A M Lambeir

Summary

Affiliation: University of Antwerp
Country: Belgium

Publications

  1. ncbi request reprint Kinetic investigation of chemokine truncation by CD26/dipeptidyl peptidase IV reveals a striking selectivity within the chemokine family
    A M Lambeir
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1 S6, B 2610 Antwerp, Belgium
    J Biol Chem 276:29839-45. 2001
  2. pmc 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)
    Marie Berthe Maes
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein1, B 2610 Antwerp, Belgium
    Biochem J 386:315-24. 2005
  3. doi request reprint Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors
    Sebastiaan Van Goethem
    Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    Bioorg Med Chem Lett 18:4159-62. 2008
  4. doi request reprint The potential of carboxypeptidase M as a therapeutic target in cancer
    Catherine J Denis
    University of Antwerp, Pharmaceutical Sciences, Laboratory of Medical Biochemistry, Universiteitsplein 1, Antwerp, B 2610, Belgium
    Expert Opin Ther Targets 17:265-79. 2013
  5. ncbi request reprint A kinetic study of glucagon-like peptide-1 and glucagon-like peptide-2 truncation by dipeptidyl peptidase IV, in vitro
    Anne Marie Lambeir
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1 S6, B 2610 Wilrijk, Belgium
    Biochem Pharmacol 64:1753-6. 2002
  6. ncbi request reprint Dipeptidyl-peptidase IV from bench to bedside: an update on structural properties, functions, and clinical aspects of the enzyme DPP IV
    Anne Marie Lambeir
    Department of Pharmaceutical Sciences, Laboratory of Medical Biochemistry, University of Antwerp, Universiteitsplein 1, Wilrijk, Belgium
    Crit Rev Clin Lab Sci 40:209-94. 2003
  7. ncbi request reprint Translational research on prolyl oligopeptidase inhibitors: the long road ahead
    Anne Marie Lambeir
    University of Antwerp, Campus Drie Eiken, Laboratory of Medical Biochemistry, Universiteitsplein 1 blg S room S 515, B 2610 Wilrijk, Belgium 32 3 2652549 32 3 2652685
    Expert Opin Ther Pat 21:977-81. 2011
  8. doi request reprint DPP4 inhibitors for diabetes--what next?
    Anne Marie Lambeir
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Antwerp, Belgium
    Biochem Pharmacol 76:1637-43. 2008
  9. ncbi request reprint Interaction of prolyl oligopeptidase with α-synuclein
    Anne Marie Lambeir
    Laboratory of Medical Biochemistry, University of Antwerp Campus Drie Eiken, Wilrijk, Belgium
    CNS Neurol Disord Drug Targets 10:349-54. 2011
  10. ncbi request reprint Kinetic study of the processing by dipeptidyl-peptidase IV/CD26 of neuropeptides involved in pancreatic insulin secretion
    A M Lambeir
    Laboratory of Medical Biochemistry, University of Antwerp, Belgium
    FEBS Lett 507:327-30. 2001

Collaborators

  • Marc Vanderheyden
  • J E Nielsen
  • Pieter Van der Veken
  • Xin Chen
  • I De Meester
  • K Augustyns
  • Veronique Dubois
  • P Proost
  • J Backmann
  • R K Wierenga
  • T Sasaki
  • N Oyama
  • K Heremans
  • W Martinet
  • Jonathan D Cheng
  • J Balzarini
  • P Kursula
  • P Neubauer
  • Barbara Leiting
  • Simon L Croft
  • Simon Scharpe
  • Inger Brandt
  • Marie Berthe Maes
  • Achiel Haemers
  • Kristel Senten
  • Jurgen Joossens
  • Kathleen Deiteren
  • Anna Soroka
  • Gunther Bal
  • Georgiana Surpateanu
  • Ibrahim El-Sayed
  • Catherine J Denis
  • S Sercu
  • Leah Marquez-Curtis
  • Sebastiaan Van Goethem
  • Carlos García-Aparicio
  • Omar M Ali
  • Bart Devreese
  • Marco G Casteleijn
  • Kambiz Gilany
  • J Joossens
  • Katie Amssoms
  • Jan Depreitere
  • E Steenackers
  • A El Ghalbzouri
  • J Merregaert
  • K Geentjens
  • Neeta Shirvaikar
  • Veerle Baekelandt
  • Melanie Gerard
  • Yves Engelborghs
  • Kjell Sergeant
  • Ali Jalili
  • Anna Janowska-Wieczorek
  • John A Foekens
  • Sonsoles Velazquez
  • Dirk F Hendriks
  • Wolfgang Schmalix
  • Anneliese Schneider
  • Buddy Setyono-Han
  • Yves Laroche
  • Maria Jose Camarasa
  • Johan L Willemse
  • Alberto Diez-Torrubia
  • Guido R Y De Meyer
  • Katrin Groebel
  • Benedicte De Winter
  • Jean Marie Ketelslegers
  • Dorien M Schrijvers
  • Markus Alahuhta
  • Walter Van Dongen
  • Jozef Van Beeumen
  • Kris De Vriendt
  • A Haemers
  • Dimitri Antonov
  • Philippe Grellier
  • Liesbeth Daniels
  • Werner De Potter
  • Brigitte Bauvois
  • Zesheng Wang
  • Sandra L Oza
  • Abdellah Yamani
  • Edmond Coen
  • Etienne J Nouwen
  • Alan H Fairlamb
  • Christine Durinx

