PHOSHINIC PSEUDOPEPTIDE DERIVATIVES FOR POTENT INHIBITION OF AMINOPEPTIDASES OF THE OXYTOCINASE SUBFAMILY OF M1 AMINOPEPTIDASES

摘要

This invention relates to the use of phosphinic pseudopeptide derivatives for the production of medicaments that inhibit the action of aminopeptidases of the oxytocinase sub-family of M1 aminopeptidases that includes ERAP1, ERAP2 and 1RAP (also known as PLAP). These derivatives are of formula A: (chemical formula) where R1 and R2 correspond to natural or un-natural amino acid side chains, R3 corresponds to an amino (-NH2) group or a peptide sequence bearing at their carboxy terminus a hydroxyl or an amino group and R4 corresponds to a hydrogen atom or a counterion. Applications: For the modulation of antigen processing leading to altered cell-surface antigen presentation and altered or novel cytotoxic T-cell or NK-cell responses for the treatment of viral and bacterial infections, autoimmunity or cancer immunotherapy.