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Mammals have three known Gli proteins Gli and
2022-06-10
Mammals have three known Gli proteins: Gli-1, -2 and -3. Gli-1 does not undergo proteosomal degradation and hence, remains untruncated and always acts as a transcription promoter. Gli-1 is an important target gene for Gli-2. Full-length Gli-2 accumulates when Smo is activated because activated Smo p
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Hepatitis C virus HCV is a frequent cause of
2022-06-10
Hepatitis C virus (HCV) is a frequent cause of infectious chronic hepatitis. Unlike hepatitis A and B, there is no vaccine to prevent hepatitis C infection yet. According to WHO, around 200 million people are infected with HCV worldwide [1], in addition to three to four million newly infected patien
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Furthermore we observed a striking difference between BR
2022-06-10
Furthermore, we observed a striking difference between BR 11257 and activators from the dicarboxylic MAPK Inhibitor Library type in thermofluor measurements on thermostability. The dicarboxylic acids cinaciguat [30] and BAY 60-2770 (see Fig. 3) induced a significant melting temperature increase of s
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Compared with the tetrazole derivative the potency
2022-06-10
Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, su
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br NO GC pathway and implications for glaucoma Direct in
2022-06-10
NO-GC-1 pathway and implications for glaucoma Direct in vivo measurement of NO in the eye is not yet feasible. However, measurement of nitrate and nitrite levels are routinely used as markers for the activity of NOS and the production of NO radicals [98]. Several studies in human glaucoma patient
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bapta synthesis While the specific set of challenges associa
2022-06-10
While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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Several studies have found that GPR
2022-06-10
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 GSK180 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rimona
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In experiments using D to displace binding of
2022-06-09
In experiments using D22 to displace binding of specific high-affinity radioligands for DAT, NET, and SERT in mouse α-Cyperone tissue, we observed a ranking with D22 displacement efficiency in the order of DAT > SERT > NET (IC50 values being ~ 11 (DAT), 26 (SERT), and 101 (NET) µM; Fig. 1, Fig. 2,
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Moreover to evaluate the properties
2022-06-09
Moreover, to evaluate the properties of immobilized β-glucosidase further, the anti-protease test was also carried out. The result showed that the residual activity of the β-glucosidase@ZIF-8 was higher than that of the nano-SiO2@β-glucosidase and free β-glucosidase. Because free β-glucosidase and t
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br GR Is a Transcriptional Activator How
2022-06-09
GR Is a Transcriptional Activator How GR activates some genes while repressing others remains unsettled after decades of study. While significant controversy exists regarding GR-mediated repression, a consensus model for transcriptional activation has emerged: GR activates transcription through s
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br Xenobiotics and the Glucocorticoid Receptor br Conclusion
2022-06-09
Xenobiotics and the Glucocorticoid Receptor Conclusion Transparency document Acknowledgements The author wishes to thank Professor Wilhelm Engström from the Swedish University of Agricultural Sciences (Department of Biomedical Sciences and Veterinary Public Health) for his proof reading
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It is generally considered that
2022-06-09
It is generally considered that elevated blood glucose due to insulin resistance is an important factor in islet compensation to high fat feeding [27]. However, we have shown recently that insulin resistance induced in mice by hydrocortisone injection provokes significant islet cholecystokinin recep
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Cabazitaxel Further we examined the degradation of
2022-06-09
Further, we examined the degradation of Cx43. Autophagy and the proteasome system have previously been implicated in Cx43 degradation (Falk et al., 2014). DEX inhibited communication between Cabazitaxel by promoting the degradation of Cx43 through autophagy in osteocytes (Gao et al., 2016). In our
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The role of GJs in
2022-06-09
The role of GJs in liver fibrogenesis was studied recently. Studies showed a significant decrease in liver fibrosis in Cx32 knockout mice compared to wild-type mice. Although the mechanism underlying this protective effect of Cx32 deletion is not clear, reduced oxidative stress was suggested as a po
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There is a dual inducer of both
2022-06-09
There is a dual inducer of both galanin and super-threshold pain. First, injury-induced pain may stimulate galanin secretion. After peripheral nerve injury, the galanin expression level was upregulated in dorsal root ganglion (DRG), dorsal horn and hypothalamic arcuate of rats [25], [28], [33]. The
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