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Insights into the molecular mechanism of positive cooperativity between partial agonist MK-8666 and full allosteric agonist AP8 of hGPR40 by Gaussian accelerated molecular dynamics (GaMD) simulations
2021
Computational and Structural Biotechnology Journal
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Yao, Insights into the molecular mechanism of positive cooperativity between partial agonist MK-8666 and full allosteric agonist AP8 of hGPR40 by Gaussian accelerated molecular dynamics (GaMD) simulations ...
Abstract Activation of human free fatty acid receptor 1 (FFAR1, also called hGPR40) enhances insulin secretion in a glucose-dependent manner. ...
Moreover, we have clarified the mechanism of positive cooperativity between the partial agonist and AgoPAM binding sites. ...
doi:10.1016/j.csbj.2021.07.008
fatcat:5r2amxgllvejvbbhsjex4ofzla
Identification and Pharmacological Characterization of Multiple Allosteric Binding Sites on the Free Fatty Acid 1 Receptor
2012
Molecular Pharmacology
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Activation of free fatty acid 1 receptor (FFAR1) by each of these agonists is differentially affected by mutations of two arginine residues, previously found to be important for FFAR1 binding and activation ...
Analysis of functional data reveals positive functional cooperativity between the full agonists and partial agonists in various functional assays (in vitro and ex vivo) and also in vivo. ...
We are also thankful to Jenny Lu, Jeff Reagan, and Ralf Schwandner for providing the stable cell lines. ...
doi:10.1124/mol.112.079640
pmid:22859723
pmcid:PMC3477236
fatcat:xjcuxwjiyrd6patf5upkmgau6a
Recent Advances in Structure, Function, and Pharmacology of Class A Lipid GPCRs: Opportunities and Challenges for Drug Discovery
2021
Pharmaceuticals
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and allosteric ligand binding sites, and molecular mechanisms of ligand binding. ...
The extraordinary progress in structural biology and pharmacology of GPCRs, coupled with rapid advances in computational approaches to study receptor dynamics and receptor-ligand interactions, has broadened ...
Acknowledgments: This research was supported by Biomedical Research Council of Agency for Science, Technology and Research (A*STAR), Singapore (to H.F.). ...
doi:10.3390/ph15010012
pmid:35056070
pmcid:PMC8779880
fatcat:cqbgiz4sj5hz5kjbd4o2z7udwy
Mucosal Interactions between Genetics, Diet, and Microbiome in Inflammatory Bowel Disease
2016
Frontiers in Immunology
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The possibility that these effects may reflect a number of other interconnected (i.e., pantropic) mechanisms, activated in parallel, particularly concerning various bacterial metabolites, is in the process ...
fatty acids; (3) the effect of diet on bile acid composition, and the modulator role of bile acids on the gut microbiota; (4) the impact of endogenous and exogenous intestinal micronutrients and metabolites ...
Host genetics and gene expression modulate immune mechanism of microbial molecular pattern recognition to influence the diversity and functionality of local microbiota (11). ...
doi:10.3389/fimmu.2016.00290
pmid:27531998
pmcid:PMC4970383
fatcat:cfryycl6wfa6bdxoblz42pkbm4
The bromodomain and extra-terminal domain degrader MZ1 exhibits preclinical anti-tumoral activity in diffuse large B-cell lymphoma of the activated B cell-like type
2021
Exploration of Targeted Anti-tumor Therapy
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Here are presented data on the anti-tumor activity and the mechanism of action of the BET degrader MZ1 in diffuse large B cell lymphoma (DLBCL) of the activated B-cell like (ABC, ABC DLBCL), using a BET ...
Results: MZ1, and not its negative control epimer cisMZ1, was very active with a median half maximal inhibitory concentration (IC50) of 49 nmol/L. ...
New molecular and therapeutic
insights into canine diffuse large B-cell lymphoma elucidates the role of the dog as a model for human
disease. Haematologica. 2019;104:e256-9. ...
doi:10.37349/etat.2021.00065
fatcat:rnjkevbzrbf3bmi5d5pku6xsda
Free Communications (Oral Sessions)
2015
Journal of Pharmacological Sciences
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Here, we report novel activators of transient receptor potential canonical (TRPC) channels which regulate neuronal function via modulation of Ca 2+ signaling. ...
However, its molecular mechanism remains unknown. We have analyzed a role for mDia in emotional changes induced by chronic stress. ...
This study was undertaken using the mouse macrophage cell line RAW264.7 to gain insight into its anti-in ammatory mechanisms. ...
doi:10.1016/j.jphs.2015.07.028
fatcat:ryzemiuhbvcbng6ymlirll245e
Islet Biology/Insulin Secretion
2013
Diabetes
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Inhibitors of NOX activity reduce cellular ROS and the expression of NOX1. This observation suggests a feed-forward regulation of NOX1 in beta cells involving ROS elevation. ...
We have also shown that NOX1 is upregulated by 12-lipoxygenase (12-LO) activity POSTERS ISLET BIOLOGY-APOPTOSIS in beta cells. 12-HETE (a product of 12-LO activity) upregulates NOX1 13±3fold (p<0.01) and ...
