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Based on work from our labs with mGlu NAMs
2022-05-04
Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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An alternative to the chemoenzymatic preparation
2022-05-04
An alternative to the chemoenzymatic preparation of glycoproteins is the production through total chemical synthesis or semi-synthesis [2,3,]. Many successful glycoprotein syntheses are based on native chemical ligation (NCL) [11], a reaction where unprotected peptides and glycopeptides of any leng
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To maintain low Glu concentrations in the synaptic cleft bel
2022-05-04
To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino Y27632 is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, and in to
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br NMDA receptor LBDs The study
2022-05-04
NMDA receptor LBDs The study of GluA2 was later expanded to include NMDA receptors [22]. NMDA receptors are obligate heterotetramers that are composed of two glutamate-binding subunits and two glycine-, or d-serine-, binding subunits. In this study, crystal structures of the NMDA receptor glycine
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Several studies have shown that regulation of glutamate home
2022-05-04
Several studies have shown that regulation of glutamate homeostasis is critical in relapse to many drugs of abuse [84,85]. Glutamate is transported by GLT-1, which accounted for about 90% of glutamate clearance from the synaptic cleft [14,15]. CEF is known to produce its effects through GLT-1 upregu
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br Conclusions br Acknowledgements br Introduction Glucose m
2022-05-04
Conclusions Acknowledgements Introduction Glucose metabolism is vital to prepare uterine epithelium and stroma for embryo implantation and for the differentiation of the functionalis layer to support the developing conceptus [[1], [2], [3], [4]]. Due to its polar nature and hydrophilic cond
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LbGlcK and the HsHxKIV d glucose complex PDB
2022-05-04
LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key SGC-CBP30 mg binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, such as K16
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GLP and glucose dependent insulinotropic peptide GIP are
2022-05-04
GLP-1 and glucose-dependent insulinotropic peptide (GIP) are gut hormones secreted from intestinal L 1 98 and K cells, respectively. Together, these hormones account for the vast majority of the incretin effect, the enhanced postprandial insulin secretion observed in healthy adults (Dupre et al., 1
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Another key component of proper DA cell physiology
2022-05-04
Another key component of proper DA cell physiology is the basal firing activity of SN DA neurons, which maintains extracellular levels of dopamine in the dorsal striatum that are essential for voluntary movement [106]. Changes in SN DA neuron activity directly impacts the amount of dopamine released
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br Presenilins in protein trafficking
2022-05-04
Presenilins in protein trafficking, proteolysis and degradation An obvious explanation for the role of presenilins and γ-secretase in protein trafficking and degradation is that many reported γ-secretase substrates are functionally involved in protein transport. For example, members of the mammal
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Pattern recognition receptors key elements in the innate
2022-05-04
Pattern recognition receptors - key elements in the innate immune response Every day, human beings are exposed to a broad range of microbes and foreign substances. Most of them are entirely harmless, however, some are pathogenic and have the potential to cause severe harm. The distinction between
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Glucose induced nuclear translocation of several enzymes inc
2022-04-29
Glucose-induced nuclear translocation of several enzymes, including GK, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), muscle GS, aldolase, lactate dehydrogenase (LDH) and phosphoglycerate kinase (PGK) is a well-known phenomenon. Additional functions have been proposed for these enzymes in the nu
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(R)-baclofen receptor br Cellular transportation of nanopart
2022-04-29
Cellular transportation of nanoparticles and nanocomplexes Endocytosis and exocytosis are critically important phenomena in cellular metabolism, which involve the complex vesicular system. They deal with major cellular transportation activities including membrane homeostasis by transporting prote
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Liposomes that are less than nm in diameter
2022-04-29
Liposomes that are less than 200nm in diameter are necessary to optimize uptake of liposomes by PLX-4720 (Oesterling et al., 2014). The liposomes constructed in these experiments were found to be sufficiently small in diameter for use in in vivo and in vitro experiments. Even smaller diameters are a
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Myelination by oligodendrocytes is required
2022-04-29
Myelination by oligodendrocytes is required for saltatory nerve impulse conduction and proper CNS function (Bercury and Macklin, 2015). Defects in myelination and remyelination impair saltatory nerve conduction and functional connectivity leading to cognitive, behavioral, and motor deficits in neuro
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