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Structural Analysis of Chemokine Receptor–Ligand Interactions
This review focuses on the construction and application of structural chemokine receptor models for the elucidation of molecular determinants of chemokine receptor modulation and the structure-basedExpand
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Modulators of CXCR4 and CXCR7/ACKR3 Function
The two G protein-coupled receptors (GPCRs) C-X-C chemokine receptor type 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are part of the class A chemokine GPCR family and represent importantExpand
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Nanobody‐Fc constructs targeting chemokine receptor CXCR4 potently inhibit signaling and CXCR4‐mediated HIV‐entry and induce antibody effector functions
&NA; Upregulation of the chemokine receptor CXCR4 contributes to the progression and metastasis of both solid and hematological malignancies, rendering this receptor an attractive therapeutic target.Expand
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CXCR4‐targeting nanobodies differentially inhibit CXCR4 function and HIV entry
&NA; The chemokine receptor CXCR4 and its ligand CXCL12 contribute to a variety of human diseases, such as cancer. CXCR4 is also a major co‐receptor facilitating HIV entry. Accordingly, CXCR4 isExpand
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Antibodies Targeting Chemokine Receptors CXCR4 and ACKR3
Dysregulation of the chemokine system is implicated in a number of autoimmune and inflammatory diseases, as well as cancer. Modulation of chemokine receptor function is a very promising approach forExpand
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4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H3 Receptor Agonists with in Vivo Central Nervous System Activity
Despite the high diversity of histamine H3 receptor (H3R) antagonist/inverse agonist structures, partial or full H3R agonists have typically been imidazole derivatives. An in-house screening campaignExpand
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Chemokine Receptor Crystal Structures: What Can Be Learned from Them?
Chemokine receptors belong to the class A of G protein–coupled receptors (GPCRs) and are implicated in a wide variety of physiologic functions, mostly related to the homeostasis of the immune system.Expand
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Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists.
Using the available structural information of the chemokine receptor CXCR4, we present hit finding and hit exploration studies that make use of virtual fragment screening, design, synthesis andExpand
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Identification of Key Structural Motifs Involved in 7 Transmembrane Signaling of Adhesion GPCRs
The adhesion class B2 family of G protein-coupled receptors (GPCRs) plays a key role in important physiological processes and their dysfunction is linked to brain malformations and tumorigenesis.Expand
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Advanced fluorescence microscopy reveals disruption of dynamic CXCR4 dimerization by subpocket-specific inverse agonists
Significance Class A G protein−coupled receptors (GPCRs) can form dimers and oligomers via poorly understood mechanisms. We show here that the chemokine receptor CXCR4, which is a majorExpand