Denes L, Szende B, Ember J, Major J, Szporny L, Hajos G, Nyeki O, Schon I, Lapis K, Kisfaludy L
Chemical Works of Gedeon Richter, Ltd., Budpest, Hungary.
Immunopharmacol Immunotoxicol. 1987;9(1):1-18. doi: 10.3109/08923978709035198.
The effects of seventeen synthetic analogs of thymopentin (TP-5) have been studied in the active and azathioprine-inhibited E-rosette tests. Thymopentin was gradually shortened from the C terminus to peptides and single amino acids. Thymopoietin 32-34 (Arg-Lys-Asp-RGH-0205-TP-3) (II) and thymopoietin 32-35 (Arg-Lys-Asp-Val-RGH-0206-TP-4) (I) were the most active peptides. Dipeptide Arg-Lys produced significant stimulatory effect on azathioprine (ED75) inhibited E-receptor. Treatment of azathioprine (ED75)-inhibited E-rosette forming cells (ERFC) with arginine or especially lysine increased the number of ERFC. Some of TP-4 analogs decreased further the number of ERFC decreased by azathioprine ED30. These "suppressive" peptides as well as TP-3 caused a partial arrest of K 562 cell proliferation up to 96 hours. Results suggest that TP-5 is not the smallest active fragment of thymopoietins, since peptides (TP-3 and TP-4) exhibit similar or higher T-cell membrane activation on E-receptor. Arginine, lysine, and acidic aspartyl residue seem to be a necessary basic structure to produce a cumulative chemical signal on the activity of T-lymphocytes.
在活性和硫唑嘌呤抑制的E花环试验中，研究了胸腺五肽（TP-5）的17种合成类似物的作用。胸腺五肽从C末端逐渐缩短为肽段和单个氨基酸。胸腺生成素32-34（精氨酸-赖氨酸-天冬氨酸-RGH-0205-TP-3）（II）和胸腺生成素32-35（精氨酸-赖氨酸-天冬氨酸-缬氨酸-RGH-0206-TP-4）（I）是活性最强的肽段。二肽精氨酸-赖氨酸对硫唑嘌呤（ED75）抑制的E受体产生显著的刺激作用。用精氨酸或特别是赖氨酸处理硫唑嘌呤（ED75）抑制的E花环形成细胞（ERFC）可增加ERFC的数量。一些TP-4类似物进一步减少了硫唑嘌呤ED30导致减少的ERFC数量。这些“抑制性”肽段以及TP-3可使K 562细胞增殖部分停滞长达96小时。结果表明，TP-5不是胸腺生成素最小的活性片段，因为肽段（TP-3和TP-4）在E受体上表现出相似或更高的T细胞膜激活作用。精氨酸、赖氨酸和酸性天冬氨酰残基似乎是在T淋巴细胞活性上产生累积化学信号的必要基本结构。
