Functional characteristics of calcitonin gene-related peptide receptors in human Ewing's sarcoma WE-68 cells.
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 (Kd = 15 pM, and Bmax = 1.9 fmol/mg protein). The potency order of unlabeled peptides in the presence of radioligand, was: human CGRP-II greater than human CGRP = chick CGRP greater than rat CGRP = rat [Tyr0]CGRP greater than human [Tyr0] CGRP much greater than salmon calcitonin (CT) greater than rat [Tyr0]CGRP-(28-37). Each peptide except CT and [Tyr0]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
van Valen
F
F
Universitätskinderklinik, Abt. für Hämatologie und Onkologie, Düsseldorf, FRG.
Keck
E
E
Jürgens
H
H
D000818:Animals; D015740:Calcitonin Gene-Related Peptide / Q000494:pharmacology*; D002645:Chickens; D000242:Cyclic AMP / Q000096:biosynthesis; D006801:Humans; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects* / Q000378:metabolism; D012474:Salmon; D012512:Sarcoma, Ewing / Q000378:metabolism*; D013045:Species Specificity; D014407:Tumor Cells, Cultured
D011956:Receptors, Cell Surface; D000242:Cyclic AMP; D015740:Calcitonin Gene-Related Peptide