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In an RNAi screen to interrogate
2021-09-28

In an RNAi screen to interrogate the function of transmembrane proteins in ISCs/EBs, we identified the SJ protein tetraspanin 2A (Tsp2A) as a tumor suppressor. Further characterization reveals that Tsp2A expression initiates in ISCs and Tsp2A protein assembles at the SJs in the progenitor Statistica
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RG-108 We are pursuing a hit to
2021-09-28

We are pursuing a hit-to-lead medicinal chemistry campaign to optimize inhibitors of the HBV RNaseH. Here, we report the activity of seven new HIDs and nine new HPDs, with significant improvements in in vitro potency and cytotoxicity profiles for the HPD compounds. Materials and methods Result
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br Other mechanisms In vitamin B
2021-09-28

Other mechanisms In vitamin B6 deficiency, antibody production may be indirectly impaired [38]. Grindley et al. [4] showed that high dietary intake of vitamin B6 (74.3 mg PN/kg diet) suppresses herpes simplex virus type 2 transformed cell-induced tumor growth and enhances immune status compared w
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Pharmacologic approaches of inhibiting GSNOR activity have r
2021-09-28

Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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Several studies have found that GPR
2021-09-28

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected E3330 synthesis expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR14171
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br GnRH receptor expression is altered within
2021-09-28

GnRH receptor expression is altered within GnRH neuronal cells Kisspeptin failed to stimulate GnRH expression in our line of GT1-7 cells. Instead, we have found that kisspeptin increased the expression of the GnRH receptor in these Hypotaurine (Sukhbaatar et al., 2013). Based on the results of e
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The soluble receptor for advanced
2021-09-28

The soluble receptor for advanced glycation end products has been already studied in physiological and pathological pregnancy. In accordance to our previous studies we showed increased sRAGE serum levels in women with threatening premature labor [15] and we described a negative correlation of sRAGE
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br Conclusions We have shown that
2021-09-28

Conclusions We have shown that despite the development of severe insulin intolerance and marked alterations in whole body substrate oxidation that Gcgr−/− mice are protected against olanzapine-induced hyperglycemia. Our data provides evidence that this protective effect is likely due in large par
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Whether or not SMO and SMO dependent HH signaling play
2021-09-28

Whether or not SMO and SMO-dependent HH signaling play a role in hematopoiesis is a subject of strong controversy. Obviously, the effects of SMO deletion are highly contextual and dependent on the timing of deletion. transplanted murine Smo−/− fetal liver apomorphine into sublethally irradiated mice
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br Clinical trials testing GLP mimetics in
2021-09-28

Clinical trials testing GLP-1 mimetics in AD or PD patients GIP analogues show good neuroprotective effects in animal models of AD and PD Glucose-dependent insulinotropic polypeptide (GIP) is a 42-amino SEW 2871 incretin growth factor which activates pancreatic islets to enhance insulin secre
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It was recently reported that aged GHSR mice
2021-09-28

It was recently reported that aged GHSR−/− mice, in addition to showing alterations in meal pattern microstructure, exhibit NPY and AgRP mRNA upregulation in the ARC [56]. After an overnight fast, our animals exhibited a similar pattern of upregulated NPY and AgRP mRNA expression. Given that GHSR1a
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br Acknowledgements Research was funded
2021-09-27

Acknowledgements Research was funded by the Natural Sciences and Engineering Council of Canada (NSERC) (Grant #210290) SGF. The funding body played no role in the design or execution of the study. The authors declare no conflict of interest. Introduction HBO2 therapy is the use of 100% oxygen
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br G protein coupled receptor GPR also known
2021-09-27

G-protein coupled receptor 40 (GPR40), also known as a free fatty natural product libraries 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 G
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A new series of pyrimidones with C and C modifications
2021-09-27

A new series of pyrimidones (14) with C-7 and C-9 modifications were furnished consisting of a hydroxypyridinone and a thiazole ring and checked against raltegravir resistant HIV mutant strains to determine their in vitro anti-HIV IN potency. Compounds 14a–14a, 14b–14b and 14c–14c appeared with 6.4
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The overall response rate to
2021-09-27

The 13% overall response rate to afatinib is comparable to a 19% response rate reported by Peters et al. [20] in a separate retrospective series investigating the use of afatinib in more heavily pretreated patients with HER2-mutant lung adenocarcinomas. Our 13% response rate is also comparable to an
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