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We also explored various nitrogen substituents with an
2022-05-07

We also explored various nitrogen substituents with an aim toward modulating sterics and basicity within the ABH series. No glycine uptake inhibition was detected with non-basic bicycles (data not shown). Isopropyl was the best compromise between desired on-target effect and clearance, however, eff
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Due to the therapeutic potential of GlyT inhibitors numerous
2022-05-07

Due to the therapeutic potential of GlyT1 inhibitors, numerous drug screening campaigns have been started - and are still going on - which aimed at the identification of compounds with biological activity at or affinity for this drug target. For characterization of biological activity at GlyT1, tran
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The differentially expressed proteins during somatic embryog
2022-05-07

The differentially expressed proteins during somatic embryogenesis are described as the proteins that are induced by oxidative stress and respond to higher cell division activity including ascorbate peroxidase, dehydroascorbate reductase, glutathione transferase and mitochondrial manganese superoxid
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Medroxyprogesterone acetate br Introduction Glycoproteins re
2022-05-07

Introduction Glycoproteins represent a staggeringly small fraction of proteins analyzed by high-resolution techniques despite high concentrations at the cell surface and critical roles in many human diseases. Though one-half or more of all human proteins are predicted to contain a carbohydrate ch
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ru listings mg br Vesicular glutamate transporters VGLUTs br
2022-05-07

Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,
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The transporter was successfully expressed
2022-05-07

The transporter was successfully expressed in MSCs and HEK 293 cells. In both cell types, the expression of YFP-EAAT2 was confirmed by immunological staining and flow cytometry. The functionality of the transporter was determined by [3H]glutamate uptake assays, and the blood glutamate-grabbing activ
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br Sodium glucose co transporter inhibitors SGLT
2022-05-07

Sodium-glucose co-transporter-2 inhibitors (SGLT2i) are the latest class of non-insulin glucose-lowering agents that facilitate glycaemic control by inhibiting renal glucose reabsorption, thus promoting glycosuria. Canagliflozin, dapagliflozin, and empagliflozin are the three commonly used agents
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br Acknowledgements This work was supported by the National
2022-05-07

Acknowledgements This work was supported by the National Institutes of Health [grant number GM024417]. Introduction In mammals, glucose is the major energy substrate supporting conceptus development after rad51 formation [1,2]. While the equine morula uses similar amounts of pyruvate and glu
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br Xenobiotics and the Glucocorticoid Receptor br Conclusion
2022-05-07

Xenobiotics and the Glucocorticoid Receptor Conclusion Transparency document Acknowledgements The author wishes to thank Professor Wilhelm Engström from the Swedish University of Agricultural Sciences (Department of Biomedical Sciences and Veterinary Public Health) for his proof reading
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br Regulation of the GLI code
2022-05-07

Regulation of the GLI code by non-HH signals and by the oncogenic load The GLI code may be seen as the essential parameter to regulate canonical HH output. Its regulation first appeared to be strictly dependent on the presence of specific levels of HH ligands. Indeed, GLI1 transcription is so far
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etomoxir receptor To directly address whether pharmacologica
2022-05-07

To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N
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In summary the SAR of a series of phenylpropanoic
2022-05-07

In summary, the SAR of a series of phenylpropanoic acid-free fatty 4-IPP receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust efficacy
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Introduction Osteoclasts are large multinuclear cells that a
2022-05-07

Introduction Osteoclasts are large, multinuclear Famprofazone that are responsible for the resorption (breakdown) of bone [1]. Together with osteoblasts, the bone forming cell, they maintain the integrity of the skeleton through constant resorption and repair of bone. Osteoclast precursors of mono
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Disuflo Cy5 azide In addition to removing proteins and
2022-05-07

In addition to removing proteins and organelles related to iron and lipid metabolism, an alternative mechanism by which autophagy promotes ferroptosis is through the formation of the BECN1-solute carrier family 7 member 11 (SLC7A11) complex [42,43]. SLC7A11 is the main component of the antiporter sy
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Sumoylation is involved in regulating protein protein intera
2022-05-07

Sumoylation is involved in regulating protein-protein interactions, subcellular protein localization, protein stability, and transcriptional factor activity (reviewed in [29]). The small ubiquitin-like modifier (SUMO) protein is covalently attached to a lysine residue in a Ψ-K-X-D/E consensus sequen
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