Extended Data Figure 2: BMS-681 binding may disrupt a chemokine-recognizing conformation of the CCR2 N terminus and helix I.
From: Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists
a, Model of CCR2–CCL2 built by homology from the structure of CXCR4–vMIP-II11 suggests that a productive chemokine-compatible conformation of the receptor requires re-orientation of the N terminus from almost parallel to almost perpendicular to the membrane plane, and formation of an extra helical turn in helix I to bring it closer to helix VII and ECL3. b, Binding of BMS-681 may disrupt this chemokine-compatible conformation by inserting between helices I and VII.
