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72 items found for "chemokine truncation"

  • Involvement of various chemokine/chemokine receptor axes in trafficking and oriented locomotion ...

    Involvement of various chemokine/chemokine receptor axes in trafficking and oriented locomotion of mesenchymal Chemokine and chemokine receptors are of the most important and effective molecules in MSC trafficking Chemokine/chemokine receptor axes play a pivotal role in the recruitment and oriented trafficking of immune cells both towards and within the CNS and it appears that chemokine/chemokine receptor signaling In this article, we hypothesized that the chemokine/chemokine receptor axes network have crucial and

  • Canonical chemokine receptors as scavenging “decoys”

    The immune system depends on chemokines to direct cell migration during immune surveillance and inflammation However, an imbalance in the chemokine system can also contribute to various diseases, such as inflammatory In all these situations, chemokines interact with seven-transmembrane chemokine-type G protein-coupled In humans there are approximately 45 chemokines, 19 chemotactic or G-protein coupled chemokine receptors Indeed, ACKRs behave as scavenging “decoys” in order to either limit chemokines spatial availability

  • Structural landscape of the Chemokine Receptor system

    The chemokine system exhibits great versatility, with more than 50 chemokines interacting with over 20 receptor-chemokine complexes and revealing the diverse and multifaceted nature of the chemokine receptor Chemokine Binding Mode – from CRS1 to CRS3 Chemokines possess a conserved tertiary structure known as are bound to a G-protein - two of the structures involve complex formation with endogenous N-terminal truncation It has been demonstrated that the shorter truncation variant, CCL15L, exhibits bias toward G-protein

  • Chemokine receptor-targeted drug discovery: progress and challenges

    The chemokine receptor system is implicated in a wide range of inflammatory, autoimmune and infectious The involvement of chemokines and their receptors in several aspects of cancer biology, represents a Therefore, an alternative approach is to make use of chemokine receptors redundancy and the fact that different chemokine receptors are overexpressed and promote cancer progression, and use promiscuous In the chemokine-receptor system, different chemokines are able to activate different pathways, which

  • Glyco-sulfo hotspots in the chemokine receptor system

    Glycosylation and sulfation – N-terminal PTMs on chemokine receptors The interaction of chemokine receptors with their cognate chemokine ligands is generally described by the two-step/two-site model - the first interaction between the extracellular domains of the receptor and the structural core domain of the chemokine (CRS1); and the second step featured by the interaction between the N-terminus of the chemokine and Within the CRS1 ineraction mode, the N-terminal region of chemokine receptors is indispensable for chemokine

  • Activation of the human chemokine receptor CX3CR1 regulated by cholesterol

    August 2022 "As the only member of the CX3C chemokine receptor subfamily, CX3CR1 binds to its sole endogenous

  • CD28 and chemokine receptors: Signalling amplifiers at the immunological synapse

    signalling amplification and compartmentalization in T cell activation, focusing on the role of CD28, chemokine

  • Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine..

    October 2022 Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases "The chemokine receptor CXCR3 is a seven-transmembrane G-protein-coupled It is activated by the three chemokine ligands CXCL9, CXCL10, and CXCL11 and enables the recruitment

  • Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1) and its...

    September 2022 Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1 ) and its interactions with antagonist and agonist ligands "The CX3C chemokine receptor 1 (CX3CR1), a

  • Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2

    development of fluorescent ligands targeting the intracellular allosteric binding site (IABS) of the CC chemokine

  • Murine bone marrow macrophages and human monocytes do not express atypical chemokine receptor 1

    August 2022 "The atypical chemokine receptor 1 (ACKR1) was discovered on erythrocytes as the Duffy blood group antigen ( Cutbush et al., 1950 ), also called Duffy-antigen/receptor for chemokines, or DARC (

  • MSX-122: Is an effective small molecule CXCR4 antagonist in cancer therapy?

    August 2022 "Chemokines, a subgroup of cytokines along with their receptors, are involved in various C-X-C motif chemokine receptor 4 (CXCR4), a G-protein-coupled receptor (GPCR), has one identified natural

  • Tracking receptor motions at the plasma membrane reveals distinct effects of ligands on CCR5...

    Here, we investigated this issue in living cells for the CC chemokine receptor 5 (CCR5), a major receptor

  • Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of ...

    Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of the chemokine While several gain-of-function mutations that lead to C-terminal truncations, frame shifts and point mutations in the chemokine receptor CXCR4 have been identified in WHIM syndrome patients, the functional

  • Viral G Protein-Coupled Receptors Encoded by β- and γ-Herpesviruses

    genes are transmembrane proteins and cytokines, such as viral G protein-coupled receptors (vGPCRs), chemokines , and chemokine-binding proteins.

