Literature for peptidase C01.070: dipeptidyl-peptidase I

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Inhibitors Pharma

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    2025
  1. Zhang,D., Zhang,W., Hu,P. and Zhang,W.
    Dipeptidyl peptidase 1 inhibitors for inflammatory respiratory diseases: mechanisms, clinical trials, and therapeutic prospects
    Front Pharmacol (2025) 16, 1656316-1656316. PubMed  Europe PubMed DOI  PMC  EPMC  I
  2. Zhou,F.L., Zhang,Y., Chang,C., Shi,D.X., Chen,X., Liu,X.H. and Shen,X.B.
    Identification of Marrubiin as a Cathepsin C Inhibitor for Treating Rheumatoid Arthritis
    Molecules (2025) 30 PubMed  Europe PubMed DOI  PMC  EPMC  I
  3. 2024
  4. Nishibata,Y., Arai,S., Taniguchi,M., Nakade,I., Ogawa,H., Kitano,S., Hosoi,Y., Shindo,A., Nishiyama,R., Masuda,S., Nakazawa,D., Tomaru,U., Shimizu,T., Sinko,W., Nagakura,T., Terada,Y. and Ishizu,A.
    Cathepsin C inhibition reduces neutrophil serine protease activity and improves activated neutrophil-mediated disorders
    Nat Commun (2024) 15, 6519-6519. PubMed  Europe PubMed DOI  PMC  EPMC  I
  5. 2023
  6. Chalmers,J.D., Gupta,A., Chotirmall,S.H., Armstrong,A., Eickholz,P., Hasegawa,N., McShane,P.J., O'Donnell,A.E., Shteinberg,M., Watz,H., Eleftheraki,A., Diefenbach,C. and Sauter,W.
    A Phase 2 randomised study to establish efficacy, safety and dosing of a novel oral cathepsin C inhibitor, BI 1291583, in adults with bronchiectasis: Airleaf
    ERJ Open Res (2023) 9 PubMed  Europe PubMed DOI  PMC  EPMC  I
  7. Kreideweiss,S., Schänzle,G., Schnapp,G., Vintonyak,V. and Grundl,M.A.
    BI 1291583: a novel selective inhibitor of cathepsin C with superior in vivo profile for the treatment of bronchiectasis
    Inflamm Res (2023) 72, 1709-1717. PubMed  Europe PubMed  I
  8. 2022
  9. Chen,X., Yan,Y., Du,J., Shen,X., He,C., Pan,H., Zhu,J. and Liu,X.
    Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo
    Eur J Med Chem (2022) 236, 114368-114368. PubMed  Europe PubMed DOI  I
  10. 2021
  11. Banerjee,A., Velagaleti,R., Patil,S., Pawar,M., Yadav,P., Kadam,P., Qadri,M.M., Chakraborti,S., Saini,J.S., Behera,D.B., Karanjai,K., Iyer,P.S., Gharat,L.A. and Das,S.
    Development of potent and selective Cathepsin C inhibitors free of aortic binding liability by application of a conformational restriction strategy
    Bioorg Med Chem Lett (2021) 47, 128202-128202. PubMed  Europe PubMed DOI  I
  12. Chen,X., Yan,Y., Zhang,Z., Zhang,F., Liu,M., Du,L., Zhang,H., Shen,X., Zhao,D., Shi,J.B. and Liu,X.
    Discovery and In Vivo Anti-inflammatory Activity Evaluation of a Novel Non-peptidyl Non-covalent Cathepsin C Inhibitor
    J Med Chem (2021) 64, 11857-11885. PubMed  Europe PubMed DOI  I
  13. Shen,X.B., Chen,X., Zhang,Z.Y., Wu,F.F. and Liu,X.H.
    Cathepsin C inhibitors as anti-inflammatory drug discovery: Challenges and opportunities
    Eur J Med Chem (2021) 225, 113818-113818. PubMed  Europe PubMed DOI  I
  14. 2020
  15. Chalmers,J.D., Haworth,C.S., Metersky,M.L., Loebinger,M.R., Blasi,F., Sibila,O., O'Donnell,A.E., Sullivan,E.J., Mange,K.C., Fernandez,C., Zou,J. and Daley,C.L.
