Peptide linkage unit comprising methylene phosphinic acid

Details Peptide linkage unit comprising methylene phosphinic acid Peptide linkage unit comprising methylene phosphinic acid

C - Chemistry, Metallurgy

07

K

C07K 7/02 (2006.01) C07F 9/30 (2006.01) C07F 9/32 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2127295

2127295 9314114 PCTABS00024 A peptide linkage unit is employed for joining peptide and pseudopeptide sequences, including peptides and pseudopeptides that inhibit aspartic proteinase enzymes. The peptide linkage unit includes a phosphinate methylene ammonium linkage in place of a peptidyl carboxamide bond. If the peptide linkage unit is incorporated into a peptide sequence that would otherwise serve as an aspartic proteinase substrate and if it is positioned at a cleavage site within such peptide sequence, the phosphinate methylene ammonium linkage is resistant to cleavage and serves as an exploding transition state analog of such cleavage site. When so incorporated, the phosphinate methylene ammonium linkage can bind or interfere with the active site of aspartic proteinase enzymes and inhibit its activity. Preferred inhibitors contain a phosphinic acid methylene amine group joining the P1 and P1' residues and have a length of 3 to about 15 amino acid residues.

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