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Identification of endothelin receptors in normal and hyperplasic human prostate tissues
Author(s) -
Le Brun Gaëlle,
Moldovan Florina,
Aubin Philippe,
Ropiquet Frédéric,
Cussenot Olivier,
Fiet Jean
Publication year - 1996
Publication title -
the prostate
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.295
H-Index - 123
eISSN - 1097-0045
pISSN - 0270-4137
DOI - 10.1002/(sici)1097-0045(199606)28:6<379::aid-pros7>3.0.co;2-5
Subject(s) - receptor , endothelin receptor , prostate , population , chemistry , endothelin 1 , microbiology and biotechnology , endocrinology , medicine , biology , environmental health , cancer
Specific endothelin‐1 (ET1) binding sites have been demonstrated in membranes derived from normal (NP) and benign hyperplasic (BPH) human prostate using an 125 I‐ET1 binding assay. 125 I saturation experiments and Scatchard analysis demonstrated the existence of a homogeneous population of binding sites with high affinity (Kd app ) and density (B max ), respectively, 106 ± 15 pM and 1086 ± 399 fmol/mg protein for NP (n = 5) and 168 ± 26 pM and 964 ± 445 fmol/mg protein for BPH (n = 5). We demonstrated the presence of two subtypes of ET1 receptors, ETA and ETB, by means of the following ET1 competitors: ET2, ET3, and BQ123 (which is selective for the ETA receptor), and IRL1620 and sarafotoxine c (S6c) (which are selective for the ETB receptor). The displacement curves allowed us to conclude that the large majority (85%) of the ET1 receptors in normal and hyperplasic human prostate are of the A subtype. © 1996 Wiley‐Liss, Inc.