Method of screening a candidate compound for activity as an elastase 2A (ELA2A) inhibitor
US10829563B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Jun 16, 2017 |
| Grant date | Nov 10, 2020 |
| Priority date | — |
| Expiry date | Jun 16, 2037 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2800/065
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention is in the field of therapy of gut inflammatory diseases such as Inflammatory Bowel Diseases (IBD) or Irritable Bowel Syndrome (IBS) including Gluten hypersensitivity. The inventors showed that ELA2A secreted by epithelial cells in the extracellular space is over-expressed in IBD conditions degrading tight junction proteins and controlling cytokines expression. Overexpression of ELA2A conferred a pro-inflammatory phenotype both in cell expression systems and in vivo in animal model of IBD. The inventors also showed that ELA2 over-expressing intestinal epithelial cells increase the release of CXCL8 protein compared to control cells. The increased CXCL-8 protein release observed in cells overexpressing ELA2A is inhibited by ELAFIN addition to the culture, in a dose-dependent manner. In particular, the invention relates to inhibitors of Elastase ELA2A, for use in the treatment of Inflammatory Bowel Diseases, such as Crohn's Disease, Ulcerative Colitis, Celiac disease, and Pouchitis.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.