Matschinsky Franz M, Porte Daniel
F1000 Med Rep. 2010 Jun 16;2:43. doi: 10.3410/M2-43.
The glucose-phosphorylating enzyme glucokinase, a promising target for developing new antidiabetic agents, was identified through the combined efforts of basic research and human biochemical genetics. Allosteric glucokinase activators (GKAs) were discovered by high-throughput screening of a large compound library and first reported in 2003. GKAs stimulate insulin release and glucose metabolism in the liver thereby lowering blood sugar, and promising trials in humans demonstrate that they are highly effective in patients with type 2 diabetes mellitus. Many companies are now attempting to develop effective and safe GKAs for treating diabetics.
葡萄糖磷酸化酶葡萄糖激酶是开发新型抗糖尿病药物的一个有前景的靶点，它是通过基础研究和人类生化遗传学的共同努力而确定的。变构葡萄糖激酶激活剂（GKAs）是通过对一个大型化合物库进行高通量筛选而发现的，并于2003年首次报道。GKAs可刺激肝脏中的胰岛素释放和葡萄糖代谢，从而降低血糖，而在人体进行的有前景的试验表明，它们对2型糖尿病患者非常有效。许多公司目前正试图开发有效且安全的GKAs用于治疗糖尿病患者。
