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br G protein coupled receptor GPR also known as
2022-01-27

G-protein coupled receptor 40 (GPR40), also known as a free fatty Atglistatin receptor, is dominantly expressed in pancreatic β cells and intestine K, L cells., . Besides, GPR40 is also reported to be expressed in brain, but its function is still unknown. It is well documented that GPR40 agonist
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In the course of studies leading to the discovery of
2022-01-27

In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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Our study has strengths and limitations
2022-01-27

Our study has strengths and limitations. We believe we are the 1st to report a novel model of secondary hypogonadism. Several animal models for hypogonadotropic hypogonadism (kisspeptin and the kisspeptin receptor knockout) exist but we are unaware of animal models of secondary hypogonadism with di
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Type diabetes mellitus T DM causes vascular complications an
2022-01-27

Type 2 LY-411575 (T2DM) causes vascular complications and is a major public health problem associated with lifestyle diseases such as obesity, liver steatosis, hypertension, and so on. Although serum lactate is reportedly elevated in diabetic patients [12], [13], the physiological effects remain unc
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The discovery that the physiological functions of
2022-01-27

The discovery that the physiological functions of LPI are associated with the activation of specific GPR55 membrane receptor [4] has launched a new era of research on this lysophospholipid. However, the activation of membrane receptors by lysophospholipids is extremely complex due to the multitude o
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Based on the results of compound appeared to have the
2022-01-27

Based on the results of , LY83583 appeared to have the best overall profile, so our efforts were then devoted to using 5-(-propyl)pyrimidine as the right-hand nitrogen attachment to optimize the R group of (). Analog was synthesized using the reaction conditions from , while analogs and were s
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Conjugated BAs via S PR also activate
2022-01-27

Conjugated BAs via S1PR2 also activate ERK1/2- and AKT-signaling pathways leading to the growth and invasion of cholangiocarcinoma cells. The role of conjugated BAs via S1PR2 to regulate apoptosis or cancer progression remains to be dissected. Nevertheless, there is no doubt that the composition of
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While NR upregulation in the spinal cord is known
2022-01-27

While NR1 upregulation in the spinal cord is known to contribute to pathological pain [7], [22] and furthermore, NR1 expression in the spinal cord has been shown to be reduced by continuous administration of the GlyT1-inhibitor ALX5407 [23], little is known about possible expressional changes of NR1
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Hesperidin is an abundant and inexpensive
2022-01-27

Hesperidin is an abundant and inexpensive plant flavonoid, largely derived from citrus species including sweet orange and lemon. Hesperetin (Hst) is the aglycone of hesperidin. Hesperidin and hesperetin have been reported to show a battery of pharmacological properties, including anti-hyperlipidemic
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br Materials and methods E
2022-01-27

Materials and methods E. coli strains. Strains of E. coli with mutations in the lacZ gene for β-galactosidase [5] and a derivative with a knock-out mutation of the chromosomal gene for FPG produced with P1vir [6] were obtained from H. Schellhorn (McMaster Univ., Hamilton, Ontario, Canada). Growth
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The amino hydroxy methyl isoxazolepropionic acid AMPA recept
2022-01-27

The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic Cell Cycle Compound Library mg (AMPA) receptors are related ionotropic glutamate receptors (iGluRs) that mediate fast excitatory neurotransmission, and are also typically heteromeric ion channels, composed of GluA2 subunits in conjugation with GluA
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Here we studied GLUT targeted
2022-01-26

Here, we studied GLUT1-targeted nanomedicines as a new strategy directed to overcome vascular barrier, enhancing delivery and efficacy in solid tumors. These nanomedicines were prepared by controlled installation of glucose on polymeric micelles incorporating the antitumor agent cisplatin, which is
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In Solloway and colleagues reported that mice with alpha cel
2022-01-26

In 2015, Solloway and colleagues reported that mice with alpha cell hyperplasia due to inactive hepatic glucagon receptor signaling may most likely be caused by amino 95 9 dependent mechanisms [11]. The authors then showed these adaptations are regulated by ‘mechanistic target of rapamycin’ (mTOR)-
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Dynorphin (2-17), amide, porcine australia Importantly the l
2022-01-26

Importantly, the levels of the pro-inflammatory cytokines TNF-α and IL-1β and Nf-κB, a key transcription factor in chronic inflammatory responses that is activated by pro-inflammatory cytokines, were also reduced by the drugs, confirming our previous results that demonstrated anti-inflammatory effec
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The mechanism by which Piezo
2022-01-26

The mechanism by which Piezo1 acts in the regulation of RBC volume is not firmly established. Its curved structure implies that it is activated by an increase in membrane tension (11), a mechanism indicated by electrophysiological measurements (16). However, the RBC membrane mechanics at its physiol
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