Navolotskaya E V, Malkova N V, Zargarova T A, Lepikhova T N, Zav'yalov V P, Lipkin V M
Branch of Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry of the Russian Academy of Sciences, 142290, Pushchino, Moscow Region, Russia.
Peptides. 2001 Dec;22(12):2009-13. doi: 10.1016/s0196-9781(01)00563-0.
The synthetic decapeptide H-SLTCLVKGFY-OH (termed immunorphin) corresponding to the sequence 364-373 of the CH3 domain of human immunoglobulin G heavy chain was found to compete with [125I]beta-endorphin for high-affinity receptors on T lymphocytes from the blood of healthy donors (K(i) = 0.6 nM). Besides immunorphin, its synthetic fragments H-Val-Lys-Gly-Phe-Tyr-OH (K(i) = 15 nM), H-Leu-Val-Lys-Gly-Phe-Tyr-OH (K(i) = 8.0 nM), H-Cys-Leu-Val-Lys-Gly-Phe-Tyr-OH (K(i) = 3.4 nM), H-Thr-Cys-Leu-Val-Lys-Gly-Phe-Tyr-OH (K(i) = 2.2 nM), H-Leu-Thr-Cys-Leu-Val-Lys-Gly-Phe-Tyr-OH (K(i) = 1.0 nM) possessed the ability to inhibit specific binding of [125I]beta-endorphin to T lymphocytes. Tests of the specificity of the receptors revealed that they are not sensitive to naloxone and Met-enkephalin, i.e. they are not opioid receptors. K(d) values characterizing the specific binding of 125I- labeled immunorphin and its fragment H-Val-Lys-Gly-Phe-Tyr-OH to the receptors have been determined to be 7.4 nM and 36.3 nM, respectively.
合成十肽H-SLTCLVKGFY-OH(称为免疫吗啡肽)对应于人免疫球蛋白G重链CH3结构域的364-373序列,被发现可与[125I]β-内啡肽竞争健康供体血液中T淋巴细胞上的高亲和力受体(K(i)=0.6 nM)。除免疫吗啡肽外,其合成片段H-Val-Lys-Gly-Phe-Tyr-OH(K(i)=15 nM)、H-Leu-Val-Lys-Gly-Phe-Tyr-OH(K(i)=8.0 nM)、H-Cys-Leu-Val-Lys-Gly-Phe-Tyr-OH(K(i)=3.4 nM)、H-Thr-Cys-Leu-Val-Lys-Gly-Phe-Tyr-OH(K(i)=2.2 nM)、H-Leu-Thr-Cys-Leu-Val-Lys-Gly-Phe-Tyr-OH(K(i)=1.0 nM)均具有抑制[125I]β-内啡肽与T淋巴细胞特异性结合的能力。对受体特异性的测试表明,它们对纳洛酮和甲硫氨酸脑啡肽不敏感,即它们不是阿片受体。已确定表征125I标记的免疫吗啡肽及其片段H-Val-Lys-Gly-Phe-Tyr-OH与受体特异性结合的K(d)值分别为7.4 nM和36. nM。