Kather H, Simon B
Clin Chim Acta. 1976 Dec;73(3):497-504. doi: 10.1016/0009-8981(76)90153-4.
The effects of 5'-guanylyl-imidodiphosphate (GMP(PNP)) on the catecholamine-sensitive adenylate cyclase of human fat cell ghosts were studied. The compound increased basal and epinephrine-stimulated enzyme activity by about 300%; in addition GMP(PNP) increased hormone sensitivity by reducing the epinephrine concentration required, to produce half maximal stimulation. The rate of GMP(PNP)-induced activation was slow in onset and could be enhanced by epinephrine. The GMP(PNP)-activated state was resistant to thermal inactivation and could not be reversed by extensive washing. The application of this compound in clinical studies may be useful because of its stimulating and stabilizing action.
研究了5'-鸟苷酰亚氨基二磷酸(GMP(PNP))对人脂肪细胞膜泡中儿茶酚胺敏感的腺苷酸环化酶的影响。该化合物使基础和肾上腺素刺激的酶活性增加约300%;此外,GMP(PNP)通过降低产生半数最大刺激所需的肾上腺素浓度来提高激素敏感性。GMP(PNP)诱导的激活速率起始缓慢,肾上腺素可增强其激活速率。GMP(PNP)激活的状态对热失活具有抗性,且不能通过大量洗涤逆转。由于其刺激和稳定作用,该化合物在临床研究中的应用可能是有用的。