Issue 4, 2022

Structural insights into inhibition of the drug target dihydroorotate dehydrogenase by bacterial hydroxyalkylquinolines

Abstract

Hydroxyalkylquinolines (HAQs) are ubiquitious natural products but their interactions with associated protein targets remain elusive. We report X-ray crystal structures of two HAQs in complex with dihydroorotate dehydrogenase (DHODH). Our results reveal the structural basis of DHODH inhibition by HAQs and open the door to downstream structure–activity relationship studies.

Graphical abstract: Structural insights into inhibition of the drug target dihydroorotate dehydrogenase by bacterial hydroxyalkylquinolines

Supplementary files

Article information

Article type
Communication
Submitted
25 Dec 2021
Accepted
07 Feb 2022
First published
07 Feb 2022
This article is Open Access
Creative Commons BY-NC license

RSC Chem. Biol., 2022,3, 420-425

Structural insights into inhibition of the drug target dihydroorotate dehydrogenase by bacterial hydroxyalkylquinolines

S. M. Horwitz, T. C. Blue, J. A. Ambarian, S. Hoshino, M. R. Seyedsayamdost and K. M. Davis, RSC Chem. Biol., 2022, 3, 420 DOI: 10.1039/D1CB00255D

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