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Ulimorelin also known as TPZ is a
2021-09-23
Ulimorelin, also known as TPZ101, is a macrocyclic molecule that is a potent agonist of the ghrelin receptor (Hoveyda et al., 2011). Due to its ability to stimulate gastrointestinal motility, ulimorelin has been evaluated as a possible treatment in gastroparesis (Ejskjaer et al., 2010), ileus (Frase
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br Introduction G protein coupled receptors GPCRs
2021-09-23
Introduction G-protein coupled receptors (GPCRs) represent one of the largest family of receptors involved in cell membrane signal transduction and have become one of the leading therapeutic targets worldwide (Chakraborty and Chattopadhyay, 2015; Bouvier, 2001; Sriram and Insel, 2018). GPCRs sign
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The sexual dimorphism in dlGALR a and dlGALR b receptors
2021-09-23
The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that
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br Acknowledgments R Dalmann has obtained a
2021-09-22
Acknowledgments R. Dalmann has obtained a “bourse Cifre” (grant 304/2011) from the ‘Association Nationale de la Recherche Technique’ and Bristol-Myers-Squibb. Introduction Endocannabinoids, their molecular targets (receptors), their synthetic and degrading enzymes and proteins that transport
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ATN Ac PHSCN NH is
2021-09-22
ATN-161 (Ac-PHSCN-NH2) is a small peptide antagonist of integrin α5β1, a recently developed anticancer drug that interacts with the N-terminus of the β1 region of integrin α5β1 to lock integrin α5β1 in its non-activated conformation (Wang et al., 2016). The drug has been tested in Phase 2 clinical t
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YAP TAZ nuclear function is also influenced by
2021-09-22
YAP/TAZ nuclear function is also influenced by interaction with the TEAD family of transcription factors [96, 97, 98, 99, 100, 101]. The RAC1 Imatinib exchange factor protein TIAM1 has recently been linked to YAP/TAZ regulation in the nucleus and cytoplasm. Nuclear TIAM1 inhibits YAP/TAZ binding to
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An isoflavone type secondary metabolite Glabrescione B GlaB
2021-09-22
An isoflavone type secondary metabolite, Glabrescione B (GlaB), from Derris glabrescens (Benth.) J.F. Macbr. from the family Fabaceae, was found to possess the capacity to bind the Gli1 zinc finger domain and to further block DNA binding capacity [118]. Pyrvinium, an anthelmintic drug approved by th
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Small but statistically significant variance in PhyChem inde
2021-09-22
Small but statistically significant variance in 7 PhyChem indexes measured using intra-host HVR1 variants was shown to be strongly associated with CIP and MIP. All HVR1 sequences (N = 28,622) used here share only 6782 profiles of the selected 29 DAC’ of 7 PhyChem indexes. The significant majority (9
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HBV is an enveloped double
2021-09-22
HBV is an enveloped, double-stranded DNA virus, which is transcripted into four major transcripts [6]. Among them, the 3.5 kb pregenomic RNA (pgRNA) directs the translation of HBV polymerase, core protein and acts as template for reverse transcription. So viral transcription is a key step of virus l
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Acknowledgments The authors thank Partners Healthcare for fi
2021-09-22
Acknowledgments The authors thank Partners Healthcare for financial support. This work was also supported in part by NIH Grant R01CA122608 to J.M.G.H. Introduction The phosphorylation of histone H3 is recognized as a hallmark of mitosis. Histone H3 phosphorylation at Thr3 (H3T3ph) acts as a mit
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Here we used Drosophila and mouse models to address
2021-09-22
Here, we used Drosophila and mouse models to address the biological function of RALs in the adult intestine. Our results demonstrate a conserved in vivo role for RALs in ISC function during tissue homeostasis and regeneration. ISCs lacking RALs were at a disadvantage compared to wild-type neighbors.
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br Materials and methods br Results br Discussion
2021-09-22
Materials and methods Results Discussion Although there is general agreement that GPR109A has anti-lipolytic activity and that the NEFA reduction in response to nicotinic sch772984 is mediated by GPR109A, whether GPR109A activation has any impact on plasma TG levels is unclear. Since the p
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Throughout our studies we used
2021-09-22
Throughout our studies we used CBD under the assumption that it binds to the GPR55 receptor and has antagonist properties at the GPR55 receptor, as previously suggested (Whyte et al., 2009). To clarify whether the GPR55 receptor is involved in the O-1602-mediated effects on GI motility, we performe
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Introduction GPR is a class A type
2021-09-22
Introduction GPR119 is a class A type of G Protein coupled receptor, which is expressed primarily in pancreatic β-cells and the K and L cyclin dependent kinase inhibitor of the gastrointestinal tract [1], [2], [3]. Activation of GPR119 promotes secretion of incretins such as glucagon-like peptide-
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The rat model was validated with another agonist of
2021-09-22
The rat model was validated with another agonist of GPR109A, acipimox. Acipimox has been shown to induce vasodilatation in man, by a mechanism dependent on the release of vasodilator prostaglandins (Edlund et al., 1990, Pontiroli et al., 1992). Acipimox is a weaker agonist of the GPR109A receptor (L
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