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After the origin of the family
2022-04-25
After the origin of the family of genes for receptors for peptides similar to glucagon, the genes have not remained static. Not only have their sequences evolved, but also like peptides similar to glucagon (Irwin, 2001, Irwin, 2009, Irwin, 2012, Ng et al., 2010, Hwang et al., 2013), the numbers of g
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Our own search towards aryl imidazole derived
2022-04-25
Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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The present results indicate that oxidative damage in
2022-04-22
The present results indicate that oxidative damage in CFS muscles is not due to the decline in the efficiency of antioxidative enzymes. This suggests that there is an increase in the generation of reactive oxygen species consistent with a mitochondrial origin of the damage. Mitochondria represent t
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Receptor guanylyl cyclases play essential roles in cardiovas
2022-04-22
Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists
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As a result of the capability of
2022-04-22
As a result of the capability of modulating the dynamic changes and rearrangement of cytoskeletons, the Rho GTPases, in which RhoA, Cdc42 and Rac1 are best-characterized, have been highlighted as significant contributors for orchestrating neuronal development (Duman et al., 2015, Heasman and Ridley,
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Electrostatic potential along with measurement and modeling
2022-04-22
Electrostatic potential along with measurement and modeling of corresponding energies is vital for inferring protein properties, lone or complexed with ligands. DelPhi was used for solving Poisson Boltzmann equation, obtaining grid, total reaction and coulombic energies after solvating the proteins
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Given the involvement of dysregulated S nitrosylation in
2022-04-22
Given the involvement of dysregulated S-nitrosylation in multiple pathological conditions, a number of approaches to regulate S-nitrosylation therapeutically are being tried in multiple indications [18]. In the lung, GSNO releasing compounds and GSNOR inhibitors are being considered as potential the
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Imatinib br GSK The GSK family is highly conserved
2022-04-22
GSK-3 The GSK-3 family is highly conserved throughout evolution and is encoded by two genes, GSK-3α and GSK-3β, which are located in chromosomes 19q13.2 and 3q13.3 in human, respectively. Both GSK-3α and GSK-3β proteins exist in a variety of tissues with the highest levels found in Imatinib [1],
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While a role for YAP TAZ signaling in oligodendrocytes
2022-04-22
While a role for YAP/TAZ signaling in oligodendrocytes has not been described, these KP372-1 are also responsive to mechanical stimuli. OPC proliferation and migration can be altered by plating on substrates of varying stiffness [20], resulting in differentiation in a density-dependent manner. Plat
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As part of our discovery efforts searching for small
2022-04-22
As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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br Introduction Adipose tissue AT in
2022-04-22
Introduction Adipose tissue (AT), in addition to its function as BAF312 storage, is an important endocrine organ and it secretes adipokines (Ahima, 2006). Adipose tissue is related to different physiological processes such as energy metabolism, insulin sensitivity, and inflammation. One important
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br Introduction Over the past two decades the
2022-04-22
Introduction Over the past two decades, the prevalence of obesity and obesity-associated metabolic diseases, such as T2D, insulin resistance, atherosclerosis and stroke, have been dramatically increased globally [1], [2], and obesity has been suggested to be the leading cause of the reduced life
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The results obtained through in vitro in
2022-04-22
The results obtained through in vitro, in vivo and in silico corroborated with those presented by other works and indicate that CpMutY is involved in oxidative damage repair in this organism. In this regard, MutY conservation in evolutionarily distant bacteria suggests that this protein plays an imp
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CZC-25146 receptor To this end we evaluated novel
2022-04-22
To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell CZC-25146 receptor systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.g. 6-su
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In conclusion we demonstrated that the atypical
2022-04-22
In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 β-Sitosterol results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network acts as “Cl−
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