scholarly journals Directed Assembly of Homopentameric Cholera Toxin B-Subunit Proteins into Higher-Order Structures Using Coiled-Coil Appendages

2019 ◽  
Vol 141 (13) ◽  
pp. 5211-5219 ◽  
Author(s):  
James F. Ross ◽  
Gemma C. Wildsmith ◽  
Michael Johnson ◽  
Daniel L. Hurdiss ◽  
Kristian Hollingsworth ◽  
...  
Keyword(s):  
Cholera Toxin ◽  
Coiled Coil ◽  
Directed Assembly ◽  
Higher Order ◽  
Cholera Toxin B Subunit ◽  
Toxin B ◽  
Cholera Toxin B ◽  
B Subunit ◽  
Order Structures

scholarly journals Spray-Dried Formulation of Epicertin, a Recombinant Cholera Toxin B Subunit Variant That Induces Mucosal Healing

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 576
Author(s):  
Micaela A. Reeves ◽  
Joshua M. Royal ◽  
David A. Morris ◽  
Jessica M. Jurkiewicz ◽  
Nobuyuki Matoba ◽  
...  
Keyword(s):  
Gastric Acid ◽  
Cholera Toxin ◽  
Oral Formulation ◽  
Size Exclusion ◽  
Cholera Toxin B Subunit ◽  
Toxin B ◽  
Cholera Toxin B ◽  
B Subunit ◽  
Enteric Coated ◽  
Spray Dried

Epicertin (EPT) is a recombinant variant of the cholera toxin B subunit, modified with a C-terminal KDEL endoplasmic reticulum retention motif. EPT has therapeutic potential for ulcerative colitis treatment. Previously, orally administered EPT demonstrated colon epithelial repair activity in dextran sodium sulfate (DSS)-induced acute and chronic colitis in mice. However, the oral dosing requires cumbersome pretreatment with sodium bicarbonate to conserve the acid-labile drug substance while transit through the stomach, hampering its facile application in chronic disease treatment. Here, we developed a solid oral formulation of EPT that circumvents degradation in gastric acid. EPT was spray-dried and packed into enteric-coated capsules to allow for pH-dependent release in the colon. A GM1-capture KDEL-detection ELISA and size-exclusion HPLC indicated that EPT powder maintains activity and structural stability for up to 9 months. Capsule disintegration tests showed that EPT remained encapsulated at pH 1 but was released over 180 min at pH 6.8, the approximate pH of the proximal colon. An acute DSS colitis study confirmed the therapeutic efficacy of encapsulated EPT in C57BL/6 mice upon oral administration without gastric acid neutralization pretreatment compared to vehicle-treated mice (p < 0.05). These results provide a foundation for an enteric-coated oral formulation of spray-dried EPT.

Synthesis of Lactose Dendrimers and Multivalency Effects in Binding to the Cholera Toxin B Subunit

2001 ◽  
Vol 2001 (24) ◽  
pp. 4685 ◽  
Author(s):  
Ioannis Vrasidas ◽  
Nico J. de Mol ◽  
Rob M. J. Liskamp ◽  
Roland J. Pieters
Keyword(s):  
Cholera Toxin ◽  
Cholera Toxin B Subunit ◽  
Toxin B ◽  
Cholera Toxin B ◽  
B Subunit
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