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Cadmium directly acts on endothelin receptor and inhibits endothelin binding activity
Author(s) -
Wada Kenji,
Fujii Yukako,
Watanabe Hiroshi,
Satoh Misako,
Furuichi Yasuhiro
Publication year - 1991
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(91)80727-k
Subject(s) - ethylenediaminetetraacetic acid , receptor , chemistry , endothelin receptor , cadmium , chelation , biochemistry , microbiology and biotechnology , biophysics , biology , organic chemistry
The binding of endothelin (ET) to human placenta ET receptor was strongly inhibited by cadmium ions (Cd 2+ ) (IC 50 = 2 × 10 −5 M). Experiments with affinity cross‐linking showed that the major 40 kDa receptor was inhibited to form a [ 125 I]ET‐1/receptor complex. The mode of inhibition was noncompetitive with respect to ET‐1. The inhibitory effect of Cd 2+ on solubilized ET receptor was partially reversed by the chelating agent, ethylenediaminetetraacetic acid (EDTA), whereas the effect was irreversible for the membrane‐associated receptor. The rat aorta contractions by ET were prevented by pretreatment or addition of Cd 2+ .