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Literature for peptidase S09.018: dipeptidyl-peptidase 8

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates 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.<br>Targeting dipeptidyl peptidase-8/9 to combat inflammation-induced osteoclastogenesis in RAW264.7 macrophages and analysis of anti-osteoclastogenesis potential of chrysin<br>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.<br>Sulphostin-inspired N-phosphonopiperidones as selective covalent DPP8 and DPP9 inhibitors<br>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.<br>Active site-directed probes targeting dipeptidyl peptidases 8 and 9<br>Eur J Med Chem (2024) 270, 116389-116389. PubMed  Europe PubMed DOI
    4. 2023
  4. Donzelli,L., Bolgi,O. and Geiss-Friedlander,R.<br>The amino-dipeptidyl peptidases DPP8 and DPP9: Purification and enzymatic assays<br>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.<br>Vildagliptin-Derived Dipeptidyl Peptidase 9 (DPP9) Inhibitors: Identification of a DPP8/9-Specific Lead<br>ChemMedChem (2022) 17, e202200097-e202200097. PubMed  Europe PubMed DOI  I
  6. Cui,C., Tian,X., Wei,L., Wang,Y., Wang,K. and Fu,R.<br>New insights into the role of dipeptidyl peptidase 8 and dipeptidyl peptidase 9 and their inhibitors<br>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.<br>DPP9 sequesters the C terminus of NLRP1 to repress inflammasome activation<br>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.<br>Dipeptidyl peptidase 9 sets a threshold for CARD8 inflammasome formation by sequestering its active C-terminal fragment<br>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.<br>DPP8/DPP9 inhibition elicits canonical Nlrp1b inflammasome hallmarks in murine macrophages<br>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.<br>A chemical strategy for protease substrate profiling<br>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.<br>Structures and mechanism of dipeptidyl peptidases 8 and 9, important players in cellular homeostasis and cancer<br>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.<br>DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis<br>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.<br>Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation<br>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.<br>The dipeptidyl peptidases 4, 8, and 9 in mouse monocytes and macrophages: dpp8/9 inhibition attenuates M1 macrophage activation in mice<br>Inflammation (2016) 39, 413-424. PubMed  Europe PubMed DOI
    15. 2015
  15. Huan,Y., Jiang,Q., Liu,J.-L. and Shen,Z.-F.<br>Establishment of a dipeptidyl peptidases (DPP) 8/9 expressing cell model for evaluating the selectivity of DPP4 inhibitors<br>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.<br>Grassypeptolides as natural inhibitors of dipeptidyl peptidase 8 and T-cell activation<br>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.<br>The SUMO1-E67 interacting loop peptide is an allosteric inhibitor of the dipeptidyl peptidases 8 and 9<br>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.<br>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<br>J Biol Chem (2013) 288, 13936-13949. PubMed  Europe PubMed DOI  P
  19. Zhang,H., Chen,Y., Keane,F.M. and Gorrell,M.D.<br>Advances in understanding the expression and function of dipeptidyl peptidase 8 and 9<br>Mol Cancer Res (2013) 11, 1487-1496. PubMed  Europe PubMed DOI
    20. 2012
  20. Abbott,C.A. and Gorrell,M.D.<br>Dipeptidyl peptidase 8<br>[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.<br>4-Substituted boro-proline dipeptides: synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities<br>Bioorg Med Chem Lett (2012) 22, 5536-5540. PubMed  Europe PubMed DOI  I
    22. 2011
  22. Chen,S.J. and Jiaang,W.T.<br>Current advances and therapeutic potential of agents targeting dipeptidyl peptidases-IV, -II, 8/9 and fibroblast activation protein<br>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.<br>Expression and spatial heterogeneity of dipeptidyl peptidases in endothelial cells of conduct vessels and capillaries<br>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.<br>Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?<br>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.<br>Inhibitor selectivity in the clinical application of dipeptidyl peptidase-4 inhibition<br>Clin Sci (Lond) (2010) 118, 31-41. PubMed  Europe PubMed DOI  I
