Cadmium directly acts on endothelin receptor and inhibits endothelin binding activity

FEBS Letters

Fujii, Yukako¹  Furuichi, Yasuhiro¹  Watanabe, Hiroshi²  Satoh, Misako¹  Wada, Kenji¹ 

[1] Department of Molecular Genetics, Nippon Roche Research Center, Kajiwara 200, Kamakura 247, Japan;Department of Pharmacology, Nippon Roche Research Center, Kajiwara 200, Kamakura 247, Japan

关键词: Vaso constriction;    Hypertension;    Hypotension;    Human placenta;    Divalent metals;    Chelating agent;   

DOI  :  10.1016/0014-5793(91)80727-K

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The binding of endothelin (ET) to human placenta ET receptor was strongly inhibited by cadmium ions (Cd²⁺) (IC₅₀ = 2 × 10⁻⁵ M). Experiments with affinity cross-linking showed that the major 40 kDa receptor was inhibited to form a [¹²⁵I]ET-1/receptor complex. The mode of inhibition was noncompetitive with respect to ET-1. The inhibitory effect of Cd²⁺ 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 Cd²⁺.

【 授权许可】

Unknown