Department of Clinical Pathomorphology, Medical University of Lublin, ul. Jaczewskiego 8b, 20-090, Lublin, Poland.
J Transl Med. 2021 Oct 21;19(1):440. doi: 10.1186/s12967-021-03067-y.
Bitter taste-sensing type 2 receptors (TAS2Rs or T2Rs), belonging to the subgroup of family A G-protein coupled receptors (GPCRs), are of crucial importance in the perception of bitterness. Although in the first instance, TAS2Rs were considered to be exclusively distributed in the apical microvilli of taste bud cells, numerous studies have detected these sensory receptor proteins in several extra-oral tissues, such as in pancreatic or ovarian tissues, as well as in their corresponding malignancies. Critical points of extra-oral TAS2Rs biology, such as their structure, roles, signaling transduction pathways, extensive mutational polymorphism, and molecular evolution, have been currently broadly studied. The TAS2R cascade, for instance, has been recently considered to be a pivotal modulator of a number of (patho)physiological processes, including adipogenesis or carcinogenesis. The latest advances in taste receptor biology further raise the possibility of utilizing TAS2Rs as a therapeutic target or as an informative index to predict treatment responses in various disorders. Thus, the focus of this review is to provide an update on the expression and molecular basis of TAS2Rs functions in distinct extra-oral tissues in health and disease. We shall also discuss the therapeutic potential of novel TAS2Rs targets, which are appealing due to their ligand selectivity, expression pattern, or pharmacological profiles.
苦味感应型 2 型受体（TAS2R 或 T2R）属于 A 族 G 蛋白偶联受体（GPCR）亚群，对苦味感知具有至关重要的作用。虽然最初认为 TAS2R 仅分布在味蕾细胞的顶端微绒毛中，但许多研究已经在许多口腔外组织中检测到这些感觉受体蛋白，如胰腺或卵巢组织以及相应的恶性肿瘤。目前已经广泛研究了口腔外 TAS2R 生物学的关键点，如它们的结构、作用、信号转导途径、广泛的突变多态性和分子进化。例如，TAS2R 级联反应最近被认为是许多（病理）生理过程的关键调节剂，包括脂肪生成或癌变。味觉受体生物学的最新进展进一步提高了将 TAS2R 用作治疗靶点或作为信息指标来预测各种疾病治疗反应的可能性。因此，本综述的重点是提供有关 TAS2R 在健康和疾病状态下在不同口腔外组织中的表达和分子基础的最新信息。我们还将讨论新型 TAS2R 靶标的治疗潜力，这些靶标因其配体选择性、表达模式或药理学特征而具有吸引力。
