Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways. [PDF]
The small molecule Eeyarestatin I (ESI) inhibits the endoplasmic reticulum (ER)-cytosol dislocation and subsequent degradation of ERAD (ER associated protein degradation) substrates. Toxins such as ricin and Shiga/Shiga-like toxins (SLTx) are endocytosed
Mina-Olga Aletrari +10 more
doaj +3 more sources
An inhibitor of Staphylococcus aureus exfoliative toxin
We describe here an inhibitor of Staphylococcus aureus exfoliative toxin. The toxin was extracted from an S. aureus strain isolated from a case of staphylococcus scalded skin syndrome. The activity of the toxin was compared in tryptic soy broth and brain heart infusion broth. Both supported growth of S.
A A, Al-Sulami +2 more
openaire +3 more sources
Designing inhibitors of anthrax toxin [PDF]
Present-day rational drug design approaches are based on exploiting unique features of the target biomolecules, small- or macromolecule drug candidates and physical forces that govern their interactions. The 2013 Nobel Prize in chemistry awarded 'for the development of multiscale models for complex chemical systems' once again demonstrated the ...
Ekaterina M, Nestorovich +1 more
openaire +2 more sources
Human α-Defensin-5 Efficiently Neutralizes Clostridioides difficile Toxins TcdA, TcdB, and CDT
Infections with the pathogenic bacterium Clostridioides (C.) difficile are coming more into focus, in particular in hospitalized patients after antibiotic treatment. C. difficile produces the exotoxins TcdA and TcdB.
Michael Korbmacher +5 more
doaj +1 more source
Clostridial glucosylating toxins enter cells via clathrin-mediated endocytosis. [PDF]
Clostridium difficile toxin A (TcdA) and toxin B (TcdB), C. sordellii lethal toxin (TcsL) and C. novyi alpha-toxin (TcnA) are important pathogenicity factors, which represent the family of the clostridial glucosylating toxins (CGTs).
Panagiotis Papatheodorou +4 more
doaj +1 more source
Tetra‐ versus Pentavalent Inhibitors of Cholera Toxin [PDF]
AbstractThe five B‐subunits (CTB5) of the Vibrio cholerae (cholera) toxin can bind to the intestinal cell surface so the entire AB5 toxin can enter the cell. Simultaneous binding can occur on more than one of the monosialotetrahexosylganglioside (GM1) units present on the cell surface.
Fu, O +7 more
openaire +5 more sources
The secretion inhibitor Exo2 perturbs trafficking of Shiga toxin between endosomes and the trans-Golgi network [PDF]
The small-molecule inhibitor Exo2 {4-hydroxy-3-methoxy-(5,6,7,8-tetrahydrol[1]benzothieno[2,3-d]pyrimidin-4-yl)hydraz-one benzaldehyde} has been reported to disrupt the Golgi apparatus completely and to stimulate Golgi–ER (endoplasmic reticulum) fusion ...
Amessou, M +37 more
core +1 more source
Peptide-Conjugated Pterins as Inhibitors of Ricin Toxin A [PDF]
Several 7-peptide-substituted pterins were synthesized and tested as competitive active-site inhibitors of ricin toxin A (RTA). Focus began on dipeptide conjugates, and these results further guided the construction of several tripeptide conjugates. The binding of these compounds to RTA was studied via a luminescence-based kinetic assay, as well as ...
Ryota, Saito +8 more
openaire +2 more sources
Designed Azolopyridinium Salts Block Protective Antigen Pores In Vitro and Protect Cells from Anthrax Toxin [PDF]
Background:Several intracellular acting bacterial protein toxins of the AB-type, which are known to enter cells by endocytosis, are shown to produce channels.
Barth, Holger +24 more
core +2 more sources
Exploring the functional domain and the target of the tetanus toxin light chain in neurohypophysial terminals [PDF]
The tetanus toxin light chain blocks calcium induced vasopressin release from neurohypophysial nerve terminals. Here we show that histidine residue 233 within the putative zinc binding motif of the tetanus toxin light chain is essential for the ...
Weller, U. +7 more
core +1 more source

