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fgfr1 Importance of glucokinase in glucose homeostasis and a
2022-05-16
Importance of glucokinase in glucose homeostasis and a possibility to change its activity using the activators define the scientific interest in the development of new allosteric activators of GK (Liu et al., 2012, Pfefferkorn et al., 2011, Waring et al., 2013, Behera et al., 2015). Activation of gl
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br Ethics approval br Availability of data and materials
2022-05-16
Ethics approval Availability of data and materials Consent for publication Competing interests Authors contributions Introduction Glucose supply to tissues is maintained through a complex regulatory network mostly driven by the pancreatic hormones insulin and glucagon which control
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Conformational analysis provides further insight into the
2022-05-16
Conformational analysis provides further insight into the SAR trends apparent in . Acyclic precursors – are 25–50-fold less active than their macrocyclic counterparts – against Pyk2. The global minima for – are conformations in which the –NHCH– linker between the pyrimidine and pyridine rings is sta
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Recent findings of us suggest that compounds
2022-05-16
Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that
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Several classes of small molecules that modulate CDK activit
2022-05-13
Several classes of small molecules that modulate CDK8 activity have been reported in the patent literature (Fig. 1). A quinazoline derivative, Senexin B (SNX2-1–165, 1), showed CDK8 enzyme inhibitory activity with an IC50 value of 24–50 nM in different assay, and displayed potent, selective enzymati
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GSK is inhibited by serine phosphorylation at
2022-05-13
GSK-3 is inhibited by serine cucurbitacin sale at a residue its N-terminus (Ser 9 in GSK-3β and Ser 21 in GSK-3α) [52], [53], [54]. This raised the possibility that the N-terminal tail may function as a pseudo-substrate by mimicking the pre-phosphorylated substrate. The interaction mode of the pseu
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Because of its excellent GPR potency good hERG selectivity
2022-05-13
Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, formyl was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel of
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The HIV genome encodes for a variety of viral proteins
2022-05-13
The HIV-1 genome encodes for a variety of viral proteins necessary for target cell entry and viral replication. gp120 is an HIV-1 envelope glycoprotein that mediates viral particle entry by binding to cell surface receptor CD4 and co-receptors CXCR4 and/or CCR5 depending on viral tropism. While CXCR
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Alpha synuclein AS is a protein located in
2022-05-13
Alpha synuclein (AS) is a protein located in presynaptic terminals of neurons that functions in recycling and storage of neurotransmitters [17]. Under conditions of inflammation and oxidative stress, AS proteins misfold and accumulate into 2595 [81], [90]. The aggregates of misfolded AS oligimorize
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Four polymorphic variants of Neil namely
2022-05-13
Four polymorphic variants of Neil1, namely, S82C (rs5745905), G83D (rs5745906), C136R (rs5745907) and D252N (rs5745926) were characterized by Roy et al. in 2007 (Table 1). Analyses of AP site incision on Tg containing oligonucleotide showed that S82C and D252N variants had wild type activity and car
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P gps expressed in cells and tissues of human
2022-05-13
P-gps, expressed in R788 and tissues of human and animals, play an active role in cellular protection against multiple toxicants by transporting them out of a cell. Thus, improving transport activity of P-gp may contribute to removing Cd from living oysters. Cd accumulation in the cultured cells is
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Also considered very rare is
2022-05-13
Also considered very rare is progressive encephalomyelitis with rigidity and myoclonus (PERM); sometimes called Stiff Person Syndrome Plus (SPS Plus) and with antibodies to glutamic glucocorticoid receptor antagonist decarboxylase (GAD). However, PERM is now increasingly found with glycine receptor
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The HH Gli pathway has been demonstrated
2022-05-13
The HH-Gli pathway has been demonstrated to play an extensive role in skeletal development. India Hedgehog, derived from hypertrophic chondrocytes, and Parathyroid Hormone-like related Protein (PTHrP), derived from peri-articular chondrocytes, form a negative feedback loop to inhibit chondrocyte hyp
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Extending time action is another strategy to increase in
2022-05-13
Extending time action is another strategy to increase in vivo efficacy. Twice daily administration of the unacylated analogs herein caused greater body weight loss in DIO mice than the equivalent dose administered as a single daily injection, suggesting that protracted time action should yield more
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br Introduction The growth hormone secretagogue receptor
2022-05-13
Introduction The growth hormone secretagogue receptor (GHSR) gene, which was first isolated from rats and humans (Kojima et al., 1999), comprises two exons and one intron in mammals and chicken. The pig GHSR is located on chromosome 13 (range 110,981,465–111,006,149 on Reference Sscrofa11.1). Alt
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