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With the exception of R none of the other
2022-03-21

With the exception of R5.40310, none of the other residues would appear to be in a position to mediate direct agonist interactions in the active state GLP-1R structures. ECL2 within the GLP-1R is important for affinity and efficacy of both extended and processed GLP-1 peptides [24]. Though distal fr
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br Materials and methods br
2022-03-21

Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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The extensive worldwide research efforts
2022-03-21

The extensive worldwide research efforts in the decade following FFA1 de-orphaning aimed at developing clinically useful FFA1 agonists were nearly halted after Takeda’s first-in-class agent fasiglifam (TAK-875) was discontinued in phase III of human trials. On the date of submission of this manuscri
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The canonical tumor suppressor p has also been
2022-03-18

The canonical tumor suppressor p53 has also been implicated as a transcriptional mediator of ferroptotic death (Jiang et al., 2015, Tarangelo et al., 2018, Wang et al., 2016, Xie et al., 2017). Specifically, p53 negatively regulates transcription of SLC7A11, the cystine-glutamate antiporter (Xc-) (J
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Remarkably most of these molecules are also quite effective
2022-03-18

Remarkably, most of these molecules are also quite effective in interfering with the proliferation of the drug-resistant cancer cell lines, with IC50 values ranging from 0.59 to 2.93 μM against MCF-7/ADR cells, and from 0.160 to 1.17 μM against NSCLC-resistant H1975 cells. Among these molecules, com
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Two recently developed highly specific EZH enzymatic inhibit
2022-03-18

Two recently developed, highly specific EZH2 enzymatic inhibitors, GSK126 and EPZ-6438, are currently in clinical trials for treating lymphomas (Kim and Roberts, 2016). Although these EZH2 inhibitors have shown antitumor effects in lymphoma cells with enzyme-activating mutations of EZH2 (Knutson et
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br Discussion In our study the prevalence of severe
2022-03-18

Discussion In our study the prevalence of severe periodontitis in patients with HIV infection was 66%, almost twice as high as in uninfected controls. Our results are in line with the prevalence of severe periodontitis found in HIV-infected patients in London, United Kingdom in the pre-cART era:
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The analytical approach for the simultaneous determination
2022-03-18

The analytical approach for the simultaneous determination of HA and its metabolites is complex. There are commercial kits that allow the determination of HA through ELISA and of its metabolites through radioimmunoassay (RIA) techniques. However, these immunological-based techniques do not allow sim
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MST are involved in signalling pathways following along the
2022-03-18

MST1/2 are involved in signalling pathways following along the canonical and noncanonical Hippo pathway. The canonical pathway is highly conserved between D. melanogaster and mammals and a master regulator of tissue growth. During development and within the canonical pathway, MST1/2 seem to have red
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mt t As indicated by the wide variety of pharmaceuticals for
2022-03-18

As indicated by the wide variety of pharmaceuticals for IOP management (Table 1), each case of glaucoma is unique and requires a unique treatment regimen to effectively lower IOP. This often results in patients utilizing several medications at once and/or combining medications with surgical interven
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Both plant hormones and some second
2022-03-18

Both plant hormones and some second messengers are involved in Fe-deficiency-related responses in plants (Kobayashi and Nishizawa, 2012). Among these second messengers, nitric oxide (NO) accumulation was induced by Fe deficiencies in tomato and Arabidopsis roots, and it acts as the downstream signal
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br Materials and methods br
2022-03-18

Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 Calyculin A mg has been identified within discrete regions of the ne
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br Funding This work was
2022-03-18

Funding This work was supported by the Deutsche Forschungsgemeinschaft (SFB766 and GRK1708). Conflict of interest Acknowledgements Introduction Hepatitis C virus (HCV) infection is a global problem affecting about 3% of the world’s population [1], [2]. Mother-to-child transmission of HC
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The dramatic increase in the development of
2022-03-18

The dramatic increase in the development of EAAT inhibitors and substrates over the last several years can likely be attributed to a number of experimental advances. Firstly, the isolation of the individual EAAT clones allowed each subtype to be selectively examined in well-characterized expression
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Hippo signaling is an emerging tumor suppressor pathway that
2022-03-18

Hippo signaling is an emerging tumor suppressor pathway that plays key roles in normal physiology and tumorigenesis through the regulation of cellular proliferation and survival [4]. In humans, YAP is over-expressed as a result of genomic amplification of the 11q22 locus in a wide spectrum of human
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