Search Results - "Schmidt, James J."
-
1
Small molecules showing significant protection of mice against botulinum neurotoxin serotype A
Published in PloS one (13-04-2010)“…Botulinum neurotoxin serotype A (BoNTA) causes a life-threatening neuroparalytic disease known as botulism that could afflict large, unprotected populations if…”
Get full text
Journal Article -
2
Potent new small-molecule inhibitor of botulinum neurotoxin serotype A endopeptidase developed by synthesis-based computer-aided molecular design
Published in PloS one (10-11-2009)“…Botulinum neurotoxin serotype A (BoNTA) causes a life-threatening neuroparalytic disease known as botulism. Current treatment for post exposure of BoNTA uses…”
Get full text
Journal Article -
3
Inhibition of Metalloprotease Botulinum Serotype A from a Pseudo-peptide Binding Mode to a Small Molecule That Is Active in Primary Neurons
Published in The Journal of biological chemistry (16-02-2007)“…An efficient research strategy integrating empirically guided, structure-based modeling and chemoinformatics was used to discover potent small molecule…”
Get full text
Journal Article -
4
Fluorigenic Substrates for the Protease Activities of Botulinum Neurotoxins, Serotypes A, B, and F
Published in Applied and Environmental Microbiology (01-01-2003)“…ERRATUM ( vol. 69 , p. 3025 ) Classifications Services AEM Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg…”
Get full text
Journal Article -
5
Computer-aided lead optimization: improved small-molecule inhibitor of the zinc endopeptidase of botulinum neurotoxin serotype A
Published in PloS one (22-08-2007)“…Optimization of a serotype-selective, small-molecule inhibitor of botulinum neurotoxin serotype A (BoNTA) endopeptidase is a formidable challenge because the…”
Get full text
Journal Article -
6
Serotype-selective, small-molecule inhibitors of the zinc endopeptidase of botulinum neurotoxin serotype A
Published in Bioorganic & medicinal chemistry (15-01-2006)“…Botulinum neurotoxin serotype A (BoNTA) is one of the most toxic substances known. Currently, there is no antidote to BoNTA. Small molecules identified from…”
Get full text
Journal Article -
7
Use of a Recombinant Fluorescent Substrate with Cleavage Sites for All Botulinum Neurotoxins in High-Throughput Screening of Natural Product Extracts for Inhibitors of Serotypes A, B, and E
Published in Applied and Environmental Microbiology (01-02-2008)“…The seven serotypes of botulinum neurotoxin (BoNTs) are zinc metalloproteases that cleave and inactivate proteins critical for neurotransmission. The…”
Get full text
Journal Article -
8
Three‐Dimensional Database Mining Identifies a Unique Chemotype that Unites Structurally Diverse Botulinum Neurotoxin Serotype A Inhibitors in a Three‐Zone Pharmacophore
Published in ChemMedChem (15-12-2008)“…A search query consisting of two aromatic centers and two cationic centers was defined based on previously identified small molecule inhibitors of the…”
Get full text
Journal Article -
9
Mode of VAMP substrate recognition and inhibition of Clostridium botulinum neurotoxin F
Published in Nature structural & molecular biology (01-07-2009)“…Clostridium botulinum neurotoxins (BoNTs) cleave proteins involved in neurotransmitter release, with different serotypes showing distinct cleavage specificity…”
Get full text
Journal Article -
10
Targeted delivery into motor nerve terminals of inhibitors for SNARE‐cleaving proteases via liposomes coupled to an atoxic botulinum neurotoxin
Published in The FEBS journal (01-07-2012)“…A targeted drug carrier (TDC) is described for transferring functional proteins or peptides into motor nerve terminals, a pivotal locus for therapeutics to…”
Get full text
Journal Article -
11
Rapid product analysis and increased sensitivity for quantitative determinations of botulinum neurotoxin proteolytic activity
Published in Analytical biochemistry (15-01-2010)“…The ultimate molecular action of botulinum neurotoxin (BoNT) is a Zn-dependent endoproteolytic activity on one of the three SNARE (soluble…”
Get full text
Journal Article -
12
A Potent Peptidomimetic Inhibitor of Botulinum Neurotoxin Serotype A Has a Very Different Conformation than SNAP-25 Substrate
Published in Structure (London) (08-10-2008)“…Botulinum neurotoxin serotype A is the most lethal of all known toxins. Here, we report the crystal structure, along with SAR data, of the zinc metalloprotease…”
Get full text
Journal Article -
13
A high-affinity competitive inhibitor of type A botulinum neurotoxin protease activity
Published in FEBS letters (18-12-2002)“…The peptide N-acetyl-CRATKML-amide is an effective inhibitor of type A botulinum neurotoxin (BoNT A) protease activity [Schmidt et al., FEBS Lett. 435 (1998)…”
Get full text
Journal Article -
14
Botulinum Neurotoxin Serotype F: Identification of Substrate Recognition Requirements and Development of Inhibitors with Low Nanomolar Affinity
Published in Biochemistry (Easton) (15-03-2005)“…Botulinum neurotoxins (BoNTs A−G) are zinc metalloendoproteases that exhibit extraordinary specificities for proteins involved in neurotransmitter release. In…”
Get full text
Journal Article -
15
A Refined Pharmacophore Identifies Potent 4-Amino-7-chloroquinoline-Based Inhibitors of the Botulinum Neurotoxin Serotype A Metalloprotease
Published in Journal of medicinal chemistry (03-05-2007)“…We previously identified structurally diverse small molecule (non-peptidic) inhibitors (SMNPIs) of the botulinum neurotoxin serotype A (BoNT/A) light chain…”
Get full text
Journal Article -
16
Novel small molecule inhibitors of botulinum neurotoxin A metalloprotease activity
Published in Biochemical and biophysical research communications (10-10-2003)“…Botulinum neurotoxins (BoNTs) are among the most lethal biological substances to have been weaponized and are listed as biodefense category A agents…”
Get full text
Journal Article -
17
High-Throughput Assays for Botulinum Neurotoxin Proteolytic Activity: Serotypes A, B, D, and F
Published in Analytical biochemistry (01-09-2001)“…Botulinum neurotoxins (BoNT) are zinc metalloproteases that cleave and inactivate cellular proteins essential for neurotransmitter release. Because the…”
Get full text
Journal Article -
18
Peptide-Toxin Tools for Probing the Expression and Function of Fetal and Adult Subtypes of the Nicotinic Acetylcholine Receptor
Published in Annals of the New York Academy of Sciences (01-06-2008)“…Although the neuromuscular nicotinic acetylcholine receptor (nAChR) is one of the most intensively studied ion channels in the nervous system, the differential…”
Get full text
Journal Article -
19
Conformational sampling of the botulinum neurotoxin serotype a light chain: implications for inhibitor binding
Published in Bioorganic & medicinal chemistry (17-01-2005)“…Molecular dynamics simulations were used to explore how residue motion in and around the botulinum neurotoxin serotype A light chain (BoNT/A LC) substrate…”
Get full text
Journal Article -
20
Bis-imidazoles as molecular probes for peripheral sites of the zinc endopeptidase of botulinum neurotoxin serotype A
Published in Bioorganic & medicinal chemistry (15-05-2006)“…Botulinum neurotoxin serotype A (BoNTA) is highly toxic, and its antidote is currently unavailable. The essential light-chain subunit of BoNTA is a zinc…”
Get full text
Journal Article