Imai A, Ohno T, Iida K, Fuseya T, Furui T, Tamaya T
Department of Obstetrics and Gynecology, Gifu University School of Medicine, Japan.
Gynecol Oncol. 1994 Oct;55(1):144-8. doi: 10.1006/gyno.1994.1264.
In support of a possible clinical use of gonadotropin-releasing hormone (Gn-RH) analogs in the treatment of the endometrial carcinoma, this study was undertaken to establish the presence and characteristics of Gn-RH receptor on endometrial cancer. Materials were human endometrial carcinomas surgically removed and endometrial carcinoma cell lines. Gn-RH receptor was characterized by [3H]Gn-RH binding to plasma membrane preparations. Gn-RH receptor messenger ribonucleic acid (mRNA) was determined by reverse transcription-polymerase chain reaction (PCR) using oligonucleotide primers synthesized according to the published human Gn-RH receptor sequence. Specific Gn-RH binding sites were shown to be present in 16 of 18 well-differentiated and 4 of 7 poorly differentiated adenocarcinoma specimens (Kd = 5.89 +/- 3.59 nM, Bmax = 1.80 +/- 0.95 pmol/mg protein) and cell lines RL95-2 and HHUA with Kd of 2.38 +/- 0.86 nM. The high-affinity binding sites were also detected in six proliferative-phase endometrium (Kd = 4.24 +/- 2.32 nM, Bmax = 2.73 +/- 1.12 pmol/mg protein). Gn-RH receptor mRNA was detected in all endometrial carcinoma and endometrial specimens and cell lines where the specific binding sites were detected, but not in adenomyosis or myometrial samples. The expression of Gn-RH receptor provides a possible point of attack for therapeutic approaches using Gn-RH analogs in this malignancy.
为了支持促性腺激素释放激素（Gn-RH）类似物在子宫内膜癌治疗中可能的临床应用，本研究旨在确定子宫内膜癌中Gn-RH受体的存在及其特征。材料包括手术切除的人子宫内膜癌组织和子宫内膜癌细胞系。通过[3H]Gn-RH与质膜制剂的结合来表征Gn-RH受体。使用根据已发表的人Gn-RH受体序列合成的寡核苷酸引物，通过逆转录-聚合酶链反应（PCR）测定Gn-RH受体信使核糖核酸（mRNA）。结果显示，18例高分化腺癌标本中有16例、7例低分化腺癌标本中有4例以及细胞系RL95-2和HHUA存在特异性Gn-RH结合位点（解离常数Kd = 5.89 +/- 3.59 nM，最大结合容量Bmax = 1.80 +/- 0.95 pmol/mg蛋白），细胞系RL95-2和HHUA的Kd为2.38 +/- 0.86 nM。在六个增殖期子宫内膜中也检测到高亲和力结合位点（Kd = 4.24 +/- 2.32 nM，Bmax = 2.73 +/- 1.12 pmol/mg蛋白）。在所有检测到特异性结合位点的子宫内膜癌组织、子宫内膜标本和细胞系中均检测到Gn-RH受体mRNA，但在子宫腺肌病或子宫肌层样本中未检测到。Gn-RH受体的表达为在这种恶性肿瘤中使用Gn-RH类似物的治疗方法提供了一个可能的攻击点。
