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STF 083010 The compounds f and a
2022-07-12
The compounds 8f and 9a–e were found to be potent inhibitors of both isoforms of GSK-3 as characterized by IC50 values in the low nanomolar range. In addition, all of them showed good selectivities against other kinases. Substituents in the ortho- and para-positions of structure 8 and 9 lead to pot
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br Author contributions br Conflict of interest br
2022-07-12
Author contributions Conflict of interest Acknowledgments We appreciate technical support of the Research Support Center at the Graduate School of Medical Sciences of the Kyushu University. This study was supported by the Uehara Memorial Foundation and a KAKENHI grant from the Ministry of E
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It is interesting to note
2022-07-12
It is interesting to note that the long and short forms of GPR120 exist at different basal levels of phosphorylation, with the short form demonstrating a greater degree of constitutive activity [12]. Importantly, Burns and Moniri [12] showed that, upon activation, the long and short isoforms of GPR1
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Molecular properties as well as metabolic stability in rat a
2022-07-11
Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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br MUTYH associated polyposis br MUTYH and its metal cofacto
2022-07-11
MUTYH-associated polyposis MUTYH and its metal cofactors MUTYH harbors two vital cofactors, both of which are located remotely from the active site (Fig. 6). One of these cofactors, a [4Fe-4S]2+(Fe-S) cluster, is chelated by four Cys residues in the N-terminal domain, and positions an Fe-S clu
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Previous studies have demonstrated that cannabinoid potentia
2022-07-11
Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xio
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SGLT inhibitors have been accepted as a
2022-07-11
SGLT-2 inhibitors have been accepted as a new class of antidiabetic agent (Kurosaki and Ogasawara, 2013). They limit renal glucose reabsorption and promote urinary excretion of glucose, thereby reducing plasma glucose levels (de Leeuw and de Boer, 2016, Jojima et al., 2016, Pérez López et al., 2010,
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In this study we investigated the contribution of GCK G
2022-07-11
In this study, we investigated the contribution of GCK, G6PC, and PCK expression to glycemia in diabetes. We examined liver tissue from 40 obese subjects: 12 had normal glucose tolerance (NGT) and 28 had type 2 diabetes. Materials and methods Results Discussion This study aimed to investig
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DTP3 The relationship between estrogen and the Hedgehog path
2022-07-11
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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br Results and Discussion br STAR Methods
2022-07-11
Results and Discussion STAR★Methods Author Contributions Conflicts of Interest J.P.F. is a consultant for AstraZeneca, BMS, Johnson and Johnson, Novo Nordisk, and Sanofi, a member of the advisory panel for AstraZeneca and Sanofi, a member of the speaker’s bureau for Sanofi and Novo Nordi
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Ghsr may have therapeutic value in disorders associated with
2022-07-11
Ghsr may have therapeutic value in disorders associated with impairments in AHN. As anxiety disorders and enhanced fear responses observed in PTSD are linked with overgeneralization of similar but distinct memories (i.e poor discrimination), we suggest that acyl-ghrelin’s anti-anxiety effect (Lutter
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The caseins are a family of milk phosphoproteins whose biolo
2022-07-11
The caseins are a family of milk phosphoproteins whose biological function is to provide supersaturating concentrations of calcium, phosphates, and essential Ruxolitinib phosphate synthesis to the neonate (Vonderhaar and Ziska, 1989). α- and β-caseins, the most abundant of the milk caseins, are des
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p 00 receptor Based upon the present findings it is tempting
2022-07-11
Based upon the present findings, it is tempting to imagine that selective, and especially stable blood–brain barrier (BBB) penetrating GalR1 antagonists might be useful as drugs for acute suppression of appetite. While this may be possible, previous studies using nonspecific galanin antagonists yiel
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Somatostatin analogues are among the first peptide
2022-07-11
Somatostatin analogues are among the first peptide-based drugs used in cancer imaging and therapy (for review see Reubi, 2003). Treatment of tumors by the use of peptide analogues labeled with cytotoxic agents acting via specific receptors is also under investigation for neuropeptide Y (Koglin and B
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br Acknowledgments br The study was funded
2022-07-11
Acknowledgments The study was funded by the European Commission FP7-project Beta-JUDO (Grant 279153), and Swedish Diabetes Association (Grant DIA 2013-043) and Family Ernfors Foundation (Grant 150430). Free fatty 5 of 17000 receptors (FFARs) represent a family of G-protein coupled receptors
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