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Introduction Risk factors for colorectal cancer CRC include
2021-10-15
Introduction Risk factors for colorectal cancer (CRC) include high-fat diets, sedentary lifestyles, obesity, diabetes, and elevated serum levels of toxic bile acids (BAs) (de Aguiar Vallim et al., 2013, Degirolamo et al., 2011, Downes and Liddle, 2008, Font-Burgada et al., 2016, Kuipers et al., 201
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The typical pharmacophore for GPR agonists
2021-10-15
The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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Our results are consistent with
2021-10-15
Our results are consistent with the hypothesis that reduced Fas-mediated apoptosis in maternally activated T-lymphocytes could result in insufficient trophoblast invasion of the spiral self-flagellation as the activated T-lymphocytes become able to enhance the destruction of the cytotrophoblasts. A
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The newly synthesized compounds were evaluated
2021-10-15
The newly synthesized compounds were evaluated for their FAAH inhibitory activity in vitro. In addition, molecular modeling, selectivity and reversibility behavior of the new class of FAAH inhibitors are presented in this article. Results and discussion The potency of inhibition on the human rec
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EdU is a thymidine analog that is incorporated into replicat
2021-10-15
EdU is a thymidine analog that is incorporated into replicated chromosomal DNA during the S phase of the cell cycle. DAPI is a fluorescent dye that binds strongly to A-T-rich regions in DNA and is commonly used for cell nucleus staining. We used the EdU incorporation assay, which is a highly sensiti
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In addition to narrowing a
2021-10-15
In addition to narrowing a wide knowledge gap in Hh developmental biology research, improved understanding of Disp structure and function is likely to also be relevant to cancer. A growing body of evidence supports that Shh facilitates tumor–stroma communication in a range of cancers to influence tu
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br Methods br Results br Discussion Peptide therapeutics rep
2021-10-15
Methods Results Discussion Peptide therapeutics represents a unique class of biopharmaceuticals that continues to evolve in drug discovery and development. We and others have been particularly interested in bioengineering innovative pGC-A and/or pGC-B peptide activators. This has been succe
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br Introduction Soluble guanylyl cyclase GC maintains vascul
2021-10-15
Introduction Soluble guanylyl cyclase (GC-1) maintains vascular function through the NO/GC-1/cGMP pathway [1,2] by catalyzing the conversion of GTP into cGMP (Fig. 1). The GC-1 heme prosthetic group binds NO with picomolar affinity, resulting in a 100- to 200-fold increase in catalytic activity.
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It has been found that WHI
2021-10-15
It has been found that WHI-P131, a JAK3 inhibitor, induced apoptosis of CD4+ T citric acid sale (Cetkovic-Cvrlje et al., 2012). Also, other JAK3 inhibitors (AG490 and WHI-P154) caused apoptosis in anaplastic large cell lymphoma (Amin et al., 2003). Taking into account the proapoptotic action of JAK
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The aim of this study is to explore new
2021-10-15
The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof
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DNA repair is essential for cell survival and for
2021-10-15
DNA repair is essential for cell survival and for tissue homeostasis given that cellular DNA is constantly challenged by various endogenous and exogenous genotoxic factors that generate DNA damage: structural and chemical modifications of a primary DNA sequence. Various organisms have evolved multip
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br Introduction The glucagon receptor
2021-10-15
Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m
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Recently unimolecular multi functional peptides
2021-10-15
Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with γ-Secretase inhibitor IX and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose con
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Newt GHS R a proteins
2021-10-15
Newt GHS-R1a proteins expressed in a mammalian cell were able to bind homologous newt ghrelin, heterologous rat and bullfrog ghrelin, and a peptidyl GHS-R1a agonist, GHSRP-6, with inducing intracellular Ca signaling. This indicates that the identified cDNA encodes the ghrelin receptor from a view of
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According to the aforementioned preclinical
2021-10-15
According to the aforementioned preclinical and clinical data, GHS-R1a blockade appears to be a potential pharmacological approach to treat AUD. Given that GHS-R1a has high constitutive (ligand-independent) activity, inverse agonism of the receptor may exert more potent and desirable effects than pu
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