Zav'yalov V P, Maiorov V A, Safonova N G, Navolotskaya E V, Abramov V M
Institute of Immunology, Moscow Region, Chekhov District, Russia.
Immunol Lett. 1995 May;46(1-2):125-8. doi: 10.1016/0165-2478(95)00030-9.
The octapeptide Gly-Lys-Val-Leu-Lys-Lys-Arg-Arg (termed leukocorticotropin, LCT) corresponding to the ACTH-like sequence 81-88 of human pro-interleukin-1 alpha and its derivative Tyr-Gly-Lys-Val-Leu-Lys-Lys-Arg-Arg were synthesized. The 125I-labeled Tyr-LCT specifically interacts with one type of receptor on the surface of murine splenocytes (Kd = (1.45 +/- 0.04) x 10(-8) M, the number of binding sites is equal to 4500) and with two types of receptors on the surface of murine peritoneal macrophages (Kd1 = (5.9 +/- 1.0) x 10(-9) M and Kd2 = (2.6 +/- 2.2) x 10(-7) M). LCT and Tyr-LCT significantly increase the adenylate cyclase activity of murine peritoneal macrophages. The receptor binding and adenylate cyclase stimulation activity of LCT and Tyr-LCT are inhibited by ACTH (13-24).
合成了与人白细胞介素-1α前体81 - 88位促肾上腺皮质激素（ACTH）样序列相对应的八肽甘氨酸-赖氨酸-缬氨酸-亮氨酸-赖氨酸-赖氨酸-精氨酸-精氨酸（称为白细胞促肾上腺皮质激素，LCT）及其衍生物酪氨酸-甘氨酸-赖氨酸-缬氨酸-亮氨酸-赖氨酸-赖氨酸-精氨酸-精氨酸。125I标记的酪氨酸-LCT特异性地与小鼠脾细胞表面的一种受体相互作用（解离常数Kd = (1.45 ± 0.04)×10(-8) M，结合位点数等于4500），并与小鼠腹腔巨噬细胞表面的两种受体相互作用（Kd1 = (5.9 ± 1.0)×10(-9) M和Kd2 = (2.6 ± 2.2)×10(-7) M）。LCT和酪氨酸-LCT显著增加小鼠腹腔巨噬细胞的腺苷酸环化酶活性。LCT和酪氨酸-LCT的受体结合及腺苷酸环化酶刺激活性受到ACTH（13 - 24）的抑制。
