5LIR

Structure of the SALTY Sigma cross-reacting protein 27A (SCRP-27A) from Salmonella typhimurium

5LIR の概要

• エントリーDOI: 10.2210/pdb5lir/pdb
• 分子名称: Sigma cross-reacting protein 27A (SCRP-27A), DI(HYDROXYETHYL)ETHER (3 entities in total)
• 機能のキーワード: rossmann fold class i glutamine amidotransferase-like, transferase
• 由来する生物種: Salmonella enterica subsp. enterica serovar Typhimurium
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 25944.70

構造登録者

Schneider, S.,Mandel, M.,Sieber, S.A. (登録日: 2016-07-15, 公開日: 2016-09-14, 最終更新日: 2024-11-20)

主引用文献

Mandl, F.A.,Kirsch, V.C.,Ugur, I.,Kunold, E.,Vomacka, J.,Fetzer, C.,Schneider, S.,Richter, K.,Fuchs, T.M.,Antes, I.,Sieber, S.A.
Natural-Product-Inspired Aminoepoxybenzoquinones Kill Members of the Gram-Negative Pathogen Salmonella by Attenuating Cellular Stress Response.
Angew.Chem.Int.Ed.Engl., 55:14852-14857, 2016

PubMed Abstract: Gram-negative bacteria represent a challenging task for antibacterial drug discovery owing to their impermeable cell membrane and restricted uptake of small molecules. We herein describe the synthesis of natural-product-derived epoxycyclohexenones and explore their antibiotic activity against several pathogenic bacteria. A compound with activity against Salmonella Typhimurium was identified, and the target enzymes were unraveled by quantitative chemical proteomics. Importantly, two protein hits were linked to bacterial stress response, and corresponding assays revealed an elevated susceptibility to reactive oxygen species upon compound treatment. The consolidated inhibition of these targets provides a rationale for antibacterial activity and highlights epoxycyclohexenones as natural product scaffolds with suitable properties for killing Gram-negative Salmonella.

PubMed: 27782347
DOI: 10.1002/anie.201607338

実験手法

X-RAY DIFFRACTION (1.75 Å)