摘要
2型糖尿病是一种慢性代谢性疾病,其主要表现为高血糖和微血管并发症,是影响人类生活的重大疾病之一,目前尚无理想的治疗药物。腺苷酸活化蛋白激酶(AMP-activated protein kinase,AMPK)是一种高度保守的丝氨酸/苏氨酸蛋白激酶,在细胞和机体能量代谢与平衡等方面发挥重要作用;小分子AMPK直接激动剂因在降低血糖方面的作用而有望成为新一代治疗2型糖尿病的药物。本文按结构分类,对近几年报道的小分子AMPK直接激动剂进行综述。
Type 2 diabetes, an epidemic disorder characterized by high blood glucose level associated with micro- vascular complications, is one of the main causes of human suffer across the globe, with no effective medicine up to now. AMP-activated protein kinase （AMPK）, a highly conserved serine/threonine protein kinase, is a key sensor and regulator of intracellular and whole-body energy metabolism. Small molecule AMPK direct activators have been proven to lower blood-glucose, which is a promising candidate for the treatment of type 2 diabetes. The progress on the research of small molecule AMPK direct activators in recent years is summarized in this paper.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2015年第4期406-415,共10页
Journal of China Pharmaceutical University
关键词
腺苷酸活化蛋白激酶
AMPK直接激动剂
构效关系
2型糖尿病
新靶点
进展
AMP-activated protein kinase
AMPK direct activators
structure-activity relationship
type 2 diabe-tes
new target
advances
