Issue 16, 2019, Issue in Progress
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RSC Advances

Exploring the mode of action of inhibitors targeting the PhoP response regulator of Salmonella enterica through comprehensive pharmacophore approaches†

Keng-Chang Tsai,‡ab   Po-Pin Hung,‡c   Ching-Feng Cheng,de   Chinpan Chen ORCID logo *e  and  Tien-Sheng Tseng ORCID logo *f  

* Corresponding authors

a National Research Institute of Chinese Medicine, Ministry of Health and Welfare, Taipei 112, Taiwan

b The PhD Program in Medical Biotechnology, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan

c Division of Infectious Disease, Department of Internal Medicine, Taipei Tzu Chi Hospital, The Buddhist Tzu Chi Medical Foundation, New Taipei City 231, Taiwan

d Department of Pediatrics, Taipei Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, Taipei and Tzu Chi University, Hualien, Taiwan

e Institute of Biomedical Sciences, Academia Sinica, Taipei 115, Taiwan

f Department of Research, Taipei Tzu Chi Hospital, The Buddhist Tzu Chi Medical Foundation, New Taipei City 231, Taiwan

Abstract

The PhoQ/PhoP two-component system regulates the physiological and virulence functions of Salmonella enterica. However, the mode of action of known PhoP inhibitors is unclear. We systematically constructed a pharmacophore model of inhibitors to probe the interface pharmacophore model of the PhoP dimer, coupling it with Ligplot analysis. We found that these inhibitors bind on the α5-helix, altering the conformation and interfering with PhoP binding on DNA.

Graphical abstract: Exploring the mode of action of inhibitors targeting the PhoP response regulator of Salmonella enterica through comprehensive pharmacophore approaches

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Article information

DOI
https://doi.org/10.1039/C9RA00620F
Article type
Paper
Submitted
24 Jan 2019
Accepted
28 Feb 2019
First published
21 Mar 2019
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2019,9, 9308-9312

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Exploring the mode of action of inhibitors targeting the PhoP response regulator of Salmonella enterica through comprehensive pharmacophore approaches

K. Tsai, P. Hung, C. Cheng, C. Chen and T. Tseng, RSC Adv., 2019, 9, 9308 DOI: 10.1039/C9RA00620F

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