Leibniz-Institute for Food Systems Biology at the Technical University of Munich, 85354 Freising, Germany.
Molecules. 2020 Sep 26;25(19):4423. doi: 10.3390/molecules25194423.
The finding that bitter taste receptors are expressed in numerous tissues outside the oral cavity and fulfill important roles in metabolic regulation, innate immunity and respiratory control, have made these receptors important targets for drug discovery. Efficient drug discovery depends heavily on detailed knowledge on structure-function-relationships of the target receptors. Unfortunately, experimental structures of bitter taste receptors are still lacking, and hence, the field relies mostly on structures obtained by molecular modeling combined with functional experiments and point mutageneses. The present article summarizes the current knowledge on the structure-function relationships of human bitter taste receptors. Although these receptors are difficult to express in heterologous systems and their homology with other G protein-coupled receptors is very low, detailed information are available at least for some of these receptors.
苦味受体不仅在口腔外的众多组织中表达，而且在代谢调节、先天免疫和呼吸控制中发挥着重要作用，这一发现使这些受体成为药物发现的重要靶点。有效的药物发现在很大程度上依赖于对靶受体的结构-功能关系的详细了解。不幸的是，苦味受体的实验结构仍然缺乏，因此，该领域主要依赖于结合功能实验和定点诱变的分子建模获得的结构。本文总结了人类苦味受体结构-功能关系的最新知识。尽管这些受体很难在异源系统中表达，并且与其他 G 蛋白偶联受体的同源性很低，但至少对其中一些受体已经有了详细的信息。
