Publication detail

Examination of alpha-exosite inhibitors against Botulinum neurotoxin A protease through structure-activity relationship studies of chicoric acid

XUE, S. SEKI, H. REMEŠ, M. SILHAR, P. JANDA, K.

Original Title

Examination of alpha-exosite inhibitors against Botulinum neurotoxin A protease through structure-activity relationship studies of chicoric acid

Type

journal article in Web of Science

Language

English

Original Abstract

Botulinum neurotoxins (BoNT) are among the most toxic known substances and currently there are no effective treatments for intraneuronal BoNT intoxication. Chicoric acid (ChA) was previously reported as a BoNT/A inhibitor that binds to the enzyme's alpha-exosite. Herein, we report the synthesis and structure-activity relationships (SARs) of a series of ChA derivatives, which revealed essential binding interactions between ChA and BoNT/A. Moreover, several ChA-based inhibitors with improved potency against the BoNT/A were discovered.

Keywords

Botulinum neurotoxins; Chicoric acid; Structure-activity relationship

Authors

XUE, S.; SEKI, H.; REMEŠ, M.; SILHAR, P.; JANDA, K.

Released

15. 11. 2017

ISBN

0960-894X

Periodical

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Year of study

27

Number

22

State

United Kingdom of Great Britain and Northern Ireland

Pages from

4956

Pages to

4959

Pages count

4

BibTex

@article{BUT146946,
  author="XUE, S. and SEKI, H. and REMEŠ, M. and SILHAR, P. and JANDA, K.",
  title="Examination of alpha-exosite inhibitors against Botulinum neurotoxin A protease through structure-activity relationship studies of chicoric acid",
  journal="BIOORGANIC & MEDICINAL CHEMISTRY LETTERS",
  year="2017",
  volume="27",
  number="22",
  pages="4956--4959",
  doi="10.1016/j.bmcl.2017.10.021",
  issn="0960-894X"
}