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In summary we obtained and type of linaclotide by protein
2021-11-23
In summary, we obtained - and -type of linaclotide by protein chemical synthesis and acquired the X-ray crystal structure of linaclotide for the first time through racemic crystallization technique. The structure of linaclotide forms a compact spatial structure containing three- turns through three
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br Mutagenesis and Receptor Modeling Studies br Signal Trans
2021-11-23
Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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br GPR is a class A GPCR
2021-11-23
GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine pramipexole dihydrochloride which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119
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In women with stage I II endometriosis no difference
2021-11-23
In women with stage I–II endometriosis [17], no difference in the implantation rate per embryo or in the clinical pregnancy rate per transfer was noted between GnRH-agonist and GnRH-antagonist protocol (18.2% vs. 15.4%, P=0.9 and 31.2% vs. 30%, P=1, respectively). It has been suggested that either
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br Materials and methods br Results br Discussion
2021-11-23
Materials and methods Results Discussion The previous studies have reported that positive GLUT1 expression had a predictive value for prognosis of lung cancer patients (Younes et al. 1997a; Meijer et al., 2012; Sasaki et al., 2012). Our conclusion was accordant with these studies. Recently,
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Interestingly transgenic mice that constitutively express ac
2021-11-23
Interestingly, transgenic mice that constitutively express active FXR in the intestine (iVP16FXR) are protected from chemically-induced and genetically-induced cholestasis. This protective effect is attributed to the induction of intestinal FGF15 and repression of hepatic Cyp7a1 expression, downregu
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Natural product based drug discovery
2021-11-22
Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in GNE-617 binding assays, we used molecular modeling to predict how well these compounds fit
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1-NM-PP1 Receptor tyrosine kinases RTKs consist of subfamili
2021-11-22
Receptor tyrosine kinases (RTKs) consist of 20 subfamilies in humans, all of which share a common structure consisting of extracellular ligand-binding region, a single-pass transmembrane domain and an intracellular tyrosine kinase domain [2]. Binding of a growth factor to the ligand-binding domain r
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However the clinical development of was terminated in
2021-11-22
However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this rece
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On the other hand after injury of the adult
2021-11-22
On the other hand, after injury of the adult heart, inflammatory monocytes are abundantly recruited to damaged myocardium and they differentiate into monocyte-derived macrophages (MDMs). They have strong proinflammatory phenotype and very limited capacity to promote angiogenesis and cardiomyocyte pr
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Lieber have discussed alcohol outside the context of
2021-11-22
Lieber (2000), have discussed alcohol outside the context of hepatitis C infection exerts specific pathologic effects on the liver. Liver biopsies in patients with hepatitis C who drink alcohol are generally consistent with hepatitis C alone, with portal-based pathology, rather than alcoholic injury
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The initial beta carboline derivatives used in the in
2021-11-22
The initial beta-carboline derivatives used in the in silico docking experiments were prepared using the procedure outlined in . Harmol, , was -alkylated with -Boc-protected alkylamines in the presence of cesium carbonate to give and . The carbamate protecting group was removed under acidic conditi
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Introduction Inorganic arsenic InAs species such as arsenite
2021-11-22
Introduction Inorganic arsenic (InAs) species such as arsenite (AsIII) and arsenate (AsV) are present in groundwater. Arsenic contaminated drinking water is a global public health issue because of its natural prevalence and toxicity. Long exposure to arsenic results in chronic effect in humans, inc
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Bioinformatic analysis revealed a putative coiled coil SLD w
2021-11-22
Bioinformatic analysis revealed a putative coiled-coil SLD within CT229 which we show to be essential for intracellular replication and recruitment of Rab GTPases to the inclusion. Mutation of a single amino SL 0101-1 residue in the SLD domain (CT229L120D) significantly reduced Rab binding and rec
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stat3 inhibitor GPR shares a amino acid sequence identity
2021-11-22
GPR81 shares a 52% amino stat3 inhibitor sequence identity in humans to GPR109A [1], [2], [3]. In addition, GPR81 is localized more specifically to the adipose tissue [3]. In 2008, lactate was discovered to be the endogenous ligand for GPR81 [9], [10]. Plasma lactate levels reach concentrations capa
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