1ilq

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CXCR-1 N-TERMINAL PEPTIDE BOUND TO INTERLEUKIN-8 (MINIMIZED MEAN)

Contents 1 Overview 2 Disease 3 About this Structure 4 Reference

Overview

BACKGROUND: Interactions between CXC chemokines (e.g. interleukin-8, IL-8), and their receptors (e.g. CXCR-1) have a key role in host defense and, disease by attracting and upregulating neutrophils to sites of, inflammation. The transmembrane nature of the receptor impedes, structure-based understanding of ligand interactions. Linear peptides, based on the N-terminal, extracellular portion of the receptor CXCR-1 do, bind to IL-8, however, and inhibit the binding of IL-8 to the full-length, receptor. RESULTS: The NMR solution structure of the complex formed, between IL-8 and one such receptor-based peptide indicates that a cleft, between a loop and a beta hairpin constitute part of the receptor, interaction surface on IL-8. Nine residues from the C terminus of the, receptor peptide (corresponding to Pro21-Pro29 of CXCR-1) occupy the cleft, in an extended fashion. Intermolecular contacts are mostly hydrophobic and, sidechain mediated. CONCLUSIONS: The results offer the first details at an, atomic level of the interaction between a chemokine and its receptor., Consideration of other biochemical data allow extrapolation to a model for, the interaction of IL-8 with the full-length receptor. In this model, the, heparin-binding residues of IL-8 are exposed, thereby allowing, presentation of the chemokine from endothelial cell-surface, glycosaminoglycans. This first glimpse of how IL-8 binds to its receptor, provides a foundation for the structure-based design of chemokine, antagonists.

Disease

Known diseases associated with this structure: AIDS, slow progression to OMIM:[146929]

About this Structure

1ILQ is a Protein complex structure of sequences from Homo sapiens with ACE and NH2 as ligands. Full crystallographic information is available from OCA.

Reference

Structure of a CXC chemokine-receptor fragment in complex with interleukin-8., Skelton NJ, Quan C, Reilly D, Lowman H, Structure. 1999 Feb 15;7(2):157-68. PMID:10368283

Page seeded by OCA on Mon Nov 12 17:31:21 2007