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Literature for peptidase S09.018: dipeptidyl-peptidase 8

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

(Topics flags: S Structure, R Splicing, P Specificity, I Inhibitor, E Expression, V Review. To select only the references relevant to a single topic, click the link above. See explanation.)

    2025
  1. Ahmad,S.S., Ahmed,F., Ahmad,S., Krishnan,A. and Khan,M.A.
    Targeting dipeptidyl peptidase-8/9 to combat inflammation-induced osteoclastogenesis in RAW264.7 macrophages and analysis of anti-osteoclastogenesis potential of chrysin
    Iran J Basic Med Sci (2025) 28, 516-526. PubMed  Europe PubMed DOI  PMC  EPMC
  2. Sewald,L., Tabak,W.W.A., Fehr,L., Zolg,S., Najdzion,M., Verhoef,C.J.A., Podlesainski,D., Geiss-Friedlander,R., Lammens,A., Kaschani,F., Hellerschmied,D., Huber,R. and Kaiser,M.
    Sulphostin-inspired N-phosphonopiperidones as selective covalent DPP8 and DPP9 inhibitors
    Nat Commun (2025) 16, 3208-3208. PubMed  Europe PubMed DOI  PMC  EPMC  I
    3. 2024
  3. Espadinha,M., De Loose,J., Corthaut,S., Thys,S., Van Rymenant,Y., Verhulst,E., Benramdane,S., Filippi,N., Augustyns,K., Van Wielendaele,P., Pintelon,I., De Meester,I. and Van der Veken,P.
    Active site-directed probes targeting dipeptidyl peptidases 8 and 9
    Eur J Med Chem (2024) 270, 116389-116389. PubMed  Europe PubMed DOI
    4. 2023
  4. Donzelli,L., Bolgi,O. and Geiss-Friedlander,R.
    The amino-dipeptidyl peptidases DPP8 and DPP9: Purification and enzymatic assays
    Methods Enzymol (2023) 684, 289-323. PubMed  Europe PubMed DOI
    5. 2022
  5. Benramdane,S., De Loose,J., Beyens,O., Van Rymenant,Y., Vliegen,G., Augustyns,K., De Winter,H., De Meester,I. and Van der Veken,P.
    Vildagliptin-Derived Dipeptidyl Peptidase 9 (DPP9) Inhibitors: Identification of a DPP8/9-Specific Lead
    ChemMedChem (2022) 17, e202200097-e202200097. PubMed  Europe PubMed DOI  I
  6. Cui,C., Tian,X., Wei,L., Wang,Y., Wang,K. and Fu,R.
    New insights into the role of dipeptidyl peptidase 8 and dipeptidyl peptidase 9 and their inhibitors
    Front Pharmacol (2022) 13, 1002871-1002871. PubMed  Europe PubMed DOI  PMC  EPMC  V
    7. 2021
  7. Hollingsworth,L.R., Sharif,H., Griswold,A.R., Fontana,P., Mintseris,J., Dagbay,K.B., Paulo,J.A., Gygi,S.P., Bachovchin,D.A. and Wu,H.
    DPP9 sequesters the C terminus of NLRP1 to repress inflammasome activation
    Nature (2021) PubMed  Europe PubMed DOI
  8. Sharif,H., Hollingsworth,L.R., Griswold,A.R., Hsiao,J.C., Wang,Q., Bachovchin,D.A. and Wu,H.
    Dipeptidyl peptidase 9 sets a threshold for CARD8 inflammasome formation by sequestering its active C-terminal fragment
    Immunity (2021) PubMed  Europe PubMed DOI
    9. 2019
  9. de Vasconcelos,N.M., Vliegen,G., Goncalves,A., De Hert,E., Martin-Perez,R., Van Opdenbosch,N., Jallapally,A., Geiss-Friedlander,R., Lambeir,A.M., Augustyns,K., Van der Veken,P., De Meester,I. and Lamkanfi,M.
