Avignon A, Sultan A
Metabolic Disease Department, Lapeyronie Hospital, Montpellier, France.
Diabetes Metab. 2006 Jun;32(3):205-13. doi: 10.1016/s1262-3636(07)70270-7.
PKC comprises a superfamily of isoenzymes that is activated in response to various stimuli. Hyperglycaemia induces the activation of different PKC isoforms. However, the PKC-B isoform appears to be preferentially activated by high glucose levels and has been shown to be associated with diabetic vascular complications. In vitro and in vivo animal studies have shown that ruboxistaurin mesylate, a novel selective inhibitor of PKC-B ameliorates the biochemical and functional consequences of PKC activation and may have the potential to reduce the burden of vascular complications associated with diabetes. Results of the first phase-II and phase-III trials evaluating the efficacy of this compound on diabetic microvascular complications have been published recently. They confirm that this compound may favorably influence the evolution of diabetic microvascular complications.
蛋白激酶C（PKC）由一个同工酶超家族组成，该超家族会响应各种刺激而被激活。高血糖会诱导不同的PKC亚型活化。然而，PKC-β亚型似乎优先被高血糖水平激活，并且已被证明与糖尿病血管并发症有关。体外和体内动物研究表明，甲磺酸鲁伯斯塔林作为一种新型的PKC-β选择性抑制剂，可改善PKC激活所带来的生化和功能影响，并且可能有潜力减轻与糖尿病相关的血管并发症负担。评估该化合物对糖尿病微血管并发症疗效的首批II期和III期试验结果最近已发表。这些结果证实，该化合物可能对糖尿病微血管并发症的发展产生有利影响。
