• Source: Endopeptidase inhibitor

      • 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
      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


      References

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