Benramdane S, De Loose J, Filippi N, Espadinha M, Beyens O, Rymenant YV, Dirkx L, Bozdag M, Feijens PB, Augustyns K, Caljon G, De Winter H, De Meester I, Van der Veken P (2023)
Highly Selective Inhibitors of Dipeptidyl Peptidase 9 (DPP9) Derived from the Clinically Used DPP4-Inhibitor Vildagliptin
Journal of Medicinal Chemistry
Benramdane S, De Loose J, Beyens O, Van Rymenant Y, Vliegen G, Augustyns K, De Winter H, De Meester I, Van der Veken P (2022)
Vildagliptin-Derived Dipeptidyl Peptidase 9 (DPP9) Inhibitors: Identification of a DPP8/9-Specific Lead
ChemMedChem
Moon ES, Elvas F, Vliegen G, De Lombaerde S, Vangestel C, De Bruycker S, Bracke A, Eppard E, Greifenstein L, Klasen B, Kramer V, Staelens S, De Meester I, Van der Veken P, Rosch F (2020)
Targeting fibroblast activation protein (FAP): next generation PET radiotracers using squaramide coupled bifunctional DOTA and DATA(5m) chelators
EJNMMI Radiopharm Chem 5: 19
Bracke A, Van Elzen R, Van der Veken P, Augustyns K, De Meester I, Lambeir AM (2019)
The development and validation of a combined kinetic fluorometric activity assay for fibroblast activation protein alpha and prolyl oligopeptidase in plasma
Clinica Chimica Acta 495: 154
de Vasconcelos NM, Vliegen G, Goncalves A, De Hert E, Martin-Perez R, Van Opdenbosch N, Jallapally A, Geiss-Friedlander R, Lambeir AM, Augustyns K, Van der Veken P, De Meester I, Lamkanfi M (2019)
DPP8/DPP9 inhibition elicits canonical Nlrp1b inflammasome hallmarks in murine macrophages
Life Sciences Alliance 2:
Rea D, Van Elzen R, De Winter H, Van Goethem S, Landuyt B, Luyten W, Schoofs L, Van der Veken P, Augustyns K, De Meester I, Fulop V, Lambeir AM (2017)
Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling
Eur Journal of Medicinal Chemistry 139: 482
Van Elzen R, Schoenmakers E, Brandt I, Van der Veken P, Lambeir AM (2017)
Ligand-induced conformational changes in prolyl oligopeptidase: a kinetic approach
Protein Engineering Des Sel 30: 217
Kehoe K, Van Elzen R, Verkerk R, Sim Y, Van der Veken P, Lambeir AM, De Meester I (2016)
Prolyl carboxypeptidase purified from human placenta: its characterization and identification as an apelin-cleaving enzyme
Biochimica & Biophysica Acta 1864: 1481
Waumans Y, Vliegen G, Maes L, Rombouts M, Declerck K, Van der Veken P, Vanden Berghe W, De Meyer GRY, Schrijvers D, De Meester I (2016)
The Dipeptidyl Peptidases 4, 8, and 9 in Mouse Monocytes and Macrophages: DPP8/9 Inhibition Attenuates M1 Macrophage Activation in Mice
Inflammation 39: 413
Jansen K, Heirbaut L, Verkerk R, Cheng JD, Joossens J, Cos P, Maes L, Lambeir AM, De Meester I, Augustyns K, Van der Veken P (2014)
Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP)
Journal of Medicinal Chemistry 57: 3053
Jansen K, Heirbaut L, Cheng JD, Joossens J, Ryabtsova O, Cos P, Maes L, Lambeir AM, De Meester I, Augustyns K, Van der Veken P (2013)
Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold
ACS Med Chem Lett 4: 491
Kehoe K, Verkerk R, Sim Y, Waumans Y, Van der Veken P, Lambeir AM, De Meester I (2013)
Validation of a specific prolylcarboxypeptidase activity assay and its suitability for plasma and serum measurements
Analytical Biochemistry 443: 232
Matheeussen V, Waumans Y, Martinet W, Van Goethem S, Van der Veken P, Scharpe S, Augustyns K, De Meyer GR, De Meester I (2013)
Dipeptidyl peptidases in atherosclerosis: expression and role in macrophage differentiation, activation and apoptosis
Basic Res Cardiol 108: 350
Klimaviciusa L, Jain RK, Jaako K, Van Elzen R, Gerard M, Van der Veken P, Lambeir AM, Zharkovsky A (2012)
In situ prolyl oligopeptidase activity assay in neural cell cultures
Journal of Neuroscience Methodsods 204: 104
Matheeussen V, Lambeir AM, Jungraithmayr W, Gomez N, Mc Entee K, Van der Veken P, Scharpe S, De Meester I (2012)
Method comparison of dipeptidyl peptidase IV activity assays and their application in biological samples containing reversible inhibitors
Clinica Chimica Acta 413: 456
Myohanen TT, Hannula MJ, Van Elzen R, Gerard M, Van der Veken P, Garcia-Horsman JA, Baekelandt V, Mannisto PT, Lambeir AM (2012)
A prolyl oligopeptidase inhibitor, KYP-2047, reduces alpha-synuclein protein levels and aggregates in cellular and animal models of Parkinson's disease
British Journal of Pharmacology 166: 1097
Ryabtsova O, Jansen K, Van Goethem S, Joossens J, Cheng JD, Lambeir AM, De Meester I, Augustyns K, Van der Veken P (2012)
Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity
Bioorganic & Medicinal Chemistry Lett 22: 3412
Van der Veken P, Fulop V, Rea D, Gerard M, Van Elzen R, Joossens J, Cheng JD, Baekelandt V, De Meester I, Lambeir AM, Augustyns K (2012)
P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy
Journal of Medicinal Chemistry 55: 9856
Matheeussen V, Baerts L, De Meyer G, De Keulenaer G, Van der Veken P, Augustyns K, Dubois V, Scharpe S, De Meester I (2011)
Expression and spatial heterogeneity of dipeptidyl peptidases in endothelial cells of conduct vessels and capillaries
Biol Chem 392: 189
Van Goethem S, Matheeussen V, Joossens J, Lambeir AM, Chen X, De Meester I, Haemers A, Augustyns K, Van der Veken P (2011)
Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?