    Phase 2 Trial of the DPP-1 Inhibitor Brensocatib in Bronchiectasis
    N Engl J Med (2020) PubMed  Europe PubMed DOI  I
  16. Khaket,T.P., Singh,M.P., Khan,I. and Kang,S.C.
    In vitro and in vivo studies on potentiation of curcumin-induced lysosomal-dependent apoptosis upon silencing of cathepsin C in colorectal cancer cells
    Pharmacol Res (2020) 161, 105156-105156. PubMed  Europe PubMed DOI  I
  17. 2019
  18. Hou,W., Sun,H., Ma,Y., Liu,C. and Zhang,Z.
    Identification and optimization of novel cathepsin C inhibitors derived from EGFR inhibitors
    J Med Chem (2019) 62, 5901-5919. PubMed  Europe PubMed DOI  I
  19. Rehm,S.R.T., Smirnova,N.F., Morrone,C., Gotzfried,J., Feuchtinger,A., Pedersen,J., Korkmaz,B., Yildirim,A.O. and Jenne,D.E.
    Premedication with a cathepsin C inhibitor alleviates early primary graft dysfunction in mouse recipients after lung transplantation
    Sci Rep (2019) 9, 9925-9925. PubMed  Europe PubMed DOI  PMC  EPMC  I
  20. 2018
  21. Palmer,R., Maenpaa,J., Jauhiainen,A., Larsson,B., Mo,J., Russell,M., Root,J., Prothon,S., Chialda,L., Forte,P., Egelrud,T., Stenvall,K. and Gardiner,P.
    Dipeptidyl peptidase 1 inhibitor AZD7986 induces a sustained, exposure-dependent reduction in neutrophil elastase activity in healthy subjects
    Clin Pharmacol Ther (2018) 104, 1155-1164. PubMed  Europe PubMed DOI  I
  22. 2017
  23. Chu,Y., Guo,Y., Walls,A.F. and Zhou,X.
    The regulatory role of dipeptidyl peptidase I on the activation of immune granulocytes
    Cell Biol Int (2017) 41, 1093-1102. PubMed  Europe PubMed DOI  I
  24. Guarino,C., Hamon,Y., Croix,C., Lamort,A.S., Dallet-Choisy,S., Marchand-Adam,S., Lesner,A., Baranek,T., Viaud-Massuard,M.C., Lauritzen,C., Pedersen,J., Heuze-Vourc'h,N., Si-Tahar,M., Firatli,E., Jenne,D.E., Gauthier,F., Horwitz,M.S., Borregaard,N. and Korkmaz,B.
    Prolonged pharmacological inhibition of cathepsin C results in elimination of neutrophil serine proteases
    Biochem Pharmacol (2017) 131, 52-67. PubMed  Europe PubMed DOI  I
  25. Lenartowicz,P., Makowski,M., Oszywa,B., Haremza,K., Latajka,R., Pawelczak,M. and Kafarski,P.
    Addition of thiols to the double bond of dipeptide C-terminal dehydroalanine as a source of new inhibitors of cathepsin C
    Biochimie (2017) 139, 46-55. PubMed  Europe PubMed DOI  I
  26. 2016
  27. Doyle,K., Lönn,H., Käck,H., Van,d., Swallow,S., Gardiner,P., Connolly,S., Root,J., Wikell,C., Dahl,G., Stenvall,K. and Johannesson,P.
    Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986)
    J Med Chem (2016) 59, 9457-9472. PubMed  Europe PubMed DOI  I
  28. Szczesniak,P., Pieczykolan,M. and Stecko,S.
    The synthesis of alpha,alpha-disubstituted alpha-amino acids via Ichikawa rearrangement
    J Org Chem (2016) 81, 1057-1074. PubMed  Europe PubMed DOI  I
  29. 2015
  30. Bragg,R.A., Brocklehurst,S., Gustafsson,F., Goodman,J., Hickling,K., Macfaul,P.A., Swallow,S. and Tugwood,J.
    Aortic Binding of AZD5248: Mechanistic Insight and Reactivity Assays To Support Lead Optimzation
    Chem Res Toxicol (2015) 28, 1991-1999. PubMed  Europe PubMed DOI  I
  31. Makowski,M., Lenartowicz,P., Oszywa,B., Jewginski,M., Pawelczak,M. and Kafarski,P.
    Synthesis of dehydrodipeptide esters and their evaluation as inhibitors of cathepsin C
    Med Chem Res (2015) 24, 3157-3165. PubMed  Europe PubMed DOI  I
  32. 2014
  33. Furber,M., Tiden,A.K., Gardiner,P., Mete,A., Ford,R., Millichip,I., Stein,L., Mather,A., Kinchin,E., Luckhurst,C., Barber,S., Cage,P., Sanganee,H., Austin,R., Chohan,K., Beri,R., Thong,B., Wallace,A., Oreffo,V., Hutchinson,R., Harper,S., Debreczeni,J., Breed,J., Wissler,L. and Edman,K.
