Abstract
The family of G protein-coupled receptors that includes receptors for motilin, ghrelin, and growth hormone secretagogue has substantial potential importance as drug targets. Understanding of the molecular basis of hormone binding and receptor activation should provide insights that are helpful in the development of such drugs. We previously examined the unique second extracellular loop domain of the motilin receptor, identifying key epitopes in perimembranous locations at each end of this long loop (Matsuura, B., Dong, M., and Miller, L. J. (2002) J. Biol. Chem. 277, 9834-9839). Here, we have extended that work, examining the other predicted extracellular domains of the motilin receptor by using sequential deletions of segments ranging from one to six amino acid residues and site-directed alanine replacement mutagenesis approaches. Each construct was transiently expressed in COS cells, and characterized for motilin- and erythromycin-stimulated intracellular calcium responses and motilin radioligand binding. Only those receptor segments that included key Cys residues in positions 25, 30, and 111 or perimembranous regions at the ends of the amino terminus and the first and third extracellular loops disrupted motilin biological ac...Continue Reading
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