Detail publikace

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.

Originální název

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

Typ

článek v časopise ve Web of Science, Jimp

Jazyk

angličtina

Originální abstrakt

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.

Klíčová slova

Botulinum neurotoxins; Chicoric acid; Structure-activity relationship

Autoři

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

Vydáno

15. 11. 2017

ISSN

0960-894X

Periodikum

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Ročník

27

Číslo

22

Stát

Spojené království Velké Británie a Severního Irska

Strany od

4956

Strany do

4959

Strany počet

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"
}