INVITRO AND INVIVO ANTAGONISTS AGAINST PARATHYROID HORMONE-RELATED PROTEIN
INVITRO AND INVIVO ANTAGONISTS AGAINST PARATHYROID HORMONE-RELATED PROTEIN
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DOI：
10.1016/0006-291x(89)92826-x
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发表时间：
1989-02-15
影响因子：
3.1
通讯作者：
ABE, K
中科院分区：
文献类型：
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作者：
NAGASAKI, K;YAMAGUCHI, K;ABE, K
合成了四种甲状旁腺激素相关蛋白（PTHrP）类似物：PTHrP（7-34）NH2，（10-34）NH2，（15-34）NH2和（20-34）NH2，并在体外和体内检测了它们对PTHrP（1-34）的拮抗活性。体外研究表明，所有四种类似物均可拮抗大鼠骨肉瘤细胞 (ROS 17/2.8) 中 PTHrP 刺激的环 AMP 产生，并且 PTHrP(7-34)NH2 和 PTHrP(10-34)NH2 具有有效的拮抗活性。裸鼠体内实验还表明，PTHrP(7-34)NH2完全抑制PTHrP(1-34)诱导的高钙血症，表明这些类似物在体外和体内拮抗PTHrP(1-34)的作用。
Four analogues of parthyroid hormone-related protein (PTHrP), PTHrP(7-34)NH2, (10-34)NH2, (15-34)NH2 and (20-34)NH2, were synthesized and their antagonistic activity against PTHrP (1-34) was examined in vitro and in vivo. In vitro studies revealed that all four analogues antagonized PTHrP-stimulated cyclic AMP production in rat osteosarcoma cells (ROS 17/2.8), and that PTHrP(7-34)NH2 and PTHrP(10-34)NH2 had potent antagonistic activity. In vivo experiments in nude mice also revealed that PTHrP(7-34)NH2 completely inhibited hypercalcemia induced by PTHrP(1-34), indicating that these analogues antagonize the effects of PTHrP(1-34) in vitro and in vivo.