Detail Information

Publications46

  1. ncbi request reprint Kinetic investigation of chemokine truncation by CD26/dipeptidyl peptidase IV reveals a striking selectivity within the chemokine family
    A M Lambeir
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1 S6, B 2610 Antwerp, Belgium
    J Biol Chem 276:29839-45. 2001
    ..The data not only provide insight into the selectivity of the enzyme for specific chemokines, but they also contribute to the general understanding of CD26/dipeptidyl peptidase IV secondary substrate specificity...
  2. pmc 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)
    Marie Berthe Maes
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein1, B 2610 Antwerp, Belgium
    Biochem J 386:315-24. 2005
    ..1x10(6) s(-1) x M(-1)) and Ala-Pro-pNA (kcat/K(m) 2.6x10(6) s(-1) x M(-1)) were found to be the most sensitive chromogenic substrates for human DPPII, but were less selective than Lys-Ala-pNA (kcat/K(m) 0.4x10(6) s(-1) x M(-1))...
  3. doi request reprint Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors
    Sebastiaan Van Goethem
    Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    Bioorg Med Chem Lett 18:4159-62. 2008
    ..Within this series compound 8j was shown to be a potent and selective inhibitor of DPP8/9 with low activity toward DPP II...
  4. doi request reprint The potential of carboxypeptidase M as a therapeutic target in cancer
    Catherine J Denis
    University of Antwerp, Pharmaceutical Sciences, Laboratory of Medical Biochemistry, Universiteitsplein 1, Antwerp, B 2610, Belgium
    Expert Opin Ther Targets 17:265-79. 2013
    ..CPM modulates receptor signaling of kinins, anaphylatoxins, and chemokines. These CPM substrates affect proliferation, angiogenesis, and apoptosis of cancer cells. What is the evidence that CPM is a drug target for cancer therapy?..
  5. ncbi request reprint A kinetic study of glucagon-like peptide-1 and glucagon-like peptide-2 truncation by dipeptidyl peptidase IV, in vitro
    Anne Marie Lambeir
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1 S6, B 2610 Wilrijk, Belgium
    Biochem Pharmacol 64:1753-6. 2002
    ..The selectivity of DPP IV for the glucagon-like peptides was compared with data obtained for other natural substrates using the same enzyme source in identical conditions...
  6. ncbi request reprint Dipeptidyl-peptidase IV from bench to bedside: an update on structural properties, functions, and clinical aspects of the enzyme DPP IV
    Anne Marie Lambeir
    Department of Pharmaceutical Sciences, Laboratory of Medical Biochemistry, University of Antwerp, Universiteitsplein 1, Wilrijk, Belgium
    Crit Rev Clin Lab Sci 40:209-94. 2003
    ..This enables DPP IV/CD26 to serve as a co-stimulatory molecule to influence T cell activity and to modulate chemotaxis. DPP IV is also implicated in HIV-1 entry, malignant transformation, and tumor invasion...
  7. ncbi request reprint Translational research on prolyl oligopeptidase inhibitors: the long road ahead
    Anne Marie Lambeir
    University of Antwerp, Campus Drie Eiken, Laboratory of Medical Biochemistry, Universiteitsplein 1 blg S room S 515, B 2610 Wilrijk, Belgium 32 3 2652549 32 3 2652685
    Expert Opin Ther Pat 21:977-81. 2011
    ..Yet, with the current insights, it is difficult to correlate specific inhibitor effects with the postulated functions of prolyl oligopeptidase in the brain...
  8. doi request reprint DPP4 inhibitors for diabetes--what next?
    Anne Marie Lambeir
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Antwerp, Belgium
    Biochem Pharmacol 76:1637-43. 2008
    ..In turn, these studies increased the insights in the role of DPP4 in the body's response to various insults...
  9. ncbi request reprint Interaction of prolyl oligopeptidase with α-synuclein
    Anne Marie Lambeir
    Laboratory of Medical Biochemistry, University of Antwerp Campus Drie Eiken, Wilrijk, Belgium
    CNS Neurol Disord Drug Targets 10:349-54. 2011
    ..Whether PO also contributes to the normal physiological functions of α-syncline remains an open question, but there are some intriguing parallels between the proposed functions of both proteins that deserve further investigation...
  10. ncbi request reprint Kinetic study of the processing by dipeptidyl-peptidase IV/CD26 of neuropeptides involved in pancreatic insulin secretion
    A M Lambeir
    Laboratory of Medical Biochemistry, University of Antwerp, Belgium
    FEBS Lett 507:327-30. 2001
    ..Therefore, residues remote from the scissile bond can modulate DPPIV/CD26 substrate selectivity as well as residues flanking it...
