Identification of 3-hydroxy-1,2-dimethylpyridine-4(1H)-thione as a metal-binding motif for the inhibition of botulinum neurotoxin A-Reference-Cited by-同舟云学术

Identification of 3-hydroxy-1,2-dimethylpyridine-4(1H)-thione as a metal-binding motif for the inhibition of botulinum neurotoxin A

Published:2021 Issue:1 Volume:12 Page:137-143
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Lin Lucy¹²³⁴^ORCID,Turner Lewis D.¹²³⁴^ORCID,Šilhár Peter¹²³⁴,Pellett Sabine⁵⁶⁷⁴,Johnson Eric A.⁵⁶⁷⁴,Janda Kim D.¹²³⁴^ORCID

Affiliation:

1. Department of Chemistry and the Skaggs Institute for Chemical Biology

2. The Scripps Research Institute

3. La Jolla

4. USA

5. Department of Bacteriology

6. University of Wisconsin

7. Madison

Abstract

The 3,4-HOPTO pharmacophore was identified as an inhibitor of botulinum neurotoxin A light chain. Structure-activity relationships were explored, resulting in a compound that protects SNAP-25 cleavage in motor neurons.

Funder

Natural Sciences and Engineering Research Council of Canada

National Institute of Allergy and Infectious Diseases

Skaggs Institute for Chemical Biology, Scripps Research Institute

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2021/MD/D0MD00320D

Reference39 articles.

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4. Botulinum Toxin as a Biological Weapon

5. C. F. D. C. A. P. (CDC) , Botulism Annual Summary, 2016 , Center for Disease Control and Prevention (CDC) , Atlanta, Georgia , 2017

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