Branch of Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry of the Russian Academy of Sciences, Science Avenue, 6, Pushchino, Moscow Region, 142290, Russia.
J Pept Sci. 2013 Aug;19(8):499-503. doi: 10.1002/psc.2527. Epub 2013 Jun 23.
The synthetic peptide octarphin (TPLVTLFK) corresponding to the sequence 12-19 of β-endorphin, a selective agonist of non-opioid β-endorphin receptor, was labeled with tritium to specific activity of 29 Ci/mmol. The analysis of [(3) H]octarphin binding to human T and B lymphocytes separated from normal human blood revealed the existence of one type of high-affinity binding sites (receptors): Kd 3.0 and 3.2 nM, respectively. Besides unlabeled octarphin, unlabeled β-endorphin possessed the ability to inhibit the specific binding of [(3) H]octarphin to Т and B lymphocytes (Ki 1.9 and 2.2 nМ, respectively). Tests of the specificity of the receptors revealed that they are not sensitive to naloxone, α-endorphin, γ-endorphin, [Met(5) ]enkephalin, and [Leu(5) ]enkephalin. Thus, both T and B lymphocytes from normal human blood express non-opioid receptor for β-endorphin. Binding of the hormone to the receptor provides a fragment 12-19.
人工合成的八肽（TPLVTLFK），对应β-内啡肽的 12-19 位序列，β-内啡肽是一种非阿片类β-内啡肽受体的选择性激动剂，用氚标记，比活度为 29 Ci/mmol。分析（3）H 标记的八肽与人 T 和 B 淋巴细胞的结合，这些细胞从正常人的血液中分离出来，揭示了存在一种高亲和力结合位点（受体）：Kd 分别为 3.0 和 3.2 nM。除了未标记的八肽外，未标记的β-内啡肽也具有抑制（3）H 标记的八肽与 T 和 B 淋巴细胞特异性结合的能力（Ki 分别为 1.9 和 2.2 nM）。受体特异性测试表明，它们对纳洛酮、α-内啡肽、γ-内啡肽、[Met(5)]脑啡肽和[Leu(5)]脑啡肽不敏感。因此，正常人血液中的 T 和 B 淋巴细胞均表达非阿片类β-内啡肽受体。激素与受体的结合提供了 12-19 位的片段。
