Abstract
Calcitonin gene-related peptide (CGRP) receptor activity was studied in WE-68 human Ewing's sarcoma cells. 125I-human CGRP bound in a time-dependent, reversible and saturable manner. Scatchard plots were compatible with the presence of a homogenous population of CGRP receptors with high affinity ( K d = 15 pM, and B max = 1.9 fmol mg protein). The potency order of unlabeled peptides, in the presence of radioligand, was: human CGRP-II > human CGRP = chick CGRP > rat CGRP = rat [Tyr o]CGRP > human [Tyr o] CGRP > > salmon calcitonin (CT) > rat [Tyr o]CGRP-(28-37). Each peptide except CT and [Tyi o]CGRP-(28-37) stimulated cyclic AMP generation in a concentration-dependent manner, and the relative potencies paralleled their relative ability in inhibiting 125I-human CGRP binding. We conclude that WE-68 Ewing's sarcoma cells express genuine CGRP receptors which upon activation lead to stimulation of cyclic AMP formation. Calcitonin gene-related peptide; Calcitonin; cyclic AMP; (Human; Ewing's sarcoma cell)
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