  11. ncbi request reprint Dipeptide-derived diphenyl phosphonate esters: mechanism-based inhibitors of dipeptidyl peptidase IV
    A M Lambeir
    Department of Pharmaceutical Sciences, University of Antwerp U I A, Wilrijk, Belgium
    Biochim Biophys Acta 1290:76-82. 1996
    ..Due to their stability and the irreversible nature of the inhibition, the diphenyl phosphonate esters promise to be useful tools in the continuing investigation of the physiological function of dipeptidyl peptidase IV...
  12. ncbi request reprint The unique properties of dipeptidyl-peptidase IV (DPP IV / CD26) and the therapeutic potential of DPP IV inhibitors
    K Augustyns
    Department of Pharmaceutical Chemistry, University of Antwerp UIA, Universiteitsplein 1, Antwerpen, B 2610, Belgium
    Curr Med Chem 6:311-27. 1999
    ..Finally the therapeutical perspectives for DPP IV inhibitors will be discussed...
  13. ncbi request reprint In vivo inhibition of dipeptidyl peptidase IV activity by pro-pro-diphenyl-phosphonate (Prodipine)
    I De Meester
    Laboratory of Medical Biochemistry, University of Antwerp, Wilrijk, Belgium
    Biochem Pharmacol 54:173-9. 1997
    ....
  14. ncbi request reprint Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases
    Kristel Senten
    Department of Medicinal Chemistry and Department of Medical Biochemistry, University of Antwerp UIA, Universiteitsplein 1, B 2610 Antwerp, Belgium
    J Med Chem 46:5005-14. 2003
    ..Dab-Pip and Dab-Pip-2-CN were selected as the most promising inhibitors (IC(50) nM range) and will enable us to study the physiological role of DPP II and to differentiate between DPP II and DPP IV in biological systems...
  15. ncbi request reprint Dipeptidyl peptidase 8/9-like activity in human leukocytes
    Marie Berthe Maes
    Laboratory of Medical Biochemistry, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk, Belgium
    J Leukoc Biol 81:1252-7. 2007
    ....
  16. ncbi request reprint Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases
    Pieter Van der Veken
    Department of Medicinal Chemistry and Medical Biochemistry, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    J Med Chem 48:1768-80. 2005
    ..Most of these compounds exhibited a strong binding preference toward DPP II with IC(50) values in the low micromolar range, while only low DPP IV inhibitory potential is seen...
  17. ncbi request reprint The role of the S1 binding site of carboxypeptidase M in substrate specificity and turn-over
    Kathleen Deiteren
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    Biochim Biophys Acta 1774:267-77. 2007
    ..Extending the substrate up to P7 had little effect on the catalytic parameters. The substrates were modelled in the active site of CPM. The results indicate that P1-S1 interactions play a role in substrate binding and turn-over...
  18. ncbi request reprint Development of potent and selective dipeptidyl peptidase II inhibitors
    Kristel Senten
    Department of Medicinal Chemistry, University of Antwerp UIA, Universiteitsplein 1, Antwerpen, Belgium
    Bioorg Med Chem Lett 12:2825-8. 2002
    ..Dab-Pip has an IC(50)=0.13 microM for DPP II and a 7600-fold selectivity with respect to DPP IV. This compound will be highly valuable for the investigation of the biochemical function of DPP II...
  19. doi request reprint Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads
    Pieter Van der Veken
    Department of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    Bioorg Med Chem Lett 18:4154-8. 2008
    ..These compounds were shown to be nanomolar DPP8/9 inhibitors with modest overall selectivity toward DPP IV and DPP II...
  20. ncbi request reprint Inhibition of dipeptidyl-peptidase IV catalyzed peptide truncation by Vildagliptin ((2S)-{[(3-hydroxyadamantan-1-yl)amino]acetyl}-pyrrolidine-2-carbonitrile)
    Inger Brandt
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Drie Eiken Campus, Universiteitsplein 1 building S6 B 2610 Antwerpen Wilrijk, Belgium
    Biochem Pharmacol 70:134-43. 2005
    ..4.11.9) or aminopeptidase M (EC 3.4.11.2). There was no evidence for substrate specific inhibition of DPP IV by Vildagliptin or for important allosteric factors affecting the inhibition constant in presence of GIP and GLP-1...
  21. ncbi request reprint Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates
    Pieter Van der Veken
    Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    J Med Chem 50:5568-70. 2007
