潜在药物发现新靶点水通道蛋白

Aquaporins: a potential target for drug discovery

水通道蛋白(aquaporin,AQP)属于小分子疏水性内在膜蛋白家族,目前发现有13种。近年来研究表明,AQPs参与了哺乳动物的一些重要的生理病理学过程,如尿浓缩、脑水肿的形成、眼内压的调节、脂肪代谢、外分泌腺分泌、肿瘤血管发生等。调节AQPs表达的药物具有广阔的治疗应用前景。尽管目前还没有发现有效的AQPs调节剂,该蛋白仍是一个潜在的药物靶点,特别是高通量筛选等方法学的发展为证明该靶点的作用带来了希望。

Aquaporins （AQPs） are a family of small hydrophobic, integral membrane proteins, with thirteen aquaporins identified up to date. AQPs have recently been implicated in mammalian physiological and pathophysiologic mechanisms, such as urinary concentrating function, brain edema formation, regulation of intraocular pressure, fat metabolism, exocrine glandular fluid secretion, as well as tumor angiogenesis. Interfering with the expression of AQPs will undoubtedly have therapeutic applications. Although AQP modulators remain to be discovered, it is a potential drug target and the method of high-throughput screening will promote the proceeding for finding new drug based on AQPs.