Regular ArticleThe Molecular Basis of the Chemokine/Chemokine Receptor Interaction—Scope for Design of Chemokine Antagonists
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CCR5: Established paradigms and new frontiers for a ‘celebrity’ chemokine receptor
2018, CytokineCitation Excerpt :These ligands share the characteristic structural features common to chemokines: a rigidly structured core region, stabilized by disulfide bridges, from which a flexible N-terminal region is appended [71,72]. Interaction of CCR5 with its ligands occurs according to the two-site model that has been established as a general principal for chemokine – chemokine receptor interactions [72,73]. An ‘address’ interaction, which takes place between the extracellular domains of the receptor and the structured core domain of the chemokine (known as CRS1), provides high binding affinity and selectivity, and a ‘message’ interaction, which takes place between the transmembrane region of the receptor and the flexible N-terminal domain of the chemokine (known as CRS2), provides the capacity for receptor activation, by engaging the transmembrane domain of the receptor and eliciting the conformational changes that lead to signal transduction (Fig. 1).
Generating Chemokine Analogs with Enhanced Pharmacological Properties Using Phage Display
2016, Methods in EnzymologyCitation Excerpt :Chemokines share a characteristic tertiary structure featuring a folded core region, stabilized by disulfide bridges, from which appends a flexible N-terminal domain (Fernandez & Lolis, 2002) (Fig. 1). Numerous structure–activity studies have revealed a two-site mechanism for chemokine–chemokine receptor engagement (Fernandez & Lolis, 2002; Wells et al., 1996; Allen, Crown, & Handel, 2007). Initially, high-affinity and high-specificity engagement is achieved through an “address” interaction between the folded core region of the chemokine and the extracellular region of the chemokine receptor (also referred to as chemokine recognition site 1, CRS1 (Scholten et al., 2012)).
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