Heavner G A, Audhya T, Kroon D, Goldstein G
Arch Biochem Biophys. 1985 Oct;242(1):248-55. doi: 10.1016/0003-9861(85)90499-0.
Thymopentin, the synthetic pentapeptide Arg-Lys-Asp-Val-Tyr, corresponds to residues 32-36 of the thymic hormone thymopoietin. Thymopentin, like thymopoietin, induces intracellular cGMP elevations in the human T-cell line, CEM. Thymopentin also displaces radiolabeled thymopoietin from a receptor glycoprotein prepared from CEM cells, provided that a nonapeptide corresponding to thymopoietin is added to block thymopoietin binding to an additional binding site. Twenty nine analogs with single position substitutions were synthesized by solid-phase or classical solution synthesis, and are evaluated in these assays. All analogs that were active gave positive effects in both assays. A number of substitutions were tolerated at positions 2, 4, and 5, but there was an absolute requirement for L- or D-Arg at position 1 and L- or D-Asp at position 3 to maintain biological activity.
胸腺五肽，即合成的五肽精氨酸-赖氨酸-天冬氨酸-缬氨酸-酪氨酸，相当于胸腺激素促胸腺生成素的32 - 36位氨基酸残基。与促胸腺生成素一样，胸腺五肽可诱导人T细胞系CEM细胞内的环鸟苷酸（cGMP）升高。胸腺五肽还能从CEM细胞制备的受体糖蛋白上取代放射性标记的促胸腺生成素，前提是添加一种与促胸腺生成素对应的九肽来阻断促胸腺生成素与另一个结合位点的结合。通过固相或经典溶液合成法合成了29种单一位点取代的类似物，并在这些试验中进行了评估。所有具有活性的类似物在两种试验中均产生了积极效果。2、4和5位可耐受多种取代，但1位的L-或D-精氨酸以及3位的L-或D-天冬氨酸对于维持生物活性是绝对必需的。