  • Chemerin Forms: Their Generation and Activity

    September 2022 "Chemerin is the product of the RARRES2 gene which is secreted as a precursor of 143 amino Chemerin can signal via two G protein-coupled receptors, chem1 and chem2, as well as be bound to a third This review discusses the specific tissue expression of the components of the chemerin system, and the role of different proteases in regulating the activation and inactivation of chemerin. with obesity or diabetes, leading to the possibility of using chemerin as a biomarker."

  • Feeder or trigger – CCR2 as a scavenger and regulator of cell migration

    Canonical chemokine receptors – scavenging “decoys” Chemokine receptors coordinate cell migration upon interaction with their cognate chemokines. The chemokine receptor family comprises 19 canonical chemokine receptors together with 4 atypical chemokine chemokines and chemokines from tissue microenvironments has been well described for ACKRs which work But why do canonical chemokine receptors have this dual role in physiology?

  • Effects of Small Molecule Ligands on ACKR3 Receptors

    August 2022 "Abstract Chemokines such as stromal derived factor 1 and their G protein coupled receptors C-X-C motif chemokine ligand 12 (CXCL12) has two receptors: C-X-C chemokine motif receptor 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3). SIGNIFICANCE STATEMENT: We are interested in the signaling produced by the G protein coupled receptor atypical chemokine

  • Location bias contributes to functionally selective responses of biased CXCR3 agonists

    signaling contributes to the biased signaling generated by three endogenous ligands of the GPCR CXC chemokine In CD8 + T cells, the chemokines promote unique transcriptional responses predicted to regulate inflammatory the overall biased response observed at CXCR3, which has important implications for drugs targeting chemokine

  • Profiling Immune Cell and Platelet Transcriptomes

    For instance, the expression of specific chemokine receptors in monocytes and macrophages indicates their to elucidate their specific contributions.Moreover, the study's findings on the unique expression of chemokine

  • CCL25/CCR9 interaction promotes the malignant behavior of salivary adenoid cystic carcinoma via...

    malignant behavior of salivary adenoid cystic carcinoma via the PI3K/AKT signaling pathway "Background CC chemokine receptor 9 (CCR9), an organ-specific chemokine receptor, interacts with its exclusive ligand CCL25 to

  • GPCR kinase phosphorylation of distal C-tail sites specifies βarrestin1-mediated signaling by...

    provide evidence that distal carboxyl-terminal tail (C-tail), but not proximal, phosphorylation of the chemokine We demonstrate by pharmacologic inhibition of GRK2/3-mediated phosphorylation of the chemokine receptor

  • 📰 GPCR Weekly News, May 22 to 28, 2023

    Structural and Molecular Insights into GPCR Function Cholesterol Biases the Conformational Landscape of the Chemokine dopamine receptor system Structural Insights into Molecular Recognition and Receptor Activation in ChemokineChemokine

  • 📰 GPCR Weekly News, July 17 to July 23, 2023

    GPCR Activation and Signaling Atypical Chemokine Receptor 3 'Senses' CXC Chemokine Receptor 4 Activation Fluorescent Ligands Enable Target Engagement Studies for the Intracellular Allosteric Binding Site of the Chemokine

  • Unlocking the Future of Medicine: Advancements in GPCR Research

    Chris de Graaf, Cherine Bechara, et al. for their work on Conformational dynamics underlying atypical chemokine from July 15th to 21st, 2024 GPCR Activation and Signaling Conformational dynamics underlying atypical chemokine Cyanobacterium Fluorophore-Labeled Pyrrolones Targeting the Intracellular Allosteric Binding Site of the Chemokine

  • 📰 GPCR Weekly News, January 30 to February 5, 2023

    GPCR Activation and Signaling The dual-function chemokine receptor CCR2 drives migration and chemokine Simultaneous activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling The chemokines CXCL8 and CXCL12: molecular and functional properties, role in disease and efforts towards

  • Exciting GPCR Events for Next Year! + GPCR Weekly Rocket Launch ⦿ Oct 28 - Nov 3, 2024

    al. for their excellent work on Receptor determinants for ß-arrestin functional specificity at C-X-C chemokine like and β2 adrenergic receptors Receptor determinants for ß-arrestin functional specificity at C-X-C chemokine receptors for the treatment of alcohol use disorders: Opportunities and hurdles for clinical development Chemokine

  • Targeting Intracellular Allosteric Sites in GPCRs

    of spatio-temporal attributes in signaling is demonstrated in processes like neurotransmission and chemokine with receptor subtypes that exhibit significant similarity in their orthosteric binding sites, such as chemokine discovery of an intracellular allosteric site common in class A and class B GPCRs, particularly in chemokine

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