Forskolin requires more than the catalytic unit to activate adenylate cyclase
Forskolin requires more than the catalytic unit to activate adenylate cyclase
复制标题
毛喉素需要的不仅仅是催化单元来激活腺苷酸环化酶
DOI：
10.1016/0303-7207(82)90155-1
复制
发表时间：
1982
影响因子：
4.1
通讯作者：
J. Hanoune
中科院分区：
文献类型：
--
作者：
D. Stengel;L. Guenet;M. Desmier;P. Insel;J. Hanoune
Forskolin 是一种天然二萜，是多种腺苷酸环化酶系统的新型、有效激活剂；其作用机制和作用部位仍存在争议。我们在此报告，虽然毛喉素可激活肝腺苷酸环化酶高达 15 倍，但它不会激活包含纯催化亚基的公羊精子的环化酶。然而，在用富含调节成分的人红细胞膜重建后，可以观察到毛喉素对精子腺苷酸环化酶活性的激活。二萜微弱地（3-5倍）激活大鼠和公羊睾丸中发现的胞质可溶性环化酶，但当通过凝胶色谱纯化环化酶时，这种作用消失了。我们的数据与毛喉素直接作用于催化亚基的假设不相符，而是表明它通过另一个调节成分（GTP 结合调节复合物的一部分或不同于 GTP 结合调节复合物）发挥作用。
Forskolin, a natural diterpene, is a novel, potent activator of a variety of adenylate cyclase systems; its mechanism and site of action are still disputed. We report here that, while forskolin activates liver adenylate cyclase up to 15-fold, it does not activate cyclase of ram sperm which comprises a pure catalytic subunit. However, forskolin activation of sperm adenylate cyclase activity could be observed after reconstitution with the regulatory component-enriched membrane from human erythrocytes. The diterpene weakly (3–5-fold) activated the cytosolic, soluble cyclase found in rat and ram testes, but this effect was lost when the cyclase was purified by gel chromatography. Our data are not compatible with the hypothesis that forskolin acts directly on the catalytic subunit, but rather suggest that it acts via another regulatory component, part of, or different from, the GTP-binding regulatory complex.