Search Results
521 items found for "Jespers W"
- Free-Energy Simulations Support a Lipophilic Binding Route for Melatonin Receptors
We investigated the feasibility of this lipophilic entry route for 2-iodomelatonin, a nonselective agonist calculations. 2-Iodomelatonin unbinding was investigated with steered molecular dynamics simulations which together, our simulations are consistent with the possibility that the gap between TM IV and V is a way also suggest that the open state of Tyr5.38 generates a small pocket on the surface of MT1 receptor, which
- SLAS2022 International Conference and Exhibition
"We are moving ahead with SLAS2022 as an in-person event with a hybrid component. We are closely monitoring any regulation changes from both Boston and Massachusetts with regard to in-person If there are any changes made that will impact our ability to hold the event in-person, we will notify
- Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for ...
not a static entity, but one that is altered under pathophysiological conditions and, in this review, we have compared expression of GPCR mRNAs in human islets obtained from normal weight range donors, and those with a weight range classified as obese. We have also considered the likely outcomes on islet function that the altered GPCR expression status
- Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β-Arrestin ...
bioluminescence resonance energy transfer -based biosensors, second messenger assays, and biochemical techniques, we We characterized the effects of extracellular loop mutations on agonist-promoted interactions of GPCRs
- Exendin-4 Attenuates Remodeling in the Remote Myocardium of Rats After an Acute Myocardial ...
GLP-1 agonist Exendin-4 after an acute myocardial infarction (MI) in rats involves inhibition of the Wnt1 Methods: Rats were divided into sham, sham + Exendin-4 (10 μg/day, i.p), MI, and MI + Exendin-4. as protein levels of Wnt1, phospho-Akt, transforming growth factor (TGF-β1), Smad, phospho-Smad3, α-SMA altering protein levels of TGF-1β and Wnt1 or Akt activation. After MI, TGF-β1, and Wnt 1 levels are significantly increased, the overproduction of Wnt1 induces β-catenin
- TeachOpenCADD - A teaching platform for computer-aided drug design
While documentation for such tools is available, only few freely accessible examples teach underlying TeachOpenCADD is a teaching platform developed by students for students, which provides teaching material Since we cover both the theoretical as well as practical aspect of these topics, the platform addresses students and researchers with a biological/chemical as well as a computational background.
- Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas ...
Here, we outlined the expression of brain ORs and investigated OR expression levels in glioma. Although most ORs were not ubiquitously expressed in gliomas, a subset of ORs displayed glioma subtype-specific identified as a potential biomarker of favorable overall survival in isocitrate dehydrogenase (IDH) wild-type addition to transcriptomic analysis, mutational profiles revealed that somatic mutations in OR genes were on this systematic analysis and review of the genomic and transcriptomic profiles of ORs in glioma, we
- Chronic itch: emerging treatments following new research concepts
Until recently, itch pathophysiology was poorly understood and treatments were poorly effective in relieving
- G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial ...
As GRK2 is implicated in controlling various aspects of cellular growth, we examined whether GRK2 could Using two indices of cell growth, we show that PI3K inhibition and depletion of GRK2 expression produced knockdown ablated the sustained phase of endothelin-1 and angiotensin-II-stimulated Akt phosphorylation, whilst
- Neuronal Gα subunits required for the control of response to polystyrene nanoparticles in the ...
Caenorhabditis elegans was used as an animal model, and both gene expression and functional analysis were
- Melatonin MT 2 receptor is expressed and potentiates contraction in human airway smooth muscle
melatonin are mediated via its specific G protein-coupled receptors (GPCRs) named the MT1 receptor, which couples to both Gq and Gi proteins, and the MT2 receptor, which couples to Gi. We investigated whether melatonin receptors are expressed on airway smooth muscle; whether they regulate intracellular cyclic AMP (cAMP) and calcium concentrations ([Ca2+]i), which modulate airway smooth muscle tone; and whether they promote airway smooth muscle cell proliferation.
- The development of modulators for lysophosphatidic acid receptors: A comprehensive review
Lysophosphatidic acids (LPAs) are bioactive phospholipids implicated in a wide range of cellular activities While no drugs targeting LPARs have been approved by the FDA thus far, at least three antagonists have
- On-cell nuclear magnetic resonance spectroscopy to probe cell surface interactions
In this review, we outline some key NMR techniques applied for on-cell NMR studies through both solution In particular, we focus on the application of on-cell NMR spectroscopy to characterize ligand interactions Interestingly, it is possible to avoid the barriers of production and purification of membrane proteins while We also provide a brief survey of the applicability of on-cell NMR approaches to other classes of cell
- Coordinated transcriptomics and peptidomics of central nervous system identify neuropeptides and ...
