title: Major pharmacological distinction of the ACTH receptor from other melanocortin receptors.
abstract: The mouse adrenocortical cell line Y1, that expresses ACTH receptors (MC2R), was used to probe the binding of ACTH and MSH peptides by using radio-labelled ACTH (1-39). The Y1 cells were found to bind [125I]-labelled ACTH (1-39) with high affinity (Kd approximately 130 pM). However, none of the melanocortin peptides NDP-MSH, alpha-MSH, beta-MSH or gamma 1-MSH could compete with the binding of the labelled ACTH(1-39). When other MC receptor subtype DNAs (MC1, MC3 and MC4) were transfected into the Y1 cells, characteristic binding of the [125I]NDP-MSH appeared for each of the receptor subtype, but no specific binding was present in non-transfected cells. This is the first report clearly demonstrating that the ACTH receptor binds only ACTH, but not other melanocortin peptides.
authors: Department of Pharmaceutical Pharmacology, Uppsala University, Sweden.
authors: H B
authors: HB
authors: Schiöth
authors: V
authors: V
authors: Chhajlani
authors: R
authors: R
authors: Muceniece
authors: V
authors: V
authors: Klusa
authors: J E
authors: JE
authors: Wikberg
mesh_terms: D000302:Adrenal Cortex / Q000378:metabolism; D000324:Adrenocorticotropic Hormone / Q000378:metabolism; D000818:Animals; D002460:Cell Line; D006801:Humans; D007457:Iodine Radioisotopes; D009074:Melanocyte-Stimulating Hormones / Q000378:metabolism; D051379:Mice; D010455:Peptides / Q000378:metabolism; D011869:Radioligand Assay; D018043:Receptors, Corticotropin / Q000378:metabolism*; D044101:Receptors, Melanocortin
chemical_list: D007457:Iodine Radioisotopes; D010455:Peptides; D018043:Receptors, Corticotropin; D044101:Receptors, Melanocortin; D000324:Adrenocorticotropic Hormone; D009074:Melanocyte-Stimulating Hormones