• GPR agonistic activity was evaluated

  2021-11-26

  

  GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin

• NECA In Solloway and colleagues reported that

  2021-11-25

  

  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 NECA dependent mechanisms [11]. The authors then showed these adaptations are regulated by ‘mechanistic target of rapamycin’ (mTOR)-d

• For many plasma membrane receptors including

  2021-11-25

  

  For many plasma membrane receptors including GPCRs, their density on the cell-surface is finely controlled by various transcriptional, post-transcriptional and post-translational mechanisms, and is often a determinant of overall receptor function in a cell. To date, the transcriptional regulation an

• Introduction Osteoarthritis OA is a prevalent

  2021-11-25

  

  Introduction Osteoarthritis (OA) is a prevalent disease characterized by chronic joint degeneration, including articular cartilage loss, synovitis and osteophyte formation [1], [2], [3], [4], [5]. The cause of OA is metabolic imbalance and mechanical stress, which is coupled with inflammation, lead

• The absence of differences between GalR knockout and wild ty

  2021-11-25

  

  The absence of differences between GalR1 knockout and wild type mice in kainic acid-induced seizures suggests that GalR1 do not interfere with the seizure-inducing action of kainic acid. Postsynaptic kainate receptors are excitatory ionotropic glutamate receptors and their activation leads to seizur

• Andexanet alfa works as a decoy for the FXa inhibitor

  2021-11-25

  

  Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic

• br Sources of funding This work was supported by grants

  2021-11-25

  

  Sources of funding This work was supported by grants from the Canadian Institutes of Health Research (CIHR) (No. MOP-111096) and from the Heart and Stroke Foundation of Canada awarded to Dr. Danielle Jacques. Disclosures Acknowledgments Introduction A large number of epidemiological, hu

• Histamine H and H receptor expression

  2021-11-25

  

  Histamine H2 and H3 receptor expression is altered in the sitagliptin phosphate of Hdc mice (Chepkova et al, 2012, Fitzsimons and et al, 2001). Because these mice lack HA, expression of HA receptors might be thought to be irrelevant. This is not the case in Hdc heterozygotes, however, or in patients

• br Conclusion br Conflict of interest Please

  2021-11-25

  

  Conclusion Conflict of interest Please refer to the accompanying ICMJE disclosure forms for further details. Exotic species such as hedgehogs are becoming popular companion animals. Therefore, they are more commonly seen in veterinary clinics. Acariasis is fairly common in these animals, us

• Other N substituted carboxamide oxy pyridine

  2021-11-25

  

  Other N-substituted-6-carboxamide-3-oxy-pyridine derivatives 52a, 52h, 52i, and 53h were synthesized using an alternative route. The Pd-catalyzed Heck aminocarbonylation of 44 or 45 with (PPh3)2PdCl2 catalyst in the presence of Et3N under CO atmosphere successfully provided various N-substituted-6-c

• Importantly lactate and H exert some

  2021-11-24

  

  Importantly, lactate and H+ exert some of their biological effects independently of each other, though sometimes through redundant pathways leading to a same biological effect, as for angiogenesis. In other cases, they can have antagonist effects: lactate was shown to stimulate extracellular matrix

• br Materials and methods br Conflicts of interest Some

  2021-11-24

  

  Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He

• This excellent tolerability is especially interesting

  2021-11-24

  

  This excellent tolerability is especially interesting in the light of the fact that intravenous administration of liposomal ponatinib was predicted to yield much higher plasma concentrations as compared to the orally administered free drug. In addition, liposomal drug dose in absolute numbers was te

• br What are the local exocytotic protein targets of PKC

  2021-11-24

  

  What are the local exocytotic protein targets of PKC? A direct method for PKC to potentiate insulin release would be to phosphorylate and activate components of the exocytotic machinery. Bulk measurements show that potentiation occurs by enhancement of the calcium sensitivity of exocytosis [56],

• In the Joint United Nations Program on HIV AIDS

  2021-11-24

  

  In 2015, the Joint United Nations Program on HIV/AIDS (UNAIDS) proposed that by 2020, 90% of people living with HIV should be aware of their HIV status, as the first part of 90-90-90 strategy to end AIDS epidemic. Early detection of HIV allows initiating care for proper treatment, which impacts in m

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