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br Acknowledgments We would like to thank Coordena o de
2022-01-25

Acknowledgments We would like to thank Coordenação de Aperfeiçoamento de Pessoal do Ensino Superior (CAPES) and Conselho Nacional de Desenvolvimento Cientifico e Tecnológico (CNPq) for the grants and scholarships provide to the authors of this work. Introduction Human Immunodeficiency Virus t
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When studying the potential of HATi for the treatment
2022-01-25

When studying the potential of HATi for the treatment of inflammatory lung diseases, investigating lung tissue specific effects may be particularly relevant since local administration of small molecule inhibitors in lung tissue is possible and is already applied for inhaled glucocorticoids in the tr
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Histamine modulates an attentional state which might affect
2022-01-25

Histamine modulates an attentional state, which might affect performances in the object recognition test. Indeed, systemic injection of H3 receptor inverse agonists enhances the attentional state (41). However, the memory recovery in our study is unlikely to be due to the enhanced attentional state.
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Immunohistochemical evaluation of gastric cancer tumor sampl
2022-01-25

Immunohistochemical evaluation of gastric cancer tumor samples revealed that 57.8% (59/101) were positive for GLI1, and 71.3% (72/101) stained positive for SHH [27]. Overexpression of SHH and GLI1 protein were significantly associated with larger tumor size, tumor aggressiveness, and less differenti
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kasugamycin Sonidegib is currently under investigation for t
2022-01-25

Sonidegib is currently under investigation for the treatment of relapsed/refractory acute leukemia (NCT01826214) [76]. All patients experienced at least 1 AE, including anemia, diarrhea, fatigue, nausea, muscle spasms, decreased appetite, and blood creatine phosphokinase increased. The ongoing phas
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At days and hours after MI the protein expressions
2022-01-25

At 21 days and 24 hours after MI, the protein expressions of active JNK1 (P YM 155 of p38 was down-regulated only at 21 days after MI (P Discussion This study demonstrates the role of GSTP1 in HF by inhibiting the TRAF2-induced MAPK activation and the potent inhibitory effect of GSTP1 on TNF-α–in
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Nutlin-3 GSTP catalyzed reduction of Prdx enhances its perox
2022-01-25

GSTP1-1 catalyzed reduction of Prdx6 enhances its peroxidase activity. Using standard NADPH/GR/GSH-coupled assays we used cell lysates from the transiently transfected Nutlin-3 to measure the influence of GSTP1 allelic variation on peroxidase activity. Specificity for detection of Prdx6 activity was
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INCB28060 GSK is inhibited by serine phosphorylation at
2022-01-25

GSK-3 is inhibited by serine INCB28060 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 pseudo-subst
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br Action of GPR in
2022-01-25

Action of GPR55 in metabolically active tissues In addition to being highly expressed by discrete brain regions, as described in Section 2, GPR55 is also expressed in a wide range of peripheral tissues, including spleen, adrenals and bone (Sawzdargo et al., 1999, Ryberg et al., 2007, Whyte et al.
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In three independent groups identified
2022-01-25

In 2003, three independent groups identified GPR109A (HM74A) and GPR109B (HM74), two GPCRs, as the receptors for niacin., , GPR109A, which is present in all species, is a high affinity receptor for niacin., GPR109B, which is only present in human and chimpanzee, is a low affinity receptor for niacin
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To this end we evaluated novel D analogs for selectivity
2022-01-24

To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell Dimethyl Fumarate systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.g. 6-sub
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Solid tumors usually present insufficient supply
2022-01-24

Solid tumors usually present insufficient supply of oxygen, activating the hypoxia inducible factor-1 (HIF-1) pathway, which prompts an adaptive response on genes that regulate glycolytic metabolism, promoting glucose uptake through the transcription of GLUTs [54]. Increasing evidence indicates that
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Most excitingly we found the increased cells hold
2022-01-24

Most excitingly, we found the increased δ-cells hold the ability to trans-differentiate into β-cells in T1D mice. It has been shown that after near-total β-cell loss, juvenile mice display δ-to-β-cell conversion to recover diabetes, involving de-differentiation, proliferation and re-expression of is
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There are multiple docking platforms suitable for use with n
2022-01-24

There are multiple docking platforms suitable for use with nucleic TAPI-1 receptors. These include: DOCK v4-6 (UCSF) [[68], [69], [70]], AutoDock (Scripps) [71], AutoDock Vina (Scripps) [72], GOLD (Cambridge Crystallographic Data Centre) [73], Surflex-DOCK (BioPharmics) [74], Glide (Schrӧdinger) [7
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In soft agar colony formation assay transformed cells
2022-01-24

In soft agar colony formation assay, transformed 2 hydroxyglutarate indicate anchorage-independent growth and colony formation without attachment on the bottom of cell culture plate. This assay can investigate transformation and tumorigenic activities [24]. Our recent study showed that the long-term
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