Journal of Medicinal Chemistry 54: 5737
Dubois V, Van Ginneken C, De Cock H, Lambeir AM, Van der Veken P, Augustyns K, Chen X, Scharpe S, De Meester I (2009)
Enzyme activity and immunohistochemical localization of dipeptidyl peptidase 8 and 9 in male reproductive tissues
Journal of Histochemistry & Cytochemistry 57: 531
Dubois V, Lambeir AM, Van der Veken P, Augustyns K, Creemers J, Chen X, Scharpe S, De Meester I (2008)
Purification and characterization of dipeptidyl peptidase IV-like enzymes from bovine testes
Front Biosci 13: 3558
Van Goethem S, Van der Veken P, Dubois V, Soroka A, Lambeir AM, Chen X, Haemers A, Scharpe S, De Meester I, Augustyns K (2008)
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors
Bioorganic & Medicinal Chemistry Lett 18: 4159
Van der Veken P, De Meester I, Dubois V, Soroka A, Van Goethem S, Maes MB, Brandt I, Lambeir AM, Chen X, Haemers A, Scharpe S, Augustyns K (2008)
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads
Bioorganic & Medicinal Chemistry Lett 18: 4154
Maes MB, Dubois V, Brandt I, Lambeir AM, Van der Veken P, Augustyns K, Cheng JD, Chen X, Scharpe S, De Meester I (2007)
Dipeptidyl peptidase 8/9-like activity in human leukocytes
J Leukoc Biol 81: 1252
Van der Veken P, Soroka A, Brandt I, Chen YS, Maes MB, Lambeir AM, Chen X, Haemers A, Scharpe S, Augustyns K, De Meester I (2007)
Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates
Journal of Medicinal Chemistry 50: 5568
Van der Veken P, Haemers A, Augustyns K (2007)
Prolyl peptidases related to dipeptidyl peptidase IV: potential of specific inhibitors in drug discovery
Curr Top Med Chem 7: 621
Maes MB, Martinet W, Schrijvers DM, Van der Veken P, De Meyer GR, Augustyns K, Lambeir AM, Scharpe S, De Meester I (2006)
Dipeptidyl peptidase II and leukocyte cell death
Biochemical Pharmacology 72: 70
Maes MB, Lambeir AM, Van der Veken P, De Winter B, Augustyns K, Scharpe S, De Meester I (2006)
In vivo effects of a potent, selective DPPII inhibitor: UAMC00039 is a possible tool for the elucidation of the physiological function of DPPII
Advances in Experimental Medicine & Biology 575: 73
Soroka A, Van der Veken P, De Meester I, Lambeir AM, Maes MB, Scharpe S, Haemers A, Augustyns K (2006)
Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines
Bioorganic & Medicinal Chemistry Lett 16: 4777
Augustyns K, Van der Veken P, Senten K, Haemers A (2005)
The therapeutic potential of inhibitors of dipeptidyl peptidase IV (DPP IV) and related proline-specific dipeptidyl aminopeptidases
Curr Med Chem 12: 971
Maes MB, Lambeir AM, Gilany K, Senten K, Van der Veken P, Leiting B, Augustyns K, Scharpe S, De Meester I (2005)
Kinetic investigation of human dipeptidyl peptidase II (DPPII)-mediated hydrolysis of dipeptide derivatives and its identification as quiescent cell proline dipeptidase (QPP)/dipeptidyl peptidase 7 (DPP7)
Biochemical Journal 386: 315
Van der Veken P, Senten K, Kertesz I, De Meester I, Lambeir AM, Maes MB, Scharpe S, Haemers A, Augustyns K (2005)
Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases
Journal of Medicinal Chemistry 48: 1768
Senten K, Van der Veken P, De Meester I, Lambeir AM, Scharpe S, Haemers A, Augustyns K (2004)
Gamma-amino-substituted analogues of 1-[(S)-2,4-diaminobutanoyl]piperidine as highly potent and selective dipeptidyl peptidase II inhibitors
Journal of Medicinal Chemistry 47: 2906
Bal G, Van der Veken P, Antonov D, Lambeir AM, Grellier P, Croft SL, Augustyns K, Haemers A (2003)
Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity
Bioorganic & Medicinal Chemistry Lett 13: 2875
Senten K, Daniels L, Van der Veken P, De Meester I, Lambeir AM, Scharpe S, Haemers A, Augustyns K (2003)
Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases
J Comb Chem 5: 336
Senten K, Van der Veken P, De Meester I, Lambeir AM, Scharpe S, Haemers A, Augustyns K (2003)
Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases
Journal of Medicinal Chemistry 46: 5005