Fig. 3.

Spiegelmer l-NOX-B11 binds the n-octanoylated N terminus of ghrelin. l-NOX-B11 requires the octanoylated N terminus of ghrelin for binding and inhibition. GHS-R1a-expressing CHO cells were stimulated with 10 nM ghrelin (A) or ghrelin-(1–5) (B) in the presence of 30 nM l-NOX-B11, 300 nM desoctanoyl ghrelin (d.-o. Ghr.), or both. Ca²⁺-associated fluorescence triggered by ghrelin's binding to the receptor was measured. (C) The sequence of rat ghrelin, showing the minimal binding motif for l-NOX-B11 (boxed) and the differing amino acids in the human sequence (shaded). See Results for details.