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Antibacterial Strategy against H. pylori: Inhibition of the Radical SAM Enzyme MqnE in Menaquinone Biosynthesis.
Joshi, Sumedh; Fedoseyenko, Dmytro; Mahanta, Nilkamal; Ducati, Rodrigo G; Feng, Mu; Schramm, Vern L; Begley, Tadhg P.
Afiliación
  • Joshi S; Department of Chemistry, Texas A&M University, College Station, Texas 77842, United States.
  • Fedoseyenko D; Department of Chemistry, Texas A&M University, College Station, Texas 77842, United States.
  • Mahanta N; Department of Chemistry, Texas A&M University, College Station, Texas 77842, United States.
  • Ducati RG; Department of Biochemistry, Albert Einstein College of Medicine, Bronx, New York 10461, United States.
  • Feng M; Department of Biochemistry, Albert Einstein College of Medicine, Bronx, New York 10461, United States.
  • Schramm VL; Department of Biochemistry, Albert Einstein College of Medicine, Bronx, New York 10461, United States.
  • Begley TP; Department of Chemistry, Texas A&M University, College Station, Texas 77842, United States.
ACS Med Chem Lett ; 10(3): 363-366, 2019 Mar 14.
Article en En | MEDLINE | ID: mdl-30891141
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 H. pylori (IC50 = 1.8 ± 0.4 µM) and identifies MqnE as a promising target for antibiotic development.
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Texto completo: 1 Bases de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2019 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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XML
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Texto completo: 1 Bases de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2019 Tipo del documento: Article País de afiliación: Estados Unidos