Joshi Sumedh, Fedoseyenko Dmytro, Mahanta Nilkamal, Ducati Rodrigo G, Feng Mu, Schramm Vern L, Begley Tadhg P
Department of Chemistry, Texas A&M University, College Station, Texas 77842, United States.
Department of Biochemistry, Albert Einstein College of Medicine, Bronx, New York 10461, United States.
ACS Med Chem Lett. 2019 Feb 15;10(3):363-366. doi: 10.1021/acsmedchemlett.8b00649. eCollection 2019 Mar 14.
Aminofutalosine synthase (MqnE) catalyzes an important rearrangement reaction in menaquinone biosynthesis by the futalosine pathway. In this Letter, we report the identification of previously unreported inhibitors of MqnE using a mechanism-guided approach. The best inhibitor shows efficient inhibitory activity against (IC = 1.8 ± 0.4 μM) and identifies MqnE as a promising target for antibiotic development.
氨基呋咱糖苷合酶（MqnE）通过呋咱糖苷途径催化甲萘醌生物合成中的一个重要重排反应。在本信函中，我们报告了使用机制导向方法鉴定出此前未报道的MqnE抑制剂。最佳抑制剂对（IC = 1.8 ± 0.4 μM）显示出高效抑制活性，并确定MqnE是抗生素开发的一个有前景的靶点。
