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br Histamine and glycaemia Histamine is involved
2022-06-02

Histamine and glycaemia Histamine is involved in a wide variety of pathophysiological events mostly related to the inflammatory response through four receptors, namely H1-4Rs. The first studies of AVL-292 and diabetes date back to the 1950s. Since that time the involvement of histamine in diabet
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The exact mechanism by which mitochondrial hexokinases such
2022-06-02

The exact mechanism by which mitochondrial hexokinases such as HK1 and HK2 prevent apoptosis is unclear. Mitochondrial hexokinases have been shown to bind with the voltage-dependent anion channel 1 (VDAC1), giving them direct access to ATP for use as an energy source [36]. Akt has been shown to prom
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In the same research group released
2022-06-02

In 2017, the same research group released a free internet accessible database (HemeOxDB, http://www.researchdsf.unict.it/hemeoxdb), to make it easier the analysis of the literature and, consequently, the design of potent and selective HO-1 inhibitors. The database reported the entire set of HO-1 and
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Initial structural and biochemical work showed
2022-06-02

Initial structural and biochemical work showed that Get3 forms an obligate dimer whose conformation is regulated by the bound nucleotide. Analogous to SRP and SR, Get3 contains a P-loop nucleotide hydrolase domain in which the bound ATPs face one another at the dimer interface (Figure 3A, top right
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Here we investigate the structural and
2022-06-02

Here we investigate the structural and biochemical properties of the N-GTPase domain of p190RhoGAP-A. We determine the crystal structure and find that N-GTPase adopts an extended GTPase-like fold with six unique inserts that seem to preclude its ability to bind typical GAP, GEF, or Riociguat molecu
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Two different genes encode GSK
2022-06-02

Two different genes encode GSK-3 isoforms α and β that have very similar catalytic domains but significantly differ in their N- and C-termini. The α and β isoforms split from a common precursor approximately at the emergence of vertebrates, suggesting that at least one of the isoforms took on a new
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GPR co localizes with ghrelin in the duodenum
2022-06-02

GPR120 co-localizes with ghrelin in the duodenum [17], α-gustducin in the small intestine and type II taste bud cells 18, 19, neuropeptide Y centrally in the arcuate nucleus [20] and glucagon-like peptide 1 (GLP-1) in the colon and circumvallate papillae taste bud cells 6, 21, 22. Interestingly GPR1
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Ponceau S Staining Solution br Conclusion In summary a serie
2022-06-01

Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic Ponceau S Staining Solution motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist p
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In vitro studies have shown that some antidepressant
2022-06-01

In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found th
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br Introduction As is now
2022-06-01

Introduction As is now well known, obesity is major risk factor for various diseases such as nonalcoholic fatty liver disease, cardiovascular disease, some cancers (McWilliams and Petersen, 2009), type-2 diabetes mellitus (Jakobsen et al., 2007), and hypertension (Aneja et al., 2004), among other
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br Acknowledgements br Introduction Glucagon
2022-06-01

Acknowledgements Introduction Glucagon, a 29-amino Anastrozole peptide, is released from the pancreatic islets, intestine and stomach. Glucagon is released under hypoglycemic conditions and then elevates blood glucose levels, serving as a major counter hormone [1]. The regulation of glucose m
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br Acknowledgments We would like to acknowledge Jenna Hall M
2022-06-01

Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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More recently Dal Peraro and coworkers carried out s CG
2022-06-01

More recently, Dal Peraro and coworkers [38] carried out 4 μs CG MD simulations of GS with six randomly placed C9915-55 peptides embedded into a synaptic plasma bilayer model. This lipid raft model was constituted by 32 different equol receptor and cholesterol (54.74%). In this study, the authors o
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Two types of processes intrinsic and extrinsic
2022-06-01

Two types of processes, intrinsic and extrinsic, contribute synergistically to the age-related change on structural integrity and physiological function of the skin (Farage, Miller, Elsner, & Maibach, 2008). Intrinsic aging arise from genetically programmed cell aging, normal metabolic activities, a
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We tested formyl MYVKWPWYVWL which we had previously shown
2022-06-01

We tested formyl-MYVKWPWYVWL, which we had previously shown to have essentially identical Kis for W190/N192, R190/K192 and R190/N190 [8] of 130 nM, for its ability to downregulate surface receptor (Fig. 5A). R190/K192 exhibited the lowest EC50 of 44±4 nM about 3 fold below the observed Ki and a maxi
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