Navolotskaya E V, Zargarova T A, Lepikhova T N, Turobov V I, Nurieva R I, Malkova N V, Lipkin V M, Zav'yalov V P
Branch of Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino, Moscow Region, 142292, Russia.
Biochemistry (Mosc). 1999 Jul;64(7):758-64.
The synthetic ACTH-like decapeptide H-Val-Lys-Lys-Pro-Gly- Ser-Ser-Val-Lys-Val-OH, corresponding to amino acid residues 11-20 of the variable part of the human IgG1 heavy chain (referred to as immunocortin) was found to have an immunosuppressive effect on cells in vitro: it inhibits blast transformation of mouse thymocytes and reduces spontaneous motility of mouse peritoneal macrophages as well as their bactericidal activity against the virulent bacterial strain Salmonella typhimurium 415. Tritium-labeled immunocortin binds with high affinity to ACTH receptors on thymocytes and macrophages (Kd 2. 1 and 2.5 nM, respectively) and activates adenylate cyclase in these cells. Thus, the interaction of immunocortin with the target cell includes the following main steps: binding to the receptor, activation of adenylate cyclase, and elevation of the intracellular content of cAMP.
合成的促肾上腺皮质激素样十肽H-Val-Lys-Lys-Pro-Gly-Ser-Ser-Val-Lys-Val-OH，对应于人IgG1重链可变部分的第11至20位氨基酸残基（称为免疫皮质素），被发现对体外细胞具有免疫抑制作用：它抑制小鼠胸腺细胞的母细胞转化，并降低小鼠腹腔巨噬细胞的自发运动性及其对强毒菌株鼠伤寒沙门氏菌415的杀菌活性。氚标记的免疫皮质素与胸腺细胞和巨噬细胞上的促肾上腺皮质激素受体具有高亲和力结合（解离常数分别为2.1和2.5 nM），并激活这些细胞中的腺苷酸环化酶。因此，免疫皮质素与靶细胞的相互作用包括以下主要步骤：与受体结合、激活腺苷酸环化酶以及提高细胞内cAMP含量。
