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The MeO CFO phen yl group was
2022-03-16

The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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The relationship between estrogen and the Hedgehog pathway a
2022-03-16

The relationship between estrogen and the Hedgehog pathway as well as the associated mechanism have already been investigated in many tissues, especially in breast cancer (Chang et al., 2012, Katayama et al., 2006, Ramaswamy et al., 2012). Hitherto, even though we have proved that HH-Gli pathway pro
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MAPK are involved in a large
2022-03-16

MAPK are involved in a large variety of solid and hematolgical neoplasms and, indeed, several components of the MAPK network have already been proposed as targets in cancer therapy, such as p38, JNK, ERK1/2, MEK1/2, RAF, RAS, DUSP1 and ERK5 [11], [12]. Among them, alteration of the RAS-RAF-MEK1/2-ER
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br Contributions br Acknowledgements This research was
2022-03-16

Contributions Acknowledgements This research was supported by Natural Sciences and Engineering Research Council (NSERC) Discovery grant No. 341538 and Ontario Graduate Scholarships to HM and VS. Introduction Sexual size dimorphism describes size difference between male and female individua
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Cx has been shown to
2022-03-16

Cx45 has been shown to be serine phosphorylated by CaMKII, CK1, PKA, and MAPK in HeLa C-type natriuretic peptide (1-22) (human, rat, swine) [77], [78]. Phosphorylation by PKA and MAPK were associated with decreased junctional conductance [78], suggesting that phosphorylation of Cx45 may influence co
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br The bile acid farnesoid X receptor FXR
2022-03-16

The “bile acid” farnesoid X receptor (FXR) The Farnesoid X Receptor (FXR) is a ligand-activated nuclear receptor belonging to the Nuclear Receptor superfamily of transcription factors exploiting various crucial functions in mammalian physiology, including reproduction, development and metabolism
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The current gold standard for diagnosing
2022-03-16

The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) SB431542 (also known as the SeHCAT retention test). SeHCAT test involves the use of a synthetic analogue of naturally occurring conjugated taurocholic acid and m
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Michiel S van der Heijden had full
2022-03-16

Michiel S. van der Heijden had full access to all KNK437 data in the study and takes responsibility for the integrity of the data and the accuracy of the data analysis. Wang, Sustic, de Oliveira, van den Heuvel, Bernards, van der Heijden. Wang, Sustic, de Oliveira, van de Ven. Wang, Sustic, d
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Methods and materials Escherichia coli
2022-03-15

Methods and materials Escherichia coli JM109(DE3) ATI-2341 containing a derivative plasmid of pUCmod that encodes E. coli FDPS (IspA) previously described by Schmidt-Dannert and co-workers [22] were grown in LB media containing 150μg/mL of ampilicin. E. coli was grown directly from stock cells sto
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br Interference in coagulation assays Conversely to heparin
2022-03-15

Interference in coagulation assays Conversely to heparin, or heparin like emodin (LMWH, Fondaparinux, Sodium Danaparoid), which are catalytic inhibitors requiring the presence of AT for their activity, as depicted on Fig. 2, DiXaIs are directly targeted to Factor Xa, and are reversible [39]. DiX
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Next we were interested in replacing the
2022-03-15

Next, we were interested in replacing the ketobenzimidazole fragment of our inhibitors with a noncarbonyl bearing heterocycle. We reasoned that if we could replace the carbonyl while maintaining comparable FAAH inhibition, it would provide evidence for a noncovalent mechanism of action. Thus, we eva
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br Conclusion br Disclosure of
2022-03-15

Conclusion Disclosure of interest Introduction The Joint United Nations Program on HIV and AIDS (UNAIDS) proposed the ambitious global goal of achieving the "90-90-90" target by 2020 and ending the HIV epidemic by 2030 (Barton-Knott, 2014). One important measure is to monitor the incidence
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The importance of the histone chaperone
2022-03-15

The importance of the histone chaperone function of Hat1p was highlighted by the recent demonstration that the catalytic activity of Hat1p is not sufficient for its function in vivo. Fusion of a nuclear export signal (NES) to yeast Hat1p effectively excluded the enzyme from the nucleus, with a conco
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Taken together the four HRs couple with several different
2022-03-15

Taken together, the four HRs couple with several different signaling pathways modulating various G-proteins (Fig. 1). Histamine H1R The H1R, including many other biogenic amine receptors, is one of the GPCR family members (see for a complete list e.g. http://www.gpcr.org/7tm/ or http://tools.gpc
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Although we showed that RBL H Sc cells took up
2022-03-15

Although we showed that RBL-2H3 Sc98 a nice person took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, including
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