ISSN:
1420-9071
Keywords:
Phorbol ester receptor
;
desensitization
;
transformed human urothelial cell line
;
human urinary bladder carcinogenesis
Source:
Springer Online Journal Archives 1860-2000
Topics:
Biology
,
Medicine
Notes:
Abstract The presence of specific binding sites for phorbol esters was studied in a transformed but non-tumorigenic human urothelial cell line HCV-29 by assay of specific binding of3H-phorbol-12,13-dibutyrate (3H-PDBu) to intact living cells.3H-PDBu bound specifically to HCV-29 cells in a saturable and competitive manner. Scatchard plot analysis of specific binding yielded a curved plot consistent with two binding sites with Kd of 11 nM and 102 nM, respectively. At saturation the corresponding PDBu binding capacities (Bmax) were 8.8 pmol/106 cells (5.2×106 molecules bound per cell) and 2.8 pmol/106 cells (1.7×106 molecules bound per cell).3H-PDBu binding was displaced by biologically active phorbol ester tumor promoters such as 12-O-tetradecanoylphorbol-13-acetate (TPA) and mezerein,but not by tumor promoters such as L-tryptophan, anthranilic acid and sodium saccharin. In cells desensitized by pretreatment with 1 μg/ml (2μM) TPA or PDBu for 24 h the level of binding was reduced to 28% of the level in non-exposed cells. The ability of desensitized cells to bind3H-PDBu was gradually restored within 5–6 days. At the same time the cells became sensitive to the morphological alteration induced by PDBu. This suggests that desensitization of HCV-29 cells is due to a decreased receptor-ligand binding capacity probably associated with down regulation of the phorbol ester receptors.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01928796
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