    DPP8/DPP9 inhibition elicits canonical Nlrp1b inflammasome hallmarks in murine macrophages
    Life Sci Alliance (2019) 2 PubMed  Europe PubMed DOI  PMC  EPMC  I
  10. Griswold,A.R., Cifani,P., Rao,S.D., Axelrod,A.J., Miele,M.M., Hendrickson,R.C., Kentsis,A. and Bachovchin,D.A.
    A chemical strategy for protease substrate profiling
    Cell Chem Biol (2019) 26, 901-907. PubMed  Europe PubMed DOI
    11. 2018
  11. Ross,B., Krapp,S., Augustin,M., Kierfersauer,R., Arciniega,M., Geiss-Friedlander,R. and Huber,R.
    Structures and mechanism of dipeptidyl peptidases 8 and 9, important players in cellular homeostasis and cancer
    Proc Natl Acad Sci U S A (2018) 115, E1437-E1437. PubMed  Europe PubMed DOI  PMC  EPMC  S
    12. 2017
  12. Okondo,M.C., Johnson,D.C., Sridharan,R., Go,E.B., Chui,A.J., Wang,M.S., Poplawski,S.E., Wu,W., Liu,Y., Lai,J.H., Sanford,D.G., Arciprete,M.O., Golub,T.R., Bachovchin,W.W. and Bachovchin,D.A.
    DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis
    Nat Chem Biol (2017) 13, 46-53. PubMed  Europe PubMed DOI  I
    13. 2016
  13. Heirbaut,L., VanGoethem,S., Jansen,K., DeWinter,H., Lamoen,N., Joossens,J., Cheng,J., Chen,X., Lambeir,A.-M., DeMeester,I., Augustyns,K. and VanDer Veken,P.
    Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation
    MedChemComm (2016) 7, 433-438. DOI  I
  14. Waumans,Y., Vliegen,G., Maes,L., Rombouts,M., Declerck,K., Van der Veken,P., Vanden Berghe,W., De Meyer,G.R., Schrijvers,D. and De Meester,I.
    The dipeptidyl peptidases 4, 8, and 9 in mouse monocytes and macrophages: dpp8/9 inhibition attenuates M1 macrophage activation in mice
    Inflammation (2016) 39, 413-424. PubMed  Europe PubMed DOI
    15. 2015
  15. Huan,Y., Jiang,Q., Liu,J.-L. and Shen,Z.-F.
    Establishment of a dipeptidyl peptidases (DPP) 8/9 expressing cell model for evaluating the selectivity of DPP4 inhibitors
    J Pharmacol Toxicol Methods (2015) 71, 8-12. PubMed  Europe PubMed DOI  I
    16. 2014
  16. Kwan,J.C., Liu,Y., Ratnayake,R., Hatano,R., Kuribara,A., Morimoto,C., Ohnuma,K., Paul,V.J., Ye,T. and Luesch,H.
    Grassypeptolides as natural inhibitors of dipeptidyl peptidase 8 and T-cell activation
    Chembiochem (2014) 15, 799-804. PubMed  Europe PubMed DOI  I
    17. 2013
  17. Pilla,E., Kilisch,M., Lenz,C., Urlaub,H. and Geiss-Friedlander,R.
    The SUMO1-E67 interacting loop peptide is an allosteric inhibitor of the dipeptidyl peptidases 8 and 9
    J Biol Chem (2013) 288, 32787-32796. PubMed  Europe PubMed DOI  I
  18. Wilson,C.H., Indarto,D., Doucet,A., Pogson,L.D., Pitman,M.R., McNicholas,K., Menz,R.I., Overall,C.M. and Abbott,C.A.
    Identifying natural substrates for dipeptidyl peptidases 8 and 9 using terminal amine isotopic labeling of substrates (TAILS) reveals in vivo roles in cellular homeostasis and energy metabolism
    J Biol Chem (2013) 288, 13936-13949. PubMed  Europe PubMed DOI  P
  19. Zhang,H., Chen,Y., Keane,F.M. and Gorrell,M.D.
    Advances in understanding the expression and function of dipeptidyl peptidase 8 and 9
    Mol Cancer Res (2013) 11, 1487-1496. PubMed  Europe PubMed DOI
    20. 2012
  20. Abbott,C.A. and Gorrell,M.D.
    Dipeptidyl peptidase 8
    [ISSN:978-0-12-407742-3] (2012) 3, 3379-3384. DOI
  21. Wu,W., Liu,Y., Milo,L.J., Jr., Shu,Y., Zhao,P., Li,Y., Woznica,I., Yu,G., Sanford,D.G., Zhou,Y., Poplawski,S.E., Connolly,B.A., Sudmeier,J.L., Bachovchin,W.W. and Lai,J.H.