    ..Within this latter series, compound 2e was shown to be a potent, irreversible inhibitor of DPP8, demonstrating very low affinity for DPP IV and DPP II...
  22. ncbi request reprint A prediction of DPP IV/CD26 domain structure from a physico-chemical investigation of dipeptidyl peptidase IV (CD26) from human seminal plasma
    A M Lambeir
    Department of Pharmaceutical Sciences, University of Antwerp U I A, Wilrijk, Belgium
    Biochim Biophys Acta 1340:215-26. 1997
    ..Our results provide compelling experimental evidence for the three-domain structure of the extracellular part of DPP IV...
  23. ncbi request reprint Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases
    Kristel Senten
    Department of Medicinal Chemistry and Department of Medical Biochemistry, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    J Comb Chem 5:336-44. 2003
    ..35), that will be useful to discriminate between DPP II and DPP IV in biological systems in order to further elucidate the biological function of DPP II...
  24. ncbi request reprint Dipeptidyl-peptidase IV converts intact B-type natriuretic peptide into its des-SerPro form
    Inger Brandt
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Antwerp, Belgium
    Clin Chem 52:82-7. 2006
    ..4.14.5) and (b) whether this truncation affects the susceptibility to cleavage by neutral endopeptidase (NEP; EC 3.4.24.11)...
  25. ncbi request reprint Dipeptidyl peptidase IV substrates. An update on in vitro peptide hydrolysis by human DPPIV
    Ingrid De Meester
    Department of Pharmaceutical Sciences University of Antwerp, Universiteitsplein 1, Antwerp, Belgium
    Adv Exp Med Biol 524:3-17. 2003
  26. ncbi request reprint Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator
    J Joossens
    Department of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B 2610, Antwerp, Belgium
    J Med Chem 47:2411-3. 2004
    ..A k(app) value in the 10(3) M(-1) s(-1) range for uPA was obtained, together with a selectivity index higher than 240 toward other trypsin-like proteases such as tPA, thrombin, plasmin, and FXa...
  27. ncbi request reprint Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position
    Jurgen Joossens
    Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, BE 2610 Antwerp, Belgium
    J Med Chem 49:5785-93. 2006
    ..It is shown that uPA is irreversibly inhibited, and interactions with the active site were modeled. Finally, a diparacetamol phosphonate analogue was developed to circumvent the release of cytotoxic phenol...
  28. ncbi request reprint Exploration of the active site of dipeptidyl peptidase IV from Porphyromonas gingivalis. Comparison with the human enzyme
    Anne Marie Lambeir
    Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, Wilrijk, Belgium
    Adv Exp Med Biol 524:29-35. 2003
  29. ncbi request reprint In vivo effects of a potent, selective DPPII inhibitor: UAMC00039 is a possible tool for the elucidation of the physiological function of DPPII
    Marie Berthe Maes
    Laboratory for Medical Biochemistry, Department of Pharmaceutical Sciences 3Division of Gastroenterology, Faculty of Medicine, University of Antwerp, Universiteitsplein 1, B 2610 Wilrijk, Belgium
    Adv Exp Med Biol 575:73-85. 2006
  30. ncbi request reprint Peptide substrates of dipeptidyl peptidases
    Inger Brandt
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    Adv Exp Med Biol 575:3-18. 2006
  31. ncbi request reprint Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines
    Anna Soroka
    Laboratory of Medicinal Chemistry University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    Bioorg Med Chem Lett 16:4777-9. 2006
    ..The (4S)-methyl compound showed subnanomolar inhibition, comparable with the parent compound. The (4R)-methyl group or bigger substituents decreased the activity...
  32. ncbi request reprint Gamma-amino-substituted analogues of 1-[(S)-2,4-diaminobutanoyl]piperidine as highly potent and selective dipeptidyl peptidase II inhibitors
    Kristel Senten
    Department of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    J Med Chem 47:2906-16. 2004
    ..Piperidine-2-nitriles did not show an increase in potency but rather reduced the selectivity. Introduction of a 4-methyl or a 3-fluorine on piperidine improved selectivity and preserved the high potency...
  33. ncbi request reprint The ionization of a buried glutamic acid is thermodynamically linked to the stability of Leishmania mexicana triose phosphate isomerase
    A M Lambeir
    Laboratory for Medical Biochemistry, University of Antwerp UIA, Wilrijk, Belgium
    Eur J