Parathyroid hormone-like adenylate cyclase-stimulating proteins (hACSPs) have been implicated as one of the calcemic, bone-resorbing agents in patients with humoral hypercalcemia of malignancy. We report the synthesis of an amino-terminal hACSP fragment, Tyr36 hACSP (1-36) amide. The synthetic hACSP is a potent agonist of renal membrane adenylate cyclase (Km, 1.7 X 10(-10)) and of bone cell adenylate cyclase (Km 1 X 10(-9)M). It is a potent bone-resorbing agent in vitro, stimulating 45Ca release from fetal rat long bones at a concentration of 10(-9) M. When infused via osmotic minipumps into rats, it is also a potent calcemic factor in vivo, inducing a rise in serum calcium from (mean +/- SD) 10.6 +/- 0.6 to 19.7 +/- 3.2 mg/dl when infused at 1.4 micrograms/h and from 9.9 +/- 0.7 to 11.4 +/- 1.2 mg/dl when infused at 0.14 micrograms/h. These findings indicate that biologically active hACSP fragments can be synthesized. One such synthetic peptide possesses the in vitro and in vivo bioactivities demonstrated in native, tumor-derived hACSPs. It is also a potent calcemic, bone-resorbing agent.

译文

:甲状旁腺激素样腺苷酸环化酶刺激蛋白(hACSPs)已被认为是恶性体液性高钙血症患者的钙化,骨吸收剂之一。我们报告了氨基末端hACSP片段,Tyr36 hACSP(1-36)酰胺的合成。合成的hACSP是肾膜腺苷酸环化酶(Km,1.7 X 10(-10))和骨细胞腺苷酸环化酶(Km 1 X 10(-9)M)的有效激动剂。它是一种有效的骨吸收剂,在体外以10(-9)M的浓度刺激胎儿长骨中45Ca的释放。当通过渗透性微型泵注入大鼠体内时,它也是一种有效的钙化因子,可在体内诱导钙的释放。当以1.4微克/小时注入时,血清钙从(平均值/-标准差)从10.6 /-0.6增至19.7 /-3.2 mg / dl,当以0.14微克/小时注入时从9.9 /-0.7至11.4 /-1.2 mg / dl H。这些发现表明可以合成具有生物活性的hACSP片段。一种这样的合成肽具有在天然的,肿瘤来源的hACSP中证明的体外和体内生物活性。它也是强效的钙化,骨吸收剂。

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