    4-Substituted boro-proline dipeptides: synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities
    Bioorg Med Chem Lett (2012) 22, 5536-5540. PubMed  Europe PubMed DOI  I
    22. 2011
  22. Chen,S.J. and Jiaang,W.T.
    Current advances and therapeutic potential of agents targeting dipeptidyl peptidases-IV, -II, 8/9 and fibroblast activation protein
    Curr Top Med Chem (2011) 11, 1447-1463. PubMed  Europe PubMed DOI  I
  23. Matheeussen,V., Baerts,L., De Meyer,G., De Keulenaer,G., Van der Veken,P., Augustyns,K., Dubois,V., Scharpe,S. and De Meester,I.
    Expression and spatial heterogeneity of dipeptidyl peptidases in endothelial cells of conduct vessels and capillaries
    Biol Chem (2011) 392, 189-198. PubMed  Europe PubMed DOI
  24. Van Goethem,S., Matheeussen,V., Joossens,J., Lambeir,A.M., Chen,X., De Meester,I., Haemers,A., Augustyns,K. and Van der Veken,P.
    Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?
    J Med Chem (2011) 54, 5737-5746. PubMed  Europe PubMed DOI  I
    25. 2010
  25. Kirby,M., Yu,D.M., O'Connor,S. and Gorrell,M.D.
    Inhibitor selectivity in the clinical application of dipeptidyl peptidase-4 inhibition
    Clin Sci (Lond) (2010) 118, 31-41. PubMed  Europe PubMed DOI  I
  26. Pitman,M.R., Menz,R.I. and Abbott,C.A.
    Hydrophilic residues surrounding the S1 and S2 pockets contribute to dimerisation and catalysis in human dipeptidyl peptidase 8 (DP8)
    Biol Chem (2010) 391, 959-972. PubMed  Europe PubMed DOI
    27. 2009
  27. Ansorge,S., Bank,U., Heimburg,A., Helmuth,M., Koch,G., Tadje,J., Lendeckel,U., Wolke,C., Neubert,K., Faust,J., Fuchs,P., Reinhold,D., Thielitz,A. and Tager,M.
    Recent insights into the role of dipeptidyl aminopeptidase IV (DPIV) and aminopeptidase N (APN) families in immune functions
    Clin Chem Lab Med (2009) 47, 253-261. PubMed  Europe PubMed DOI
  28. Dubois,V., Van Ginneken,C., de Cock,H., Lambeir,A.M., Van der Veken,P., Augustyns,K., Chen,X., Scharpe,S. and De Meester,I.
    Enzyme activity and immunohistochemical localization of dipeptidyl peptidase 8 and 9 in male reproductive tissues
    J Histochem Cytochem (2009) 57, 531-541. PubMed  Europe PubMed DOI  PMC  EPMC
  29. Pitman,M.R., Sulda,M.L., Kuss,B. and Abbott,C.A.
    Dipeptidyl peptidase 8 and 9 - guilty by association?
    Front Biosci (2009) 14, 3619-3633. PubMed  Europe PubMed  V
  30. Reinhold,D., Goihl,A., Wrenger,S., Reinhold,A., Kuhlmann,U.C., Faust,J., Neubert,K., Thielitz,A., Brocke,S., Tager,M., Ansorge,S. and Bank,U.
    Role of dipeptidyl peptidase IV (DP IV)-like enzymes in T lymphocyte activation: investigations in DP IV/CD26-knockout mice
    Clin Chem Lab Med (2009) 47, 268-274. PubMed  Europe PubMed DOI  I
  31. Wu,J.J., Tang,H.K., Yeh,T.K., Chen,C.M., Shy,H.S., Chu,Y.R., Chien,C.H., Tsai,T.Y., Huang,Y.C., Huang,Y.L., Huang,C.H., Tseng,H.Y., Jiaang,W.T., Chao,Y.S. and Chen,X.
    Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor
    Biochem Pharmacol (2009) 78, 203-210. PubMed  Europe PubMed DOI  I
  32. Yazbeck,R., Howarth,G.S. and Abbott,C.A.
    Dipeptidyl peptidase inhibitors, an emerging drug class for inflammatory disease?
    Trends Pharmacol Sci (2009) 30, 600-607. PubMed  Europe PubMed DOI  I
  33. Yu,D.M., Ajami,K., Gall,M.G., Park,J., Lee,C.S., Evans,K.A., McLaughlin,E.A., Pitman,M.R., Abbott,C.A., McCaughan,G.W. and Gorrell,M.D.
