Batra S, Alenfall J
Kabi Pharmacia Oncology, University of Lund, Sweden.
Prostate. 1994 May;24(5):269-78. doi: 10.1002/pros.2990240509.
Using PK 11195, a high affinity ligand for peripheral benzodiazepine receptors (PBZr), binding sites in isolated mitochondrial (m-fraction) and microsomal fractions (p-fraction) from R-3327 Dunning AT-1 tumors, ventral and dorsolateral prostate were studied. Binding of PK 11195 in both m- and p-fractions from AT-1 tumors, but only in m-fraction from ventral and dorsolateral prostate, was specific, saturable, and of high affinity. The PBZr density in m-fraction from AT-1 tumor was 6-fold and 20-fold higher than that in ventral and dorsolateral prostate, respectively. The receptor density in p-fraction from AT-1 tumors was approximately 25% of that found in the m-fraction. Clear differences were observed in the competition by both diazepam and flunitrazepam for binding sites in m- and p-fractions from tumors. These data indicate that the receptors were not only localized to the mitochondria, but were also present in considerable amounts in the microsomal fractions. The unusually high amounts of receptors in the fast growing anaplastic prostatic tumor suggest their involvement in the regulation of cell proliferation and possibly in tumorigenesis.
使用外周苯二氮䓬受体（PBZr）的高亲和力配体PK 11195，研究了来自R-3327邓宁AT-1肿瘤、腹侧和背外侧前列腺的分离线粒体（m组分）和微粒体组分（p组分）中的结合位点。PK 11195在AT-1肿瘤的m组分和p组分中均有结合，但仅在腹侧和背外侧前列腺的m组分中有特异性、可饱和且高亲和力的结合。AT-1肿瘤m组分中的PBZr密度分别比腹侧和背外侧前列腺中的高6倍和20倍。AT-1肿瘤p组分中的受体密度约为m组分中的25%。观察到地西泮和氟硝西泮对肿瘤m组分和p组分中结合位点的竞争存在明显差异。这些数据表明，受体不仅定位于线粒体，在微粒体组分中也有相当数量的存在。快速生长的间变性前列腺肿瘤中异常大量的受体表明它们参与细胞增殖的调节，可能还参与肿瘤发生。
