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It is interesting to note that the long
2022-05-24
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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Despite having potent activity and good solubility showed
2022-05-24
Despite having potent activity and good solubility, showed inhibitory activities against cytochrome P450 (CYP) 2C8, 2C9, and 2C19 with an IC value of less than 10 μM. In general, the specificity of the compound to the target should improve and the off-target risk such as CYP inhibitory activity sho
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br Transporter based brain targeting nano DDS Drug delivery
2022-05-23
Transporter-based brain-targeting nano-DDS Drug delivery to the central nervous system (CNS) is still challenging due to the bloodbrain barrier (BBB)53., 54.. The BBB is a natural defense barrier protecting the Adox from harmful substances. Since only selected, neutral, lipophilic small molecules
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ddhGTP Studies of human and mouse GPR as ascertained by mRNA
2022-05-23
Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl
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Having shown that some of substitutions Cl
2022-05-23
Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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A localization of GK to both a cytoplasmic
2022-05-23
A localization of GK to both a cytoplasmic and perinuclear area of normal rat pancreatic beta-cells was reported in 1996 (Noma et al., 1996), which changed on acute hyperglycemia to a more diffuse staining throughout the cytoplasm. The localization of GK within the nucleus was first reported by Mura
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The bFGF induced upregulation of both GR and
2022-05-23
The bFGF-induced upregulation of both GR and MR levels observed in our study raises a question regarding whether the simultaneous augmentation of the two receptors has a physiological and/or medical significance. It has been suggested that MR stimulates intracellular signaling pathways to minimize s
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Medulloblastoma predominantly occurs in infants and children
2022-05-23
Medulloblastoma predominantly occurs in infants and children, and is the most-common type of paediatric malignant 4μ8C tumour, accounting for about 20% of all childhood brain tumors [63]. According to cancer genomics, medulloblastoma consists of at least 4 distinct subgroups: Hh driven, Wnt driven,
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Knowing that our strongest phenotypic
2022-05-23
Knowing that our strongest phenotypic differences between the genotypes involved feeding behavior in various contexts, we decided to examine the case of restricted feeding and food anticipatory activity. Animals faced with a restricted schedule of food availability develop a series of anticipatory b
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The Cx family of integral membrane proteins are key componen
2022-05-23
The Cx family of integral membrane proteins [13] are key components of the Gap Junction channels that provide GJIC, which is indispensable in the preservation of tissue integrity and homeostasis in multicellular organisms. Gap Junction channels form a conduit for exchange of ions (Ca2+), second mess
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Receptor activator of NF B ligand RANKL and macrophage colon
2022-05-23
Receptor activator of NF-κB ligand (RANKL) and macrophage colony-stimulating factor (M-CSF) stimulate the generation of osteoclast gssg [10], [11], [12], [13]. In response to sphingosine 1-phosphate (S1P) signaling, osteoclasts then attach to regions of bone undergoing resorption [14]. In RA when S
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Sometime ago we have described diamino
2022-05-23
Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by 2461 synthesis and zymosan. In this work we describe new
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Almost all of the series and compounds exhibited higher
2022-05-23
Almost all of the series and compounds exhibited higher activities compared with the compounds in the other series. In these series, the tetrazole group was directly linked to a nitrogen atom of the amide group at the C-28 position, and the C-3 hydroxy group was either unmodified, oxidized, esterifi
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Work is presently underway to unveil
2022-05-23
Work is presently underway to unveil mechanisms whereby SAHA-dependent restoration of cardiomyocyte autophagic flux is protective. Another interesting question pertains to mechanisms whereby class I and class II HDAC inhibitors induce autophagy. It has been demonstrated that TSA reduces transverse a
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The mD plasmid containing CD domain
2022-05-21
The mD1.2 plasmid containing CD4 domain 1 gene under the control of a promoter was obtained as a gift from Dr. Dimiter S. Dimitrov. The mD1.2 plasmid was digested using restriction endonuclease I (New England BioLabs, USA) to release the mD1.2 gene. The gene encoding the mD1.2 protein was elongated
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