During normal β-cell development, the cooperation of several transcription factors successively specifi es progenitor cells towards development into β-cells. ...
doi:10.2337/db13-2161-2296
pmid:23792721
fatcat:p7m2nxoezzdclcibpvn7zsrevy
Integrated Physiology/Obesity
2014
Diabetes
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We aimed to identify the molecular mechanism of severe IR in a 35-years-old nonobese woman who was diagnosed as having type 2 diabetes at age 31 during pregnancy. ...
Tests for insulin and INSR antibodies were both negative. To explore the underlying molecular defect of IR, we sequenced the INSR gene. ...
Those fi ndings would offer novel insights into the mechanisms of GCs induced fat distribution. ...
doi:10.2337/db14-1741-2092
fatcat:brgtjdu6yfcnxft766a2v3y6gi
Integrated Physiology/Obesity
2015
Diabetes
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UcOC was shown to correlate positively with CPR in GLT and CPR after meal taking (r = 0.32, p = 0.025; r = 0.29, p = 0.047). ...
The average of age, duration of diabetes, BMI, and HbA1c of the subjects were 59.2 y.o., 7.8 years, 26.2 kg/m2 and 9.4%, respectively. ...
cholesterol, and use of anti-hypertensive and lipid-lowering drugs. ...
doi:10.2337/db15-1929-2253
fatcat:x5hpu3ohqveifpkrby2rjwkp3m
QUANTITATIVE EVALUATION OF A NOVEL SELF-MANAGEMENT EDUCATION PROGRAM FOR COPD IN THE CONTEXT OF MULTI-MORBIDITY
2017
Respirology (Carlton South. Print)
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Acknowledgements: The grants were from Science and Technology Commission of Shanghai Municipality (No. 14411966400) and the National Science Foundation of China (NSFC81370109, 81670006). ...
All the authors contributed to the study and had no conflict of interest. ...
Further investigation of the underlying mechanisms may provide new insight into COPD pathogenesis. ...
doi:10.1111/resp.13206_193
fatcat:aocfzb5ulveorgtsqzamm5quee
Genome-wide homozygosity mapping in Congenital Hyperinsulinism of Infancy (CHI) :a family based study
[article]
2009
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molecular mechanism at the basis of the disease.. ...
Mutations in ABCC8 gene are responsible of the 50-60% of focal and diffuse CHI patients, otherwise mutations in KCNJ11 are responsible for 10-15% of cases..Other less frequent molecular mechanism responsible ...
molecular mechanism at the basis of the disease. ...
doi:10.13130/gessi-alessandra_phd2009-01
fatcat:7p4w77rukbdixn2jg4dvkmfexa
Characterisation of suppressor of cytokine signaling 1 regulation of type I interferon signaling
2017
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This thesis details the mechanism of SOCS1 regulation of type I IFN signaling as well as the consequences of this regulation in terms of its effect on IFNα induced STAT activation and the resultant transcriptional ...
STAT1 is up-regulated by type I IFN in a broad range of immune cell types including thymic and peripheral T-cells, B-cells and macrphages whereas activation of STAT3 and STAT5 is more confined to the thymic ...
A combination of ChIP-Seq studies with next generation sequencing of the RNA profile induced in the cell will also provide insight into how these STATs cooperatively regulate gene expression. ...
doi:10.4225/03/58b4e8a11950d
fatcat:uuqnn2kleff6vmyygbvcmrnrdq
Nrg4 and Gpr120 signalling in brown fat
2015
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These findings could provide insight into the requirements for Gpr120 function in BAT, the exploitation of which could generate ligands for therapeutic benefit and represents a promising opportunity to ...
Gpr120 is a member of the superfamily of G protein-coupled receptors that is activated by long chain fatty acids. ...
DISCLOSURES The authors declare that they have no conflicts of interest, financial or otherwise.
AUTHOR CONTRIBUTIONS ...
doi:10.25560/26287
fatcat:j4vywh73jndkldlf5psbq52wt4
Synthesis of Structural and Fluorescently Labelled Peptidic Ligands for Optical Imaging of G Protein-Coupled Receptors
2017
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Fluorescence imaging is capable of facilitating highly specific and non-invasive investigation of cellular and molecular events both in vitro and in vivo. ...
This thesis describes the synthesis and pharmacological properties of structural and fluorescent peptide analogues that target the GPCRs of interest. ...
A typical example is that feeding behaviour and the associated obesity appear to be regulated by multiple subtypes in highly complicated cooperating or counteracting mechanisms. ...
doi:10.4225/03/58c77bf8b2a95
fatcat:tjrnhtbsjvehhlfuopu22vnypi
Scienze e Tecnologie Agrarie Ambientali e Alimentari Ciclo XXIX Towards the development of nutrigenetic concepts in pigs by merging genomics, transcriptomics and metabolomics Presentata da: ANISA RIBANI Coordinatore Dottorato Relatore
unpublished
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pathways would be one of the envisaged perspectives of application in pig nutrigenetics and, more generally, in livestock nutrition. ...
Several approaches of target metabolomics, target re-sequencing of pig genome portions and RNA-seq have been performed, adding classical lab validations. ...
Acknowledgements We thank ANAS for providing data and samples, Sara De Fanti (University of Bologna) for technical assistance, members of the Centre for Genome Biology for their support and Rita Casadio ...
fatcat:42jd4ramwnglnbliaf3aj5uwwi
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