By interacting with the C-terminal Phe of apelin, Phe255 and Trp259 in helix VI of the apelin receptor are critical for internalization
Apelin is the endogenous ligand of the orphan seven-transmembrane domain (TM) G
protein-coupled receptor APJ. Apelin is involved in the regulation of body fluid homeostasis
and cardiovascular functions. We previously showed the importance of the C-terminal Phe of
apelin 17 (K17F) in the hypotensive activity of this peptide. Here, we show either by deleting
the Phe residue (K16P) or by substituting it by an Ala (K17A), that it plays a crucial role in
apelin receptor internalization but not in apelin binding or in Gα i-protein coupling. Then we …
protein-coupled receptor APJ. Apelin is involved in the regulation of body fluid homeostasis
and cardiovascular functions. We previously showed the importance of the C-terminal Phe of
apelin 17 (K17F) in the hypotensive activity of this peptide. Here, we show either by deleting
the Phe residue (K16P) or by substituting it by an Ala (K17A), that it plays a crucial role in
apelin receptor internalization but not in apelin binding or in Gα i-protein coupling. Then we …
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