    The in vivo expression of dipeptidyl peptidases 8 and 9
    J Histochem Cytochem (2009) 57, 1025-1040. PubMed  Europe PubMed DOI  PMC  EPMC
    34. 2008
  34. Ajami,K., Pitman,M.R., Wilson,C.H., Park,J., Menz,R.I., Starr,A.E., Cox,J.H., Abbott,C.A., Overall,C.M. and Gorrell,M.D.
    Stromal cell-derived factors 1alpha and 1beta, inflammatory protein-10 and interferon-inducible T cell chemo-attractant are novel substrates of dipeptidyl peptidase 8
    FEBS Lett (2008) 582, 819-825. PubMed  Europe PubMed DOI  P
  35. Burkey,B.F., Hoffmann,P.K., Hassiepen,U., Trappe,J., Juedes,M. and Foley,J.E.
    Adverse effects of dipeptidyl peptidases 8 and 9 inhibition in rodents revisited
    Diabetes Obes Metab (2008) 10, 1057-1061. PubMed  Europe PubMed DOI
  36. Dubois,V., Lambeir,A.M., Van der Veken,P., Augustyns,K., Creemers,J., Chen,X., Scharpe,S. and De Meester,I.
    Purification and characterization of dipeptidyl peptidase IV-like enzymes from bovine testes
    Front Biosci (2008) 13, 3558-3568. PubMed  Europe PubMed DOI
  37. Schade,J., Stephan,M., Schmiedl,A., Wagner,L., Niestroj,A.J., Demuth,H.U., Frerker,N., Klemann,C., Raber,K.A., Pabst,R. and von Horsten,S.
    Regulation of expression and function of dipeptidyl peptidase 4 (DP4), DP8/9, and DP10 in allergic responses of the lung in rats
    J Histochem Cytochem (2008) 56, 147-155. PubMed  Europe PubMed DOI  PMC  EPMC
  38. Van der Veken,P., De Meester,I., Dubois,V., Soroka,A., Van Goethem,S., Maes,M.B., Brandt,I., Lambeir,A.M., Chen,X., Haemers,A., Scharpe,S. and Augustyns,K.
    Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: Identification of dipeptide derived leads
    Bioorg Med Chem Lett (2008) 18, 4154-4158. PubMed  Europe PubMed DOI  I
  39. Van Goethem,S., Van der Veken,P., Dubois,V., Soroka,A., Lambeir,A.M., Chen,X., Haemers,A., Scharpe,S., De Meester,I. and Augustyns,K.
    Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: Isoindoline containing inhibitors
    Bioorg Med Chem Lett (2008) 18, 4159-4162. PubMed  Europe PubMed DOI  I
    40. 2007
  40. Frerker,N., Wagner,L., Wolf,R., Heiser,U., Hoffmann,T., Rahfeld,J.U., Schade,J., Karl,T., Naim,H.Y., Alfalah,M., Demuth,H.U. and von Horsten,S.
    Neuropeptide Y (NPY) cleaving enzymes: structural and functional homologues of dipeptidyl peptidase 4
    Peptides (2007) 28, 257-268. PubMed  Europe PubMed DOI
  41. Maes,M.B., Dubois,V., Brandt,I., Lambeir,A.M., Van der Veken,P., Augustyns,K., Cheng,J.D., Chen,X., Scharpe,S. and De Meester,I.
    Dipeptidyl peptidase 8/9-like activity in human leukocytes
    J Leukoc Biol (2007) 81, 1252-1257. PubMed  Europe PubMed DOI
  42. Rummey,C. and Metz,G.
    Homology models of dipeptidyl peptidases 8 and 9 with a focus on loop predictions near the active site
    Proteins (2007) 66, 160-171. PubMed  Europe PubMed DOI  S
  43. Thornberry,N.A. and Weber,A.E.
    Discovery of JANUVIA (Sitagliptin), a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
    Curr Top Med Chem (2007) 7, 557-568. PubMed  Europe PubMed DOI  I
  44. Van der Veken,P., Haemers,A. and Augustyns,K.
    Prolyl peptidases related to dipeptidyl peptidase IV: potential of specific inhibitors in drug discovery
    Curr Top Med Chem (2007) 7, 621-635. PubMed  Europe PubMed DOI  V
  45. Van der Veken,P., Soroka,A., Brandt,I., Chen,Y.S., Maes,M.B., Lambeir,A.M., Chen,X., Haemers,A., Scharpe,S., Augustyns,K. and De Meester,I.
    Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates
    J Med Chem (2007) 50, 5568-5570. PubMed  Europe PubMed DOI  I
    46. 2006
  46. Bjelke,J.R., Kanstrup,A.B. and Rasmussen,H.B.
    Selectivity among dipeptidyl peptidases of the S9b family
    Cell Mol Biol Incl Cyto Enzymol (2006) 52, 3-7. PubMed  Europe PubMed DOI  P
  47. [YEAR:13-2-2006]Bjelke,J.R., Christensen,J., Nielsen,P.F., Branner,S., Kanstrup,A.B., Wagtmann,N. and Rasmussen,H.B.
    Dipeptidyl peptidases 8 and 9: specificity and molecular characterization compared with dipeptidyl peptidase IV
    Biochem J (13-2-2006) 396, 391-399. PubMed  Europe PubMed DOI  PMC  EPMC  P
  48. Lee,H.J., Chen,Y.S., Chou,C.Y., Chien,C.H., Lin,C.H., Chang,G.G. and Chen,X.
    Investigation of the dimer interface and substrate specificity of prolyl dipeptidase DPP8
    J Biol Chem (2006) 281, 38653-38662. PubMed  Europe PubMed DOI
  49. Pitman,M.R., Menz,R.I. and Abbott,C.A.
    Prediction of dipeptidyl peptidase (DP) 8 structure by homology modelling
    Adv Exp Med Biol (2006) 575, 33-42. PubMed  Europe PubMed DOI
  50. Yu,D.M., Wang,X.M., McCaughan,G.W. and Gorrell,M.D.
    Extraenzymatic functions of the dipeptidyl peptidase IV-related proteins DP8 and DP9 in cell adhesion, migration and apoptosis
    FEBS J (2006) 273, 2447-2460. PubMed  Europe PubMed DOI
    51. 2005
  51. Jiaang,W.T., Chen,Y.S., Hsu,T., Wu,S.H., Chien,C.H., Chang,C.N., Chang,S.P., Lee,S.J. and Chen,X.
    Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8
    Bioorg Med Chem Lett (2005) 15, 687-691. PubMed  Europe PubMed DOI  I
  52. Lankas,G.R., Leiting,B., Roy,R.S., Eiermann,G.J., Beconi,M.G., Biftu,T., Chan,C.C., Edmondson,S., Feeney,W.P., He,H., Ippolito,D.E., Kim,D., Lyons,K.A., Ok,H.O., Patel,R.A., Petrov,A.N., Pryor,K.A., Qian,X., Reigle,L., Woods,A., Wu,J.K., Zaller,D., Zhang,X., Zhu,L., Weber,A.E. and Thornberry,N.A.
    Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9
    Diabetes (2005) 54, 2988-2994. PubMed  Europe PubMed DOI  I
  53. [YEAR:1-7-2005]Lu,I.L., Lee,S.J., Tsu,H., Wu,S.Y., Kao,K.H., Chien,C.H., Chang,Y.Y., Chen,Y.S., Cheng,J.H., Chang,C.N., Chen,T.W., Chang,S.P., Chen,X. and Jiaang,W.T.
    Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors
    Bioorg Med Chem Lett (1-7-2005) 15, 3271-3275. PubMed  Europe PubMed DOI  I
  54. Zhu,H., Zhou,Z.M., Lu,L., Xu,M., Wang,H., Li,J.M. and Sha,J.H.
    Expression of a novel dipeptidyl peptidase 8 (DPP8) transcript variant, DPP8-v3, in human testis
    Asian J Androl (2005) 7, 245-255. PubMed  Europe PubMed DOI  R
    55. 2004
  55. Chen,Y.S., Chien,C.H., Goparaju,C.M., Hsu,J.T., Liang,P.H. and Chen,X.
    Purification and characterization of human prolyl dipeptidase DPP8 in Sf9 insect cells
    Protein Expr Purif (2004) 35, 142-146. PubMed  Europe PubMed DOI
    56. 2000
  56. Abbott,C.A., Yu,D.M., Woollatt,E., Sutherland,G.R., McCaughan,G.W. and Gorrell,M.D.
    Cloning, expression and chromosomal localization of a novel human dipeptidyl peptidase (DPP) IV homolog, DPP8
    Eur J Biochem (2000) 267, 6140-6150. PubMed  Europe PubMed DOI  E

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