scholarly journals Structural basis for the binding of the membrane-proximal C-terminal region of chemokine receptor CCR2 with the cytosolic regulator FROUNT

FEBS Journal ◽  
2014 ◽  
Vol 281 (24) ◽  
pp. 5552-5566 ◽  
Author(s):  
Kaori Esaki ◽  
Sosuke Yoshinaga ◽  
Tatsuichiro Tsuji ◽  
Etsuko Toda ◽  
Yuya Terashima ◽  
...  
Keyword(s):  
Chemokine Receptor ◽  
Terminal Region ◽  
Structural Basis ◽  
Chemokine Receptor Ccr2

Structural Basis for the Interaction of Human β-Defensin 6 and Its Putative Chemokine Receptor CCR2 and Breast Cancer Microvesicles

2013 ◽  
Vol 425 (22) ◽  
pp. 4479-4495 ◽  
Author(s):  
V.S. De Paula ◽  
N.S.F. Gomes ◽  
L.G. Lima ◽  
C.A. Miyamoto ◽  
R.Q. Monteiro ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Chemokine Receptor ◽  
Structural Basis ◽  
Chemokine Receptor Ccr2

Discovery and Mapping of an Intracellular Antagonist Binding Site at the Chemokine Receptor CCR2

2014 ◽  
Vol 86 (4) ◽  
pp. 358-368 ◽  
Author(s):  
Annelien J.M. Zweemer ◽  
Julia Bunnik ◽  
Margo Veenhuizen ◽  
Fabiana Miraglia ◽  
Eelke B. Lenselink ◽  
...  
Keyword(s):  
Binding Site ◽  
Chemokine Receptor ◽  
Antagonist Binding ◽  
Chemokine Receptor Ccr2

scholarly journals The chemokine receptor CCR2 maintains plasmacytoid dendritic cell homeostasis

2017 ◽  
Vol 192 ◽  
pp. 72-78 ◽  
Author(s):  
Oriane Cédile ◽  
Line Østerby Jørgensen ◽  
Ida Frank ◽  
Agnieszka Wlodarczyk ◽  
Trevor Owens
Keyword(s):  
Dendritic Cell ◽  
Chemokine Receptor ◽  
Plasmacytoid Dendritic Cell ◽  
Cell Homeostasis ◽  
Chemokine Receptor Ccr2

Chemokine CCL2 and chemokine receptor CCR2 in early active multiple sclerosis

2004 ◽  
Vol 11 (7) ◽  
pp. 445-449 ◽  
Author(s):  
T. L. Sorensen ◽  
R. M. Ransohoff ◽  
R. M. Strieter ◽  
F. Sellebjerg
Keyword(s):  
Multiple Sclerosis ◽  
Chemokine Receptor ◽  
Active Multiple Sclerosis ◽  
Chemokine Receptor Ccr2

scholarly journals Structural basis of the activation of the CC chemokine receptor 5 by a chemokine agonist

2020 ◽  
Author(s):  
Polina Isaikina ◽  
Ching-Ju Tsai ◽  
Nikolaus Dietz ◽  
Filip Pamula ◽  
Anne Grahl ◽  
...  
Keyword(s):  
Chemokine Receptor ◽  
Chemokine Receptors ◽  
Binding Mode ◽  
Activation Mechanism ◽  
Structural Basis ◽  
Cc Chemokine ◽  
Gi Protein ◽  
Agonist And Antagonist ◽  
Cc Chemokine Receptor 5 ◽  
Chemokine Receptor 5

AbstractThe human CC chemokine receptor 5 (CCR5) is a G protein-coupled receptor (GPCR) that plays a major role in inflammation and is involved in the pathology of cancer, HIV, and COVID-19. Despite its significance as a drug target, the activation mechanism of CCR5, i.e. how chemokine agonists transduce the activation signal through the receptor, is yet unknown. Here, we report the cryo-EM structure of wild-type CCR5 in an active conformation bound to the chemokine super-agonist [6P4]CCL5 and the heterotrimeric Gi protein. The structure provides the rationale for the sequence-activity relation of agonist and antagonist chemokines. The N-terminus of agonist chemokines pushes onto an aromatic connector that transmits activation to the canonical GPCR microswitch network. This activation mechanism differs significantly from other CC chemokine receptors that bind shorter chemokines in a shallow binding mode and have unique sequence signatures and a specialized activation mechanism.One-sentence summaryThe structure of CCR5 in complex with the chemokine agonist [6P4]CCL5 and the heterotrimeric Gi protein reveals its activation mechanism

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