Mar 14, 2025 · CCR8, like other chemokine receptors, is a GPCR with a seven-transmembrane (7TM) domain embedded in the cell membrane. This structure enables conformational changes upon ligand binding, facilitating intracellular signaling.

Receptor for the chemokine CCL1/SCYA1/I-309. May regulate monocyte chemotaxis and thymic cell line apoptosis. Alternative coreceptor with CD4 for HIV-1 infection. Was originally thought to be a receptor for SCYA3 and SCYA17. Gene Ontology (GO) annotations organized by slimming set. Cell membrane ; Multi-pass membrane protein.

We find that although the 7TM bridge between TMIII and ECL-2 is crucial for binding and action of chemokine and small molecule ligands to and on CCR8, the CKR bridge between the N terminus and TMVII is mainly important for binding of chemokines.

Mar 15, 2007 · In summary, SAR exploration of a novel oxazolidinone series identified via HTS led to the discovery of potent human CCR8 antagonists such as SB-649701 (1a) with good chemotaxis activity, selectivity, DMPK, and hERG properties.

Aug 1, 2007 · In the present study, we identify a highly potent and selective CCR8 nonpeptide agonist, LMD-009, and describe its molecular interaction with CCR8 by combining receptor mutagenesis with studies of different chemical analogs of LMD-009.

Jul 29, 2016 · Here we investigate the importance of conserved extracellular disulfide bridges and aromatic residues in extracellular loop 2 (ECL-2) for ligand binding and activation in the chemokine receptor CCR8.

Jan 25, 2012 · UniProt is the world’s leading high-quality, comprehensive and freely accessible resource of protein sequence and functional information.

7TM ICL1 ECL1 ICL2 ECL2 ICL3 ECL3 N-term C-term Q T N G K L L L A V F Y C L L F V F S L L G N S L V I L V L V V C S I T D V Y L L N L A L S D L L F V F S F P F Q T Y ...

Feb 2, 2024 · The ligand-free and G i -coupled CCR8 exhibits a substantial constitutive activity of CCR8, which is consistent with the functional characterization. Two agonist-bound CCR8 structures present features of the orthosteric ligand-binding pocket for …

Jul 29, 2016 · We find that although the 7TM bridge between TMIII and ECL-2 is crucial for binding and action of chemokine and small molecule ligands to and on CCR8, the CKR bridge between the N terminus and TMVII is mainly important for binding of chemokines.