SYNTHESIS AND CHARACTERIZATION OF FORSKOLIN DERIVATIVES

二萜类Forskolin已被证明可以影响其他蛋白质 而不是腺苷环化酶。然而，这种情况相对较少。 有关Forskolin结合的差异的信息，请访问 功能多样的蛋白质。福斯科林的类似物已经被开发出来 可以用来区分腺苷酸环化酶、 易化葡萄糖转运蛋白与P-糖蛋白多药 传送器。Forsklin的氢结合要求 葡萄糖转运体和腺苷环化酶之间的相互作用 已经下定决心了，而且是非常不同的。此外，它已经被证明是 Forsklin对GLUT-4葡萄糖转运蛋白的亲和力是 远远高于Glut-1或Glut-3运输机。然而， Forskolin与GLUT-1结合的氢键特性， GLUT-3和GLUT-4转运体没有太大区别。这些数据将 在开发forskolin结合位点的模型方面是有用的， 葡萄糖转运蛋白。类似的实验也在进行中 腺酰环化酶亚型。此外，正在进行实验。 以确定Forskolin的构效关系 与P-糖蛋白多药转运体的相互作用。

The diterpene forskolin has been demonstrated to affect proteins other than adenylyl cyclase. However, there has been relatively little information regarding the differences in the binding of forskolin at functionally diverse proteins. Analogs of forskolin have been developed which can be used to discriminate between adenylyl cyclase, the facilitated glucose transporter, and the P-glycoprotein multidrug transporter. The hydrogen binding requirements for forskolin interactions at the glucose transporter and the adenylyl cyclase have been determined and are very different. In addition, it has been shown that the affinity of forskolin for the Glut-4 glucose transporter is much higher than for the Glut-1 or Glut-3 transporter. However, the hydrogen bonding characteristics for forskolin binding to the Glut-1, Glut-3, and Glut-4 transporters are not very different. These data will be useful in developing a model for the forskolin binding site at the glucose transporter. Similar experiments are being carried out with adenylyl cyclase subtypes. In addition, experiments are being carried out to determine the structure activity relationships of forskolin for interactions with the P-glycoprotein multidrug transporter.