Lalwani N D, Fahl W E, Reddy J K
Biochem Biophys Res Commun. 1983 Oct 31;116(2):388-93. doi: 10.1016/0006-291x(83)90534-x.
[3H]nafenopin, a known inducer of liver peroxisomal enzymes, was shown to bind to a specific, saturable pool of binding sites in cytosols from rat liver and kidney cortex. Tissue levels of this binding protein (liver greater than kidney cortex; not detectable in myocardium, skeletal muscle) were seen to correlate with the ability of nafenopin to induce peroxisomal enzymes in these organs. Clofibrate and ciprofibrate, which are structurally similar to nafenopin, competitively blocked the specific binding of [3H]nafenopin. Phenobarbital, a non-inducer of peroxisomes, and [4-chloro-6-(2,3-xylidino)-2-pyrimidinylthio]acetic acid and 4-chloro-6-(2,3-xylidino)-2-pyrimidinylthio(N-beta-hydroxyethyl)acetamide, which are structurally unrelated peroxisome proliferators, did not complete for the specific [3H]nafenopin binding sites. The [3H]nafenopin binding protein is proposed as a mediator of the drug-induced increase in peroxisomes and associated peroxisomal enzymes.
[3H]萘酚平是一种已知的肝脏过氧化物酶体酶诱导剂，它被证明能与大鼠肝脏和肾皮质胞质溶胶中特定的、可饱和的结合位点池结合。这种结合蛋白的组织水平（肝脏大于肾皮质；在心肌、骨骼肌中未检测到）与萘酚平在这些器官中诱导过氧化物酶体酶的能力相关。与萘酚平结构相似的氯贝丁酯和环丙贝特竞争性地阻断了[3H]萘酚平的特异性结合。苯巴比妥是一种过氧化物酶体非诱导剂，以及结构上不相关的过氧化物酶体增殖剂[4-氯-6-(2,3-二甲基苯胺基)-2-嘧啶硫基]乙酸和4-氯-6-(2,3-二甲基苯胺基)-2-嘧啶硫基(N-β-羟乙基)乙酰胺，它们不与特异性的[3H]萘酚平结合位点竞争。[3H]萘酚平结合蛋白被认为是药物诱导的过氧化物酶体及相关过氧化物酶体酶增加的介质。