    Cathepsin C inhibitors: property optimization and identification of a clinical candidate
    J Med Chem (2014) 57, 2357-2367. PubMed  Europe PubMed DOI  I
  34. 2013
  35. Drag,M., Wieczerzak,E., Pawelczak,M., Berlicki,L., Grzonka,Z. and Kafarski,P.
    Toward very potent, non-covalent organophosphonate inhibitors of cathepsin C and related enzymes by 2-amino-1-hydroxy-alkanephosphonates dipeptides
    Biochimie (2013) 95, 1640-1649. PubMed  Europe PubMed DOI  I
  36. Radzey,H., Rethmeier,M., Klimpel,D., Grundhuber,M., Sommerhoff,C.P. and Schaschke,N.
    E-64c-hydrazide: a lead structure for the development of irreversible cathepsin C inhibitors
    ChemMedChem (2013) 8, 1314-1321. PubMed  Europe PubMed DOI  I
  37. 2011
  38. Laine,D., Palovich,M., McCleland,B., Petitjean,E., Delhom,I., Xie,H., Deng,J., Lin,G., Davis,R., Jolit,A., Nevins,N., Zhao,B., Villa,J., Schneck,J., McDevitt,P., Midgett,R., Kmett,C., Umbrecht,S., Peck,B., Davis,A.B. and Bettoun,D.
    Discovery of novel cyanamide-based inhibitors of cathepsin C
    ACS Med Chem Lett (2011) 2, 142-147. PubMed  Europe PubMed DOI  I
  39. 2010
  40. Frizler,M., Stirnberg,M., Sisay,M.T. and Gutschow,M.
    Development of nitrile-based peptidic inhibitors of cysteine cathepsins
    Curr Top Med Chem (2010) 10, 294-322. PubMed  Europe PubMed DOI  T  I
  41. Guay,D., Beaulieu,C. and Percival,M.D.
    Therapeutic utility and medicinal chemistry of cathepsin C inhibitors
    Curr Top Med Chem (2010) 10, 708-716. PubMed  Europe PubMed DOI  V  I
  42. Laine,D.I. and Busch-Petersen,J.
    Inhibitors of cathepsin C (dipeptidyl peptidase I)
    Expert Opin Ther Pat (2010) 20, 497-506. PubMed  Europe PubMed DOI  V  I
  43. 2009
  44. Guay,D., Beaulieu,C., Jagadeeswar Reddy,T., Zamboni,R., Methot,N., Rubin,J., Ethier,D. and Percival,M.D.
    Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C
    Bioorg Med Chem Lett (2009) 19, 5392-5396. PubMed  Europe PubMed DOI  I
  45. 2008
  46. Latajka,R., Jewginski,M., Makowski,M., Pawelczak,M., Huber,T., Sewald,N. and Kafarski,P.
    Pentapeptides containing two dehydrophenylalanine residues - synthesis, structural studies and evaluation of their activity towards cathepsin C
    J Pept Sci (2008) 14, 1084-1095. PubMed  Europe PubMed DOI  I
  47. Methot,N., Guay,D., Rubin,J., Ethier,D., Ortega,K., Wong,S., Normandin,D., Beaulieu,C., Reddy,T.J., Riendeau,D. and Percival,M.D.
    In vivo inhibition of serine protease processing requires a high fractional inhibition of cathepsin C
    Mol Pharmacol (2008) 73, 1857-1865. PubMed  Europe PubMed DOI  T  I
  48. 2007
  49. Methot,N., Rubin,J., Guay,D., Beaulieu,C., Ethier,D., Reddy,T.J., Riendeau,D. and Percival,M.D.
    Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing
    J Biol Chem (2007) 282, 20836-20846. PubMed  Europe PubMed DOI  I
  50. Molgaard,A., Arnau,J., Lauritzen,C., Larsen,S., Petersen,G. and Pedersen,J.
    The crystal structure of human dipeptidyl peptidase I (cathepsin C) in complex with the inhibitor Gly-Phe-CHN2
    Biochem J (2007) 401, 645-650. PubMed  Europe PubMed DOI  PMC  EPMC  S  I
  51. 2006
  52. [YEAR:26-4-2006]Bondebjerg,J., Fuglsang,H., Valeur,K.R., Pedersen,J. and Naerum,L.
    Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors
    Bioorg Med Chem Lett (26-4-2006) 16, 3614-3617. PubMed  Europe PubMed DOI  I
  53. [YEAR:3-5-2006]Yuan,F., Verhelst,S.H., Blum,G., Coussens,L.M. and Bogyo,M.
    A selective activity-based probe for the papain family cysteine protease dipeptidyl peptidase I/cathepsin C
    J Am Chem Soc (3-5-2006) 128, 5616-5617. PubMed  Europe PubMed DOI  I
  54. 2005
  55. [YEAR:11-5-2005]Bondebjerg,J., Fuglsang,H., Valeur,K.R., Kaznelson,D.W., Hansen,J.A., Pedersen,R.O., Krogh,B.O., Jensen,B.S., Lauritzen,C., Petersen,G., Pedersen,J. and Naerum,L.
    Novel semicarbazide-derived inhibitors of human dipeptidyl peptidase I (hDPPI)
    Bioorg Med Chem (11-5-2005) 13, 4408-4424. PubMed  Europe PubMed DOI  I
  56. 2004
  57. Kam,C.M., Gotz,M.G., Koot,G., McGuire,M., Thiele,D., Hudig,D. and Powers,J.C.
    Design and evaluation of inhibitors for dipeptidyl peptidase I (cathepsin C)
    Arch Biochem Biophys (2004) 427, 123-134. PubMed  Europe PubMed DOI  I
  58. [YEAR:21-6-2004]Mucha,A., Pawel,M., Hurek,J. and Kafarski,P.
    Synthesis and activity of phosphinic tripeptide inhibitors of cathepsin C
    Bioorg Med Chem Lett (21-6-2004) 14, 3113-3116. PubMed  Europe PubMed DOI  I
  59. 2003
  60. [YEAR:1-12-2003]Sheth,P.D., Pedersen,J., Walls,A.F. and McEuen,A.R.
    Inhibition of dipeptidyl peptidase I in the human mast cell line HMC-1: blocked activation of tryptase, but not of the predominant chymotryptic activity
    Biochem Pharmacol (1-12-2003) 66, 2251-2262. PubMed  Europe PubMed DOI  I
  61. 2001
  62. Korver,G.E., Kam,C.M., Powers,J.C. and Hudig,D.
    Dipeptide vinyl sulfones suitable for intracellular inhibition of dipeptidyl peptidase I
    Int Immunopharmacol (2001) 1, 21-32. PubMed  Europe PubMed DOI  I
  63. 2000
  64. Horn,M., Pavlik,M., Doleckova,L., Baudys,M. and Mares,M.
    Arginine-based structures are specific inhibitors of cathepsin C. Application of peptide combinatorial libraries
    Eur J Biochem (2000) 267, 3330-3336. PubMed  Europe PubMed DOI  I
  65. 1998
  66. [YEAR:16-1-1998]Pham,C.T., Thomas,D.A., Mercer,J.D. and Ley,T.J.
    Production of fully active recombinant murine granzyme B in yeast
    J Biol Chem (16-1-1998) 273, 1629-1633. PubMed  Europe PubMed DOI  E  I
  67. 1997
  68. Thiele,D.L., McGuire,M.J. and Lipsky,P.E.
    A selective inhibitor of dipeptidyl peptidase I impairs generation of CD8+ T cell cytotoxic effector function
    J Immunol (1997) 158, 5200-5210. PubMed  Europe PubMed  I
  69. 1992
  70. Nikawa,T., Towatari,T. and Katunuma,N.
    Purification and characterization of cathepsin J from rat liver
    Eur J Biochem (1992) 204, 381-393. PubMed  Europe PubMed  I
  71. 1989
  72. [YEAR:15-8-1989]Angliker,H., Wikstrom,P., Kirschke,H. and Shaw,E.
    The inactivation of the cysteinyl exopeptidases cathepsin H and C by affinity-labelling reagents
    Biochem J (15-8-1989) 262, 63-68. PubMed  Europe PubMed  PMC  EPMC  I
  73. 1986
  74. Thompson,S.A., Andrews,P.R. and Hanzlik,R.P.
    Carboxyl-modified amino acids and peptides as protease inhibitors
    J Med Chem (1986) 29, 104-111. PubMed  Europe PubMed  I
  75. 1975
  76. [YEAR:2-12-1975]Metrione,R.M. and MacGeorge,N.L.
    The mechanism of action of dipeptidyl aminopeptidase. Inhibition by amino acid derivatives and amines; activation by aromatic compounds
    Biochemistry (2-12-1975) 14, 5249-5252. PubMed  Europe PubMed  I