  26. Pitman,M.R., Menz,R.I. and Abbott,C.A.<br>Hydrophilic residues surrounding the S1 and S2 pockets contribute to dimerisation and catalysis in human dipeptidyl peptidase 8 (DP8)<br>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.<br>Recent insights into the role of dipeptidyl aminopeptidase IV (DPIV) and aminopeptidase N (APN) families in immune functions<br>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.<br>Enzyme activity and immunohistochemical localization of dipeptidyl peptidase 8 and 9 in male reproductive tissues<br>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.<br>Dipeptidyl peptidase 8 and 9 - guilty by association?<br>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.<br>Role of dipeptidyl peptidase IV (DP IV)-like enzymes in T lymphocyte activation: investigations in DP IV/CD26-knockout mice<br>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.<br>Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor<br>Biochem Pharmacol (2009) 78, 203-210. PubMed  Europe PubMed DOI  I
  32. Yazbeck,R., Howarth,G.S. and Abbott,C.A.<br>Dipeptidyl peptidase inhibitors, an emerging drug class for inflammatory disease?<br>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.<br>The in vivo expression of dipeptidyl peptidases 8 and 9<br>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.<br>Stromal cell-derived factors 1alpha and 1beta, inflammatory protein-10 and interferon-inducible T cell chemo-attractant are novel substrates of dipeptidyl peptidase 8<br>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.<br>Adverse effects of dipeptidyl peptidases 8 and 9 inhibition in rodents revisited<br>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.<br>Purification and characterization of dipeptidyl peptidase IV-like enzymes from bovine testes<br>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.<br>Regulation of expression and function of dipeptidyl peptidase 4 (DP4), DP8/9, and DP10 in allergic responses of the lung in rats<br>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.<br>Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: Identification of dipeptide derived leads<br>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.<br>Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: Isoindoline containing inhibitors<br>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.<br>Neuropeptide Y (NPY) cleaving enzymes: structural and functional homologues of dipeptidyl peptidase 4<br>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.<br>Dipeptidyl peptidase 8/9-like activity in human leukocytes<br>J Leukoc Biol (2007) 81, 1252-1257. PubMed  Europe PubMed DOI
  42. Rummey,C. and Metz,G.<br>Homology models of dipeptidyl peptidases 8 and 9 with a focus on loop predictions near the active site<br>Proteins (2007) 66, 160-171. PubMed  Europe PubMed DOI  S
  43. Thornberry,N.A. and Weber,A.E.<br>Discovery of JANUVIA (Sitagliptin), a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes<br>Curr Top Med Chem (2007) 7, 557-568. PubMed  Europe PubMed DOI  I
  44. Van der Veken,P., Haemers,A. and Augustyns,K.<br>Prolyl peptidases related to dipeptidyl peptidase IV: potential of specific inhibitors in drug discovery<br>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.<br>Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates<br>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.<br>Selectivity among dipeptidyl peptidases of the S9b family<br>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.<br>Dipeptidyl peptidases 8 and 9: specificity and molecular characterization compared with dipeptidyl peptidase IV<br>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.<br>Investigation of the dimer interface and substrate specificity of prolyl dipeptidase DPP8<br>J Biol Chem (2006) 281, 38653-38662. PubMed  Europe PubMed DOI
  49. Pitman,M.R., Menz,R.I. and Abbott,C.A.<br>Prediction of dipeptidyl peptidase (DP) 8 structure by homology modelling<br>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.<br>Extraenzymatic functions of the dipeptidyl peptidase IV-related proteins DP8 and DP9 in cell adhesion, migration and apoptosis<br>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.<br>Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8<br>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.<br>Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9<br>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.<br>Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors<br>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.<br>Expression of a novel dipeptidyl peptidase 8 (DPP8) transcript variant, DPP8-v3, in human testis<br>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.<br>Purification and characterization of human prolyl dipeptidase DPP8 in Sf9 insect cells<br>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.<br>Cloning, expression and chromosomal localization of a novel human dipeptidyl peptidase (DPP) IV homolog, DPP8<br>Eur J Biochem (2000) 267, 6140-6150. PubMed  Europe PubMed DOI  E

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