Synthesis and structure–activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors

K Čapková, Y Yoneda, TJ Dickerson… - Bioorganic & medicinal …, 2007 - Elsevier
Botulinum neurotoxins are the most toxic proteins currently known. Based on a recently
identified potent lead structure, 2, 4-dichlorocinnamic acid hydroxamate, herein we report on …

Reexamining hydroxamate inhibitors of botulinum neurotoxin serotype A: Extending towards the β-exosite

GR Smith, D Caglič, P Čapek, Y Zhang… - Bioorganic & medicinal …, 2012 - Elsevier
Botulinum neurotoxins (BoNTs) are the most toxic proteins known to man, exposure to which
results in flaccid paralysis. Given their extreme potency, these proteins have become studied …

C-terminus of botulinum A protease has profound and unanticipated kinetic consequences upon the catalytic cleft

P Šilhár, MA Lardy, MS Hixon… - ACS medicinal …, 2013 - ACS Publications
Botulinum neurotoxins (BoNTs) are among the most deadly poisons known, though
ironically, they also are of great therapeutic utility. A number of research programs have …

Synthesis/biological evaluation of hydroxamic acids and their prodrugs as inhibitors for Botulinum neurotoxin A light chain

H Seki, S Pellett, P Šilhár, GN Stowe, B Blanco… - Bioorganic & Medicinal …, 2014 - Elsevier
Abstract Botulinum neurotoxin A (BoNT/A) is the most potent toxin known. Unfortunately, it is
also a potential bioweapon in terrorism, which is without an approved therapeutic treatment …

Chirality holds the key for potent inhibition of the botulinum neurotoxin serotype a protease

GN Stowe, P Šilhár, MS Hixon, NR Silvaggi… - Organic …, 2010 - ACS Publications
Botulinum neurotoxin serotype A (BoNT/A) is the most toxic protein known to man and also a
bioterrorism agent. As defined by our previous research targeting the etiological agent …

Synthesis, characterization and development of a high-throughput methodology for the discovery of botulinum neurotoxin a inhibitors

GE Boldt, JP Kennedy, MS Hixon… - Journal of …, 2006 - ACS Publications
Botulinum neurotoxins (BoNTs), etiological agents of the deadly food poisoning disease
botulism, are the most toxic proteins currently known. Although only a few hundred cases of …

Enhancing the pharmacokinetic properties of botulinum neurotoxin serotype A protease inhibitors through rational design

P Capek, Y Zhang, DJ Barlow… - ACS chemical …, 2011 - ACS Publications
Botulinum neurotoxin (BoNT), the etiological agent that causes the neuroparalytic disease
botulism, has become a highly studied drug target in light of the potential abuse of this toxin …

Evaluation of adamantane hydroxamates as botulinum neurotoxin inhibitors: synthesis, crystallography, modeling, kinetic and cellular based studies

P Šilhár, NR Silvaggi, S Pellett, K Čapková… - Bioorganic & medicinal …, 2013 - Elsevier
Botulinum neurotoxins (BoNTs) are the most lethal biotoxins known to mankind and are
responsible for the neuroparalytic disease botulism. Current treatments for botulinum …

Novel benzimidazole inhibitors of botulinum neurotoxin/A display enzyme and cell-based potency

SC Cardinale, MM Butler, G Ruthel… - The botulinum …, 2011 - inderscienceonline.com
Botulinum Neurotoxins (BoNTs) are used therapeutically and in cosmetics, providing
potential for bioterrorist activity, thus driving the search for small-molecule BoNT inhibitors …

Time-dependent botulinum neurotoxin serotype A metalloprotease inhibitors

B Li, SC Cardinale, MM Butler, R Pai, JE Nuss… - Bioorganic & medicinal …, 2011 - Elsevier
Botulinum neurotoxins (BoNTs) are the most lethal of biological substances, and are
categorized as class A biothreat agents by the Centers for Disease Control and Prevention …