Structural Features of an Extended C-Terminal Tail Modulate the Function of the Chemokine CCL21

Biochemistry. 2020 Apr 7;59(13):1338-1350. doi: 10.1021/acs.biochem.0c00047. Epub 2020 Mar 26.

Abstract

The chemokines CCL21 and CCL19, through binding of their cognate receptor CCR7, orchestrate lymph node homing of dendritic cells and naïve T cells. CCL21 differs from CCL19 via an unstructured 32 residue C-terminal domain. Previously described roles for the CCL21 C-terminus include GAG-binding, spatial localization to lymphatic vessels, and autoinhibitory modulation of CCR7-mediated chemotaxis. While truncation of the C-terminal tail induced chemical shift changes in the folded chemokine domain, the structural basis for its influence on CCL21 function remains largely unexplored. CCL21 concentration-dependent NMR chemical shifts revealed weak, nonphysiological self-association that mimics the truncation of the C-terminal tail. We generated a series of C-terminal truncation variants to dissect the C-terminus influence on CCL21 structure and receptor activation. Using NMR spectroscopy, we found that CCL21 residues 80-90 mediate contacts with the chemokine domain. In cell-based assays for CCR7 and ACKR4 activation, we also found that residues 92-100 reduced CCL21 potency in calcium flux, cAMP inhibition, and β-arrestin recruitment. Taken together, these structure-function studies support a model wherein intramolecular interactions with specific residues of the flexible C-terminus stabilize a less active monomer conformation of the CCL21. We speculate that the autoinhibitory intramolecular contacts between the C-terminal tail and chemokine body are disrupted by GAG binding and/or interactions with the CCR7 receptor to ensure optimal functionality.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Motifs
  • Calcium / metabolism
  • Chemokine CCL21 / chemistry*
  • Chemokine CCL21 / genetics
  • Chemokine CCL21 / metabolism*
  • Dendritic Cells / metabolism
  • Humans
  • Protein Binding
  • Receptors, CCR / genetics
  • Receptors, CCR / metabolism
  • Receptors, CCR7 / genetics
  • Receptors, CCR7 / metabolism

Substances

  • ACKR4 protein, human
  • CCL21 protein, human
  • Chemokine CCL21
  • Receptors, CCR
  • Receptors, CCR7
  • Calcium