title: Localization and characterization of endothelin-1 receptor binding in the blood vessels of human pulmonary tumors.
abstract: We have demonstrated endothelin-1 (ET-1) binding sites in the blood vessels of human pulmonary tumors by in vitro autoradiography. The blood vessels of the tumors were confirmed by immunostaining with von Willebrand factor. Specific [125I]ET-1 binding was identified in the blood vessels of all sizes in both tumor and stromal tissues. Nonspecific binding was observed in squamous cell carcinomas and in carcinoids. The ET-1 binding in blood vessels was specific, saturable, and time-dependent. The binding reached equilibrium at 120 min. Scatchard analysis of [125I]ET-1 binding to sections of blood vessels of squamous cell carcinoma indicated binding to a single class of binding sites, with a dissociation constant (Kd) of 0.16 nM and a maximal density of binding sites (Bmax) of 126 amol/mm2. The binding was competitively inhibited by ET-1 >> VIC > ET-2 > sarafotoxin (SRb) > ET-3 but not by other unrelated peptides. Our results provide evidence that ET-1 binding is localized in the blood vessels of pulmonary tumors and in stromal tissues surrounding the tumor nest. ET may play a role in the angiogenesis of tumor growth.
authors.affiliation: Department of Histochemistry, Royal Postgraduate Medical School, London, England.
authors.forename: Y D
authors.initials: YD
authors.lastname: Zhao
authors.forename: D R
authors.initials: DR
authors.lastname: Springall
authors.forename: Q
authors.initials: Q
authors.lastname: Hamid
authors.forename: M
authors.initials: M
authors.lastname: Levene
authors.forename: J M
authors.initials: JM
authors.lastname: Polak
mesh_terms: D001345:Autoradiography; D001808:Blood Vessels / Q000737:chemistry*; D016232:Endothelins / Q000378:metabolism; D006801:Humans; D008175:Lung Neoplasms / Q000098:blood supply*; D009389:Neovascularization, Pathologic; D017466:Receptors, Endothelin / Q000032:analysis* / Q000378:metabolism
chemical_list: D016232:Endothelins; D017466:Receptors, Endothelin