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br Cholecystokinin CCK CCK is secreted
2022-05-06
Cholecystokinin (CCK) CCK is secreted by enteroendocrine I-cells of the duodenum and jejunum in response to amino acids and lipids [14]. There are two forms of the CCK receptor, CCK1 which is expressed on pancreatic α- and β-cells while CCK2 is located on somatostatin-secreting δ-cells [8]. CCK r
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Notably Cu labeled dimeric exendin subunit which was designa
2022-05-06
Notably, 64Cu-labeled dimeric exendin-4 subunit, which was designated as 64Cu-Mal2Sar-(exendin-4)2, showed higher tumor uptake than that of the monomeric exendin-4 subunit [245]. Besides the most commonly-used GLP-1R agonists exendin-3 and -4 and their derivatives, exendin (9-39) exhibits strong bin
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Acknowledgments Financial support from the National Natural
2022-05-06
Acknowledgments Financial support from the National Natural Science Foundation of China (81730094, 81473262 and 81573299) is gratefully acknowledged. This project was also supported by the “111 Project” from the Ministry of Education of China, the State Administration of Foreign Expert Affairs of C
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Thus synthesized thienopyrimidine derivatives were evaluated
2022-05-06
Thus synthesized thienopyrimidine derivatives were evaluated in vitro for GPR119 agonistic activity, and the results are summarized in , , . First, we fixed the 4-methylsulfonylphenyl substituent at the R position on the thienopyrimidine ring, and derivatized at the R position. As shown in , and sho
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Similar to GPR A activation of G protein coupled
2022-05-06
Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic CGP 42112 receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 2008, Gold et al., 1963, Houg
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mt t Gp induces cell death by apoptotic mechanisms and incre
2022-05-06
Gp120 induces cell death by apoptotic mechanisms and increases intracellular Ca, and activates messengers related to cell death. Intracellular mechanisms of neuronal damage are mainly a consequence of the activation of the N-methyl-d-aspartate receptor (NMDAR) [2], [5], which induces excitotoxicity
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Structural analysis of the MD
2022-05-06
Structural analysis of the MD-open state unveils that the transmembrane domain features a symmetric organization of the pore-lining helices M2 similar to the semi-open structure but with a local asymmetry at the constriction point, which is critical for chloride permeation. The atomistic simulations
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br Hedgehog HH signaling plays an important role
2022-05-05
Hedgehog (HH) signaling plays an important role both during embryonic development and adult life. It is involved in the regulation of cell differentiation, cell proliferation and tissue polarity, as well as in the maintenance of stem cells, tissue repair, and regeneration (, ). Three ligands, Indi
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In terms of stimulation oxytocin
2022-05-05
In terms of stimulation, oxytocin, dopamine, noradrenaline, adrenaline and glucagon have all been reported to increase ghrelin secretion (Mundinger et al., 2006, Iwakura et al., 2011, de la Cour et al., 2007, Gagnon and Anini, 2013). Stimulatory effects on ghrelin secretion have also been observed w
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When tested in dog at mg kg showed a reduction
2022-05-05
When tested in dog at 20mg/kg, showed a reduction of 56% of Aβ42 in the cerebrospinal fluid (CSF) 8h post doing, comparable to that of (see ). Upon evaluation of E-64 mg in a one week repeated dose study in dog, at 10 and 20mg/kg/day, no increase in liver enzyme levels (ALT or AST) was observed.
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Structurally the termini of FGF are critical for
2022-05-05
Structurally, the termini of FGF21 are critical for effective signaling. Progressive amino myosin truncation at either end of the protein sequentially impairs FGF21 bioactivity, but via different mechanisms. Shortening at the N-terminus weakens its ability to activate the FGFR/KLB-complex but does
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br Materials and methods br Results The immunoblot analysis
2022-05-05
Materials and methods Results The immunoblot analysis demonstrated the presence of similar immunoreactivity by liver FBPase in hepatic and renal extracts. These results indicate that FBPase is present in a similar amount in both tissues. Moreover, the analysis revealed that the antibody detect
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Sirolimus rapamycin and everolimus both of
2022-05-05
Sirolimus (rapamycin) and everolimus, both of which are mTOR inhibitors, are released by commonly used first- and second-generation DES. Considering the relatively high rates of the target vessel failure with currently available DES [12,14,16,45,46], there is a need for a novel drug strategy that p
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br Introduction Migraine is a chronic neurological disorder
2022-05-05
Introduction Migraine is a chronic neurological disorder characterized by recurrent episodes of headache. It affects more than 10% of the population worldwide, resulting in a staggering amount of episodic disability, a substantial decrease in the quality of life and a concomitant loss in producti
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FXa is a vitamin K dependent serine protease consisting of
2022-05-05
FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 c-Myc Peptide australia and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure
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