Queensland University of Technology, Discipline of Medical Sciences, Faculty of Science and Technology, Brisbane, Australia.
Expert Opin Ther Targets. 2011 Jul;15(7):899-902. doi: 10.1517/14728222.2011.580279. Epub 2011 Apr 27.
Despite the present treatments for asthma (β(2)-adrenoceptor agonists, glucocorticoids, leukotriene receptor antagonists), many subjects with asthma have difficulty controlling it. Bitter taste receptors have recently been identified on human lung. The paper evaluated considers these receptors as a target for bronchodilation, by characterizing the effects of agonists in cultured human airway smooth muscle cells, isolated human bronchial smooth muscle and a mouse model of allergic asthma. The study confirmed that a bitter taste receptor (TAS2R) is a viable target for bronchodilation. Many diverse chemicals are known to stimulate the bitter taste receptors to produce the bitter taste, and many of these have more than one mechanism of action. Thus, it is not known whether any of these have clinical potential in asthma. It may be necessary to design and develop selective agonists for TAS2R, before the clinical potential of this target can be thoroughly investigated.
尽管目前有治疗哮喘的方法(β(2)-肾上腺素受体激动剂、糖皮质激素、白三烯受体拮抗剂),但许多哮喘患者仍难以控制病情。最近在人体肺部发现了苦味受体。本文评估了这些受体作为支气管扩张的靶点,通过在培养的人呼吸道平滑肌细胞、分离的人支气管平滑肌和过敏性哮喘小鼠模型中描述激动剂的作用来研究。研究证实,苦味受体(TAS2R)是支气管扩张的一个可行靶点。许多不同的化学物质已知可刺激苦味受体产生苦味,其中许多化学物质具有多种作用机制。因此,目前尚不清楚这些物质是否在哮喘中有临床应用潜力。在彻底研究该靶点的临床潜力之前,可能需要设计和开发针对 TAS2R 的选择性激动剂。