Computational Biology, Human Genetics, GlaxoSmithKline R&D, Collegeville, PA, USA.
Computational Biology, Human Genetics, GlaxoSmithKline R&D, Collegeville, PA, USA.
Trends Mol Med. 2020 May;26(5):435-437. doi: 10.1016/j.molmed.2020.03.006. Epub 2020 Apr 3.
A recent study by Dvořák et al. supports metabolite mimicry as a drug development strategy. A potent agonist of the human pregnane X receptor (hPXR) was designed from two ligands that are products of the microbial catabolism of tryptophan. Its validity was demonstrated in cellular assays and a murine colitis model expressing hPXR by a significant reduction in inflammation biomarkers.
多尔瓦克等人最近的一项研究支持代谢物模拟作为一种药物开发策略。从色氨酸微生物代谢产物的两种配体设计出一种人类孕烷 X 受体 (hPXR) 的有效激动剂。其在表达 hPXR 的细胞测定和小鼠结肠炎模型中的有效性通过炎症生物标志物的显著降低得到证明。