Mode of Action

General Mechanisms

PETIR™ peptidase inhibitors target two enzymes that are over-expressed on immune cells and other cell systems in cases of inflammation.
The target peptidases belong to Aminopeptidase N (APN, CD13) and Dipeptidylpeptidase IV (DPIV, CD26) families.

These peptidases are present on immune cells particularly after activation in case of inflammation. Thus, the therapeutic effects are achieved via cutting off pathologically higher enzyme activity levels.

Inhibition of these peptidases results in a growth arrest of activated lymphocytes, keratinocytes, sebocytes and fibroblasts, as well as the activation of natural regulatory T cells (Tregs).
In parallel, the release of anti-inflammatory cytokines such as TGF-β1 and IL-35 is induced.
These effects are mediated via different signalling pathways.

Remarkably, also Th17 cells - the main pathogenic population of autoimmune disorders- are strongly suppressed by PETIR™ compounds.

In summary, PETIR™ act by four general mechanisms:

• Inhibition of DNA synthesis and proliferation of inflammatory cells
• Reduction of inflammatory cytokines (Th1, Th2 and Th17)
• Activation of CD4⁺CD25⁺ Treg cells (suppressor cells) and
• Induction of anti-inflammatory cytokines (TGF-β1, IL-35)