2021年2月19日
Structural basis for selective inhibition of human serine hydroxymethyltransferase by secondary bile acid conjugate.
iScience
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- 巻
- 24
- 号
- 2
- 開始ページ
- 102036
- 終了ページ
- 102036
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1016/j.isci.2021.102036
Bile acids are metabolites of cholesterol that facilitate lipid digestion and absorption in the small bowel. Bile acids work as agonists of receptors to regulate their own metabolism. Bile acids also regulate other biological systems such as sugar metabolism, intestinal multidrug resistance, and adaptive immunity. However, numerous physiological roles of bile acids remain undetermined. In this study, we solved the crystal structure of human serine hydroxymethyltransferase (hSHMT) in complex with an endogenous secondary bile acid glycine conjugate. The specific interaction between hSHMT and the ligand was demonstrated using mutational analyses, biophysical measurements, and structure-activity relationship studies, suggesting that secondary bile acid conjugates may act as modulators of SHMT activity.
- リンク情報
- ID情報
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- DOI : 10.1016/j.isci.2021.102036
- PubMed ID : 33521601
- PubMed Central 記事ID : PMC7820547