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GPCR Retreat Program < Back to schedule Biased agonism at the GLP-1 receptor: from structure to animal models

inhibition with the porcupine inhibitor LGK974 decreases trabecular bone but not fibrosis in a murine model provide new insights into the role of Wnt and Gs-signaling in fibrosis and bone formation in a mouse model

Before focusing on the development of innovative mathematical modeling and simulation methods for drug They explored the potential of merging mathematical models with biology, the complexities of GPCRs within Integrating Mathematical Models and Biology: A Fascinating Discussion Yamina and Aurelien Rizk had a conversation about the importance of merging mathematical models and biology. and relevance of mathematical models in systems biology and pharmacology.

Here we used zebrafish and mouse models to probe the role of BLT2 in macrophage function during inflammation We detected BLT2 expression in bone marrow derived and peritoneal macrophages of mouse models. Using a zebrafish model of tailfin injury, we demonstrated that antisense morpholino-mediated knockdown We further replicated these findings in zebrafish models of islet injury and liver inflammation.

Our study aimed to identify the role of RGS20 in NSCLC prognosis and delineate associated cellular and

contrast, none of the peptides generated a signal on CCR5, but a CCL3-derived tetrapeptide was a positive modulator chemokine N-termini can be mimicked to produce small CCR1-selective agonists, as well as CCR5-selective modulators Schuermans , Anna Walser , Stavroula Louka , Ida Aaberg Lillethorup , Jon Våbenø , Katrine Qvortrup , Paul Proost , Mette M Rosenkilde Tags GPCR , allosteric modulation , chemokine , chemokine truncation , pharmacology

Committee Sponsors GPCR Retreat Program < Back to schedule Pharmacological and Genetic Preclinical Models

Genetic mouse models of CRC coupled with Gpr176-deficiency are investigated, and in vivo and in vitro GPR176 is confirmed to activate the cAMP/PKA signaling pathway and modulate mitophagy, promoting CRC A homolog model tool confirmed that GPR176 recruits GNAS intracellularly via its transmembrane helix , Yifei Feng , Kangpeng Jin , Xiaowei Wang , Yueming Sun Tags GPCR , autophagy , growth , homology modeling

The current study has attempted to close the gap by generating highly refined model structures of C5aR2 inactive), complexed to C-terminal peptide of C5a (meta-active) and the C5a (active), embedded to a model The computational modeling and the 1.5-μs molecular dynamics data presented in the current study are

Her next career step took her to AstraZeneca as a postdoctoral trainee, where she studied animal models Andrew Charles that who specialized in animal models of migraine and delta-opioid receptors as a therapeutic

receptor (GPCR)-related genes and differentially expressed genes (DEGs) in an acute lung injury (ALI) model In an in vivo study, the effects of RGS6 knockout were studied in a mouse model of ALI induced by lipopolysaccharide and 49 congruously downregulated genes) were identified among GPCR-related genes and DEGs in the ALI model RGS6 was downregulated in vivo and in vitro in the ALI model.

2024 Abstract "Recent progress in elucidating the role of specific antidiuretic hormones in Drosophila models We also acknowledged the limitations of current experimental models in this study and emphasized the

Herein we propose a model for immune conditioning, whereby metabolites such as butyrate affect immune This model helps explain how the gut microbiome may be affecting peripheral immune cells, and consequently

strategies to express, reconstitute and assay engineered GPCRs using the visual pigment rhodopsin as a model that stemmed from this work, such as the concept of “functional micro-domains” and the “helix movement model Tom’s lab also pioneered the early use of computational homology modeling, molecular dynamics simulations

biased agonism, and incorporates computational and mathematical modelling, structural and chemical biology , molecular and cellular pharmacology, medicinal chemistry, and preclinical models of behaviour and disease The conversation ended with Arthur's ongoing research and his development of a new operational model. model for allosteric modulation, emphasizing the balance between mechanism and empiricism. importance of establishing the correct disease context, setting up appropriate assays, and understanding the models

including structural biology and proteomics, molecular biology and biochemical enzymology, primary and model cell culture, and transgenic, knockout, knock-in and conditional models of mouse physiology and behavior

including structural biology and proteomics, molecular biology and biochemical enzymology, primary and model cell culture, and transgenic, knockout, knock-in and conditional models of mouse physiology and behavior

including structural biology and proteomics, molecular biology and biochemical enzymology, primary and model cell culture, and transgenic, knockout, knock-in and conditional models of mouse physiology and behavior

including structural biology and proteomics, molecular biology and biochemical enzymology, primary and model cell culture, and transgenic, knockout, knock-in and conditional models of mouse physiology and behavior

peptides such, as growth hormone-releasing hormone (GHRH), have been proposed to bind in a two-step model Indeed, peptide GHRHR antagonists have displayed promising results in many cancer models.

Statistical approaches and machine learning models were applied to identify signatures for drug response revealed in the co-occurring or mutual exclusivity pattern were further subjected to machine learning models

proteins by LPA, and by the related lipid mediator sphingosine-1-phosphate (S1P), in various cellular models In some model systems, CCN1 and CCN2 play key roles in LPA/S1P-induced cell migration and proliferation or S1P) can activate GPCR-mediated intracellular signaling to induce the production of extracellular modulators

the molecular mechanisms of adhesion GPCRs (aGPCRs) in lymphatic endothelial cells (LECs), a cellular model

conditional depletion on dendritic cell (DC-cKO), and keratin 14-conditional knockout (K14-cKO) mice models (IMQ)-induced GPR97-/- mice, which was consistent with the results in DC-cKO and K14-cKO psoriasis model

annual percentage change (EAPC) with 95 % confidence intervals (95 % CI) fitted age-period-cohort (APC) models Elisabete Weiderpass , Gholamreza Roshandel , Freddie Bray , Reza Malekzadeh Tags Age-Period-Cohort model

., PNAS, 2014) in breast cancer pathogenesis, using mouse models, three-dimensional cell culture and Mike also spoke about his initial struggles during his Ph.D., such as a difficult model system and a age and his desire to gain more knowledge about cancer biology led him to transition into using mouse models asked about his move from in vitro to in vivo work, and Mike explained that he wanted to use better models Yamina proposed further exploration of dosage and length of treatment in a mouse model and suggested

University in Australia, one of the pioneers in the medicinal chemistry, computational and mathematical modelling scientists working in the arenas of structure and signaling, neuroscience, cancer, translational and model

My initial focus was on creating an automated chimeric homology modeling pipeline for GPCRs and since