Grapholita molesta The oriental fruit moth Grapholita molesta is a cosmopolitan pest of orchard, which Here, we generated a transcriptome of the central nervous system (CNS) of G. molesta. Overall, 57 neuropeptide precursor genes were identified and 128 various mature peptides were predicted A total of 41 neuropeptide GPCR genes belonging to three classes were also identified. These GPCRs and their probable ligands were predicted.
- 4GPCRnet - International Symposium
ERNEST plus DFG-funded CRC1423 and RU2372 ) have joined forces to organize an international meeting, which We aim to connect renowned international experts of the field with early career ‘rising stars’. The event will take place in the heart of Leipzig, which offers a colorful mixture of culture and vivid
- GPCR Signaling and mTORC1 Regulation
In this review, we will discuss the regulation of mTORC1 by upstream stimuli, with a specific focus on
- Involvement of various chemokine/chemokine receptor axes in trafficking and oriented locomotion ...
sclerosis patients Multiple sclerosis (MS) is a specific type of chronic immune-mediated disease in which Chemokines are low molecular weight proteins that their functional activities are achieved by binding Chemokine and chemokine receptors are of the most important and effective molecules in MSC trafficking within In this article, we hypothesized that the chemokine/chemokine receptor axes network have crucial and Therefore, we reviewed the ability of MSCs to migrate and home into the CNS of MS patients via expression
- Rescue of Cell Surface Expression and Signaling of Mutant Follicle-Stimulating Hormone Receptors
We previously demonstrated rescue of cell surface expression of luteinizing hormone receptor mutants Here we demonstrate that a similar approach can be employed to rescue mutant follicle-stimulating hormone Seventeen FSHR mutations described in patients with reproductive dysfunction were expressed in HEK 293T Cell surface expression was severely reduced to ≤18% of wild-type (WT) for 11, modestly reduced to 66% to 84% of WT for 4, and not reduced for 2.
- TLR4 biased small molecule modulators
Toll-like receptor 4 (TLR4) is one such non-GPCR receptor, which involves MyD88-dependent and TRIF-dependent Moreover, the dysregulation of TLR4 contributes to numerous diseases, which highlights the importance In this review, we aim to provide an overview of the recent progress in the discovery of biased modulators The discovery of biased modulators of TLR4 would provide insight for the future development of biased
- Disentangling bias between G q, GRK2, and arrestin3 recruitment to the M 3 muscarinic acetylcholine
Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase 2 (GRK2), as well as arrestin3 binding to the muscarinic acetylcholine receptor M3 by utilizing FRET-based In order to avoid interference between these interactions, we studied GRK2 binding in the presence of We measured substantial differences in the agonist efficacies to induce M3R-arrestin3 versus M3R-GRK2 the same, suggesting that G protein and GRK2 binding to M3R requires similar receptor conformations, whereas
- GPCRS: AN ODYSSEY FROM STRUCTURE, SIGNALING AND REGULATION TO THERAPEUTICS
While GPCRs are considered a well-established field, recent technological advances to dissect the molecular
- Sosei Heptares Enters Antibody Discovery Agreement with Twist Bioscience to Discover and Develop ...
proprietary synthetic antibody libraries and sophisticated bioinformatics expertise with Sosei Heptares’ world-leading Japan and Cambridge, UK, 16 December 2021 – Sosei Group Corporation (“the Company”; TSE: 4565), the world
- First in Human: Early-stage COVID therapies hold promise against omicron variant
19 treatments from the likes of Vir Biotechnology Inc. and Trevena Inc. could offer potential new weapons While vaccine-makers race to test their shots against the variant, the monoclonal antibody sotrovimab
- VIB spin-off Confo Therapeutics Enters Collaborative Agreement with Regeneron
December 2021 "30/11/2021 Confo will work together with Regeneron to apply its GPCR drug discovery today announced that it has entered into a collaborative agreement with Regeneron Pharmaceuticals, Inc. whereby Confo’s technology platform, which uses conformationally selective VHH antibodies – ConfoBodies® – to
- OMass Therapeutics's founder, Carol Robinson, has been awarded the prestigious Louis-Jeantet ...
Medal in Chemistry from The Franklin Institute " Huge congratulations to our founder, Carol Robinson , who Her work in the field has been instrumental and is set to shape the future of drug discovery for years
- New structural perspectives in G protein-coupled receptor-mediated Src family kinase activation
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- Dr. Peter Robert Banks - Dr. GPCR Podcast
Listen where you get your podcasts. https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr #drgpcr #
- Dr. Adriano Marchese - Dr. GPCR Podcast
Listen where you get your podcasts https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #drgpcr #gpcr #podcast