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Activation of sGC induces the generation of
2022-03-24

Activation of sGC induces the generation of cyclic guanosine monophosphate (cGMP), phosphorylation of protein kinase G (PKG) and changes in activity of effector proteins such as phosphodiesterases (PDE), ion channels and ion pumps [43]. This pathway eventually leads to dilation of Alisol A (broncho
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In conclusion LA is able
2022-03-24

In conclusion, LA is able to enhance osteoblast differentiation that mediated by PTH in a MCT-1 independent but GPR81 signaling dependent manner. This increase requires p38 activation and an Akt activation that depended on Gβγ-protein-PLC-PKC signaling. However, the ability of LA to increase PTH–med
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As disclosed in our preceding paper
2022-03-24

As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, Epothilone D lacks
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Pregnancy per AI results at days post TAI tended
2022-03-24

Pregnancy per AI results at 32 days post TAI tended to differ among GnRH products and was greater for FER and CYS than FAC according to the Tukey-grouping analysis statistical approach (Table 1). In addition, P/AI was greater for cows treated with gonadorelin diacetate products than for cows treated
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The presented results speak for the direct
2022-03-23

The presented results speak for the direct effects of ghrelin on rat spermatozoa, which are accomplished by the activation of the GHSR-1a receptor. Thus, the results seem to be of physiological significance in vivo since ghrelin, the natural ligand of GHSR-1a, was found to be present in the seminal
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A model substance often used in the
2022-03-23

A model substance often used in the studies of oxidative processes in erythrocytes is tert-butyl hydroperoxide (t-BHP), which, being lipophilic, passes easily across the erythrocyte membrane [9]. In erythrocytes treated with t-BHP (0.1–3mM) for less than 1h, a dramatic decline in the reduced glutath
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br Mechanisms of gap junction internalization disaggregation
2022-03-23

Mechanisms of gap junction internalization: disaggregation, endocytosis and annular gap junctions It has been clearly shown that gap junction internalization can occur by a distinctive mechanism where one cell internalizes an entire gap junction via formation of double membrane structure termed a
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Studies of human and mouse GPR as
2022-03-23

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 infla
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br Nanoscale Cortical Actin Remodeling in Regulated Exocytos
2022-03-23

Nanoscale Cortical Actin Remodeling in Regulated Exocytosis The network of cortical Alosetron is formed by numerous fine actin filaments, which are only about 10nm in diameter [52]. Although the microscale role of the cortical actin network in vesicle exocytosis is well established, the function
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br Transportation from TGN toward plasma membrane The
2022-03-23

Transportation from TGN toward plasma membrane The insulin molecules are packaged along with other molecules such as C-peptides, amylin, Zn2+, ATP and GABA in synaptic-like macrovesicles (SLMVs, with the diameters of 50–100 nm) and large dense core vesicles (LDCVs, with the diameters of 200–500 n
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Classical drugs target the viral enzymes reverse transcripta
2022-03-23

Classical drugs target the viral BAY 61-3606 reverse transcriptase (RT), protease and integrase (IN) [[4], [5], [6]]. Raltegravir (ISENTRESS/MK-0518) is the prototypical integrase strand transfer inhibitor (INSTI) leading to an extremely strong reduction in viral load [7] and it has been approved f
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This profound cell type specificity of G
2022-03-23

This profound cell-type specificity of G9a/GLP complex modulation of neuronal plasticity is accentuated by studies employing genetic ablation of G9a in dopamine 1 receptor (Drd1)- and dopamine 2 receptor (Drd2)-expressing medium spiny neurons (MSNs) in the nucleus accumbens (NAc). Conditional G9a kn
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br Expression and Purification of LSD
2022-03-23

Expression and Purification of LSD1 Proteins In Vitro Enzymatic Assays Analysis of LSD1 Demethylase Activity Acknowledgments Conflict of Interest Statement: Y.S. is a cofounder of Constellation Pharmaceuticals, Inc. and is a member of its scientific advisory board. Y.S. is also a consu
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Acknowledgements We appreciated the contributions of Ana Car
2022-03-23

Acknowledgements We appreciated the contributions of Ana Carolina Galha, Selma XSL Pinheiro and Islene Azevedo for technical assistances. In addition, we wish to thank Adilson José de Almeida (in memoriam), Moyra M Portilho, Vanessa A Marques and Letícia P Scalioni, for data analysis during the set
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Immunology Compound Library Here we report the genomic struc
2022-03-23

Here we report the genomic structure and the phylogenetic analysis of testis-specific Ser/Thr kinase haspin gene. Materials and methods Results Discussion The isolation and analysis of haspin genomic DNA showed that haspin was an intron-less gene and localized in an intron of integrin αM29
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