaining glucagon activity [18], [20], [21]. It also achieves a degree of selectivity from its C-terminal residues, and a significant contribution is made by the C-terminal
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Fig a and b illustrates a
2022-03-16
Fig. 3a and b illustrates a slow inhibition by PMA in 2 μM Ca2+. Moreover, channel inhibition was reversed by addition of PKC19–31, a peptide inhibitor specific for PKC, as shown in Fig. 3c. In three experiments, Im was reduced to 14.5±0.6% of the control value by PMA to increase to 207.6±73.6% by a
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In the course of our ongoing attempts to photolabel alloster
2022-03-16
In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric Pam3CSK4 synthesis type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise t
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In the course of our ongoing attempts to photolabel alloster
2022-03-16
In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric xmu type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise the process of t
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Another small compound targeting IBAT has been evaluated in
2022-03-16
Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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br Experimental Procedures Information on
2022-03-16
Experimental Procedures Information on the materials used in this study and the details of how the in vivo and in vitro assays were performed are provided in Supplemental Information. Acknowledgments This research was supported by the National Research Foundation of Korea (NRF) grant funded b
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The PK profile and tissue distribution of which
2022-03-16
The PK profile and tissue distribution of 30, which has biological properties almost equivalent to those of 12, were examined in comparison with 12. Analog 30 was evaluated in a 6 h rat PK study at an intravenous (iv) dosing of 1 mg/kg in 10% 2-hydroxypropyl--cyclodextrin (HP-β-CD) (Table 2) and an
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Glucose metabolic pathways are well defined but the
2022-03-15
Glucose metabolic pathways are well defined but the subcellular organization of these pathways is poorly understood in liver and kidney. Several factors affect the net flux of gluconeogenesis and allow the Paprotrain sale to respond to physiological changes [1]. Ovadi and Srere have suggested that a
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br Role of funding source br
2022-03-15
Role of funding source Conflict of interest Acknowledgements We thank F. Blaskovits and P. Kesner for technical assistance. This project was supported by operating grants from the Canadian Institutes of Health Research (CIHR) to X. Zhang (MOP123249) and the National Natural Science Foundati
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Experimental conditions may be critical to
2022-03-15
Experimental conditions may be critical to explain one model or the other. The matter of Hippo-driven cytoplasmic sequestration (Varelas et al., 2008) of active SMAD complexes (Varelas et al., 2008) vs. TßR basolateral relocalization upon epithelial polarization (Nallet-Staub et al., 2015) as mechan
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