Discovery and SAR study of a sulfonamide hydroxamic acid inhibitor for the botulinum neurotoxin serotype A light chain

MedChemComm ◽  
2014 ◽  
Vol 5 (6) ◽  
pp. 706-710 ◽  
Author(s):  
Alexander Burtea ◽  
Nicholas T. Salzameda
Keyword(s):  
Light Chain ◽  
High Throughput Screening ◽  
Hydroxamic Acid ◽  
Botulinum Neurotoxin ◽  
Serotype A ◽  
Acid Inhibitor ◽  
Structure Activity ◽  
Relationship Study ◽  
Botulinum Neurotoxin Serotype A ◽  
Sar Study

Through the use of chemical synthesis and high throughput screening, we discovered a sulfonamide hydroxamic acid inhibitor for the botulinum neurotoxin serotype A light chain. A structure activity relationship study of the parent inhibitor resulted in the synthesis of a new inhibitor with an IC50of 0.95 ± 0.60 μM for the BoNT/A LC.

scholarly journals 4-Amino-7-chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity

2013 ◽  
Vol 56 (14) ◽  
pp. 5860-5871 ◽  
Author(s):  
Igor M. Opsenica ◽  
Mikloš Tot ◽  
Laura Gomba ◽  
Jonathan E. Nuss ◽  
Richard J. Sciotti ◽  
...  
Keyword(s):  
Light Chain ◽  
Botulinum Neurotoxin ◽  
Antiprotozoal Activity ◽  
Ligand Efficiency ◽  
Serotype A ◽  
Botulinum Neurotoxin Serotype A

scholarly journals Synthesis and activity of isoleucine sulfonamide derivatives as novel botulinum neurotoxin serotype A light chain inhibitors

2020 ◽  
Vol 28 (18) ◽  
pp. 115659
Author(s):  
Jordan C. Thompson ◽  
Wendy T. Dao ◽  
Alex Ku ◽  
Sandra L. Rodriguez-Beltran ◽  
Martin Amezcua ◽  
...  
Keyword(s):  
Light Chain ◽  
Botulinum Neurotoxin ◽  
Serotype A ◽  
Botulinum Neurotoxin Serotype A

scholarly journals A Chemotype That Inhibits Three Unrelated Pathogenic Targets: The Botulinum Neurotoxin Serotype A Light Chain,P. falciparumMalaria, and the Ebola Filovirus

2011 ◽  
Vol 54 (5) ◽  
pp. 1157-1169 ◽  
Author(s):  
Igor Opsenica ◽  
James C. Burnett ◽  
Rick Gussio ◽  
Dejan Opsenica ◽  
Nina Todorović ◽  
...  
Keyword(s):  
Light Chain ◽  
Botulinum Neurotoxin ◽  
Serotype A ◽  
Botulinum Neurotoxin Serotype A

A matrix-focused structure-activity and binding site flexibility study of quinolinol inhibitors of botulinum neurotoxin serotype A

2017 ◽  
Vol 27 (3) ◽  
pp. 675-678 ◽  
Author(s):  
William A. Harrell ◽  
Rebecca C. Vieira ◽  
Susan M. Ensel ◽  
Vicki Montgomery ◽  
Rebecca Guernieri ◽  
...  
Keyword(s):  
Binding Site ◽  
Botulinum Neurotoxin ◽  
Serotype A ◽  
Structure Activity ◽  
Botulinum Neurotoxin Serotype A

Light Chain of Botulinum Neurotoxin Serotype A:  Structural Resolution of a Catalytic Intermediate†,‡

Biochemistry ◽  
2006 ◽  
Vol 45 (29) ◽  
pp. 8903-8911 ◽  
Author(s):  
Zhuji Fu ◽  
Sheng Chen ◽  
Michael R. Baldwin ◽  
Grant E. Boldt ◽  
Adam Crawford ◽  
...  
Keyword(s):  
Light Chain ◽  
Botulinum Neurotoxin ◽  
Serotype A ◽  
Botulinum Neurotoxin Serotype A

scholarly journals Pharmacophore Refinement Guides the Design of Nanomolar-Range Botulinum Neurotoxin Serotype A Light Chain Inhibitors

2010 ◽  
Vol 1 (7) ◽  
pp. 301-305 ◽  
Author(s):  
Jonathan E. Nuss ◽  
Yuxiang Dong ◽  
Laura M. Wanner ◽  
Gordon Ruthel ◽  
Peter Wipf ◽  
...  
Keyword(s):  
Light Chain ◽  
Botulinum Neurotoxin ◽  
Serotype A ◽  
Botulinum Neurotoxin Serotype A ◽  
Nanomolar Range

scholarly journals Superactivation of the Botulinum Neurotoxin Serotype A Light Chain Metalloprotease:  A New Wrinkle in Botulinum Neurotoxin

2006 ◽  
Vol 128 (13) ◽  
pp. 4176-4177 ◽  
Author(s):  
Laura A. McAllister ◽  
Mark S. Hixon ◽  
Jack P. Kennedy ◽  
Tobin J. Dickerson ◽  
Kim D. Janda
Keyword(s):  
Light Chain ◽  
Botulinum Neurotoxin ◽  
Serotype A ◽  
Botulinum Neurotoxin Serotype A
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