An endopeptidase inhibitor is a drug that inhibits one or more endopeptidase enzymes. Endopeptidases are one of two types of proteases (enzymes that break down proteins and peptides), the other being exopeptidases. Endopeptidases cleave peptide bonds of non-terminal amino acids (that is, they cut proteins/peptides into two chains), whereas exopeptidases break terminal bonds, resulting in the release of a single amino acid or dipeptide from the peptide chain.
Examples of endopeptidase inhibitors Some examples of endopeptidase inhibitors include the following:
Neprilysin inhibitors Selective neprilysin inhibitors Candoxatril - prodrug to candoxatrilat Candoxatrilat - active metabolite of candoxatril Dexecadotril (retorphan) - (R)-enantiomer of racecadotril; prodrug to (R)-thiorphan Ecadotril (sinorphan) - (S)-enantiomer of racecadotril; prodrug to (S)-thiorphan Racecadotril (acetorphan) - racemic form of dexecadotril and ecadotril; prodrug to thiorphan Sacubitril - prodrug to sacubitrilat Sacubitrilat - active metabolite of sacubitril Thiorphan - active metabolite of racecadotril UK-414,495 Non-selective neprilysin inhibitors Aladotril - also inhibits angiotensin converting enzyme (ACE) (an exopeptidase) Alatriopril - also inhibits ACE Daglutril - also inhibits endothelin converting enzyme (ECE) (an exopeptidase) Fasidotril - also inhibits ACE Gemopatrilat - also inhibits ACE Ilepatril - also inhibits ACE Ketalorphan - also inhibits APN, ACE, and dipeptidyl-peptidase 3 (DPP-3) (an exopeptidase) Omapatrilat - also inhibits ACE Phosphoramidon - inhibitor of neprilysin and thermolysin; also inhibits ECE RB-101 - also inhibits aminopeptidase N (APN) (an exopeptidase) Sampatrilat Spinorphan - also inhibits APN, ACE, and DPP-3 Tynorphin - also inhibits APN, ACE, and DPP-3 Trypsin inhibitors/others Aloxistatin - inhibitor of cysteine proteases Benzamidine – inhibitor of serine Camostat - inhibitor of trypsin and various other proteases Ecallantide - kallikrein inhibitor Leupeptin - non-selective inhibitor of cysteine, serine, and threonine proteases Nafamostat - inhibitor of trypsin, tryptase, and various other serine proteases Pacifastins - trypsin and chymotrypsin inhibitor Patamostat - trypsin inhibitor Pepstatin - inhibitor of renin and various aspartyl proteases Sepimostat - inhibitor of serine proteases Sivelestat - inhibitor of neutrophil elastase Talopeptin - inhibitor of thermolysin and other metalloproteases Ulinastatin - inhibitor of trypsin and various other proteases Upamostat - serine protease inhibitor Renin inhibitors Aliskiren Ciprokiren Ditekiren Enalkiren Pepstatin Remikiren Terlakiren Zankiren
See also Exopeptidase inhibitor Enkephalinase inhibitor
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