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Sonidegib is currently under investigation for
2021-10-27

Sonidegib is currently under investigation for the treatment of relapsed/refractory acute leukemia (NCT01826214) [76]. All patients experienced at least 1 AE, including anemia, diarrhea, fatigue, nausea, muscle spasms, decreased appetite, and blood creatine phosphokinase increased. The ongoing phas
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br Introduction Soluble guanylyl cyclase GC maintains vascul
2021-10-27

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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Similarly spectrophotometric titrations were carried out und
2021-10-27

Similarly, spectrophotometric titrations were carried out under conditions identical to those used for the fluorescence titrations. exhibited a predominant wnt inhibitor band at around 493 nm. The titrations with all G-quadruplex DNAs resulted in a hypochromic effect along with a bathochromic shif
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Receptor tyrosine kinases RTKs consist
2021-10-27

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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According to the implication of the
2021-10-27

According to the implication of the endocannabinoid system in IBD, we decided in our laboratory to develop selective CB agonists and FAAH inhibitors to treat these diseases. Recently, we described 3-carboxamido-5-aryl-isoxazoles as selective CB agonists. This series of isoxazoles possesses a 2-subst
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br Discussion Our results showed that the histamine H
2021-10-27

Discussion Our results showed that the histamine H1 receptor antagonist/inverse agonists, pyrilamine and cetirizine, attenuated not only NMDAR-mediated synaptic current but also LTP in Shaffer collateral-CA1 pyramidal neuron synapses. The H1 receptor antagonist/inverse agonist-induced attenuation
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br Introduction Chronic hepatitis C CHC caused by hepatitis
2021-10-26

Introduction Chronic hepatitis C (CHC) caused by hepatitis C virus (HCV) infection affects approximately 170 million individuals worldwide [1]. HCV and human immunodeficiency virus (HIV) have similar routes of transmission, including blood-to-blood contact, sharing of injection equipment, and sex
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Compounds and were tested for pharmacodynamic effects
2021-10-26

Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a
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In this study we describe
2021-10-26

In this study, we describe the role of a specific species of LPI in the secretion of GLP-1 from enteroendocrine L-cells and primary cell preparations. We further demonstrate the specific role of GPR119 in LPI-dependent GLP-1 secretion. To achieve this, we downregulated GPR119 and GPR55 protein expre
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br Introduction Over the past two decades the
2021-10-26

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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PTMs have been shown to influence transporter kinetics both
2021-10-26

PTMs have been shown to influence transporter kinetics, both directly and indirectly (Xu & You, 2017). They do not just regulate the innate structure-function relationship driven by a transporter's global architecture, but rather are also able to regulate this relationship down to the resolution of
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br Acknowledgements This work was supported
2021-10-26

Acknowledgements This work was supported by a fellowship to C.H. under the ‘100 Foreign Expert’ scheme of the Shanxi province government(R100456). Conflict of interest: Dr. Holscher is a named inventor on a patent submitted by Lancaster University on the use of dual GLP-1/GIP analogues in neurode
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Sickle erythrocytes are known to have an increased
2021-10-26

Sickle erythrocytes are known to have an increased adhesion to endothelial UNC 0642 sale (Hebbel et al., 1980, Hebbel et al., 1981a, Hebbel et al., 1981b, Wautier et al., 1985, Mohandas and Evans, 1987). Understanding the events associated with vaso-occlusion requires a detailed knowledge of the int
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Here we dissect X chromosome
2021-10-25

Here, we dissect X chromosome dosage compensation (DC) in C. elegans to determine the effect of chromatin modifications on higher-order chromosome structure during long-range gene regulation. DC is exemplary because it controls hundreds of genes simultaneously, it distinguishes X chromosomes from au
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br Acknowledgment S A was supported by
2021-10-25

Acknowledgment S.A was supported by V Plan Propio US-Acceso USE-14793-G. Introduction The Hippo signaling pathway is an evolutionarily conserved pathway that controls organ size and cell differentiation across diverse organisms through the regulation of cell proliferation and apoptosis (Di C
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