Nagasaka A, Hidaka H
J Clin Endocrinol Metab. 1980 Apr;50(4):726-33. doi: 10.1210/jcem-50-4-726.
Thyroid tissue was found to contain at least least two separable cyclic 3',5'-nucleotide phosphodiesterase (cAMP-PDE and cGMP-PDE) activities, as determined by DEAE-cellulose or Sepharose 6B column chromatography. These activities were cAMP- and cGMP-hydrolyzing enzymes. Quantitative differences of cAMP or cGMP hydrolytic activity were observed in tissues from patients with thyroid disorders. Theophylline, modulator protein, and Mg2+ produced similar effects on cAMP or cGMP hydrolytic activity in tissues from patients with a without various thyroid disorders. The mode of the inhibitory effect of cyclic nucleotides on PDE activities in thyroid tissues was competitive, in contrast to the mode seen in other organs. Both cAMP and cGMP hydrolytic activities were elevated in the tissues from patients with hyperthyroidism and thyroid carcinoma compared with the activity in controls. cGMP hydrolysis in hyperthyroidism was 4.4-fold higher than that seen in the controls. The ratio cGMP to cAMP hydrolysis was highest in cases of hyperthyroidism and lowest in cases of thyroid carcinoma, when PDE activities were determined with a substrate concentration of 0.4 microM. Kinetic analysis revealed that higher PDE activity in tissues from patients with hyperthyroidism and thyroid carcinoma was due to an increase in maximal velocity. The apparent Km values for hydrolysis of cyclic nucleotides were similar in normal and pathological thyroid tissues.
通过DEAE - 纤维素或琼脂糖6B柱色谱法测定发现,甲状腺组织至少含有两种可分离的环3',5'-核苷酸磷酸二酯酶(cAMP - PDE和cGMP - PDE)活性。这些活性是cAMP和cGMP水解酶。在甲状腺疾病患者的组织中观察到cAMP或cGMP水解活性的定量差异。茶碱、调节蛋白和Mg2+对患有或未患有各种甲状腺疾病患者的组织中的cAMP或cGMP水解活性产生相似的影响。与在其他器官中看到的模式相反,环核苷酸对甲状腺组织中PDE活性的抑制作用模式是竞争性的。与对照组相比,甲状腺功能亢进症和甲状腺癌患者组织中的cAMP和cGMP水解活性均升高。甲状腺功能亢进症中的cGMP水解比对照组高4.4倍。当用0.4 microM的底物浓度测定PDE活性时,cGMP与cAMP水解的比率在甲状腺功能亢进症病例中最高,在甲状腺癌病例中最低。动力学分析表明,甲状腺功能亢进症和甲状腺癌患者组织中较高的PDE活性是由于最大速度增加。正常和病理甲状腺组织中环核苷酸水解的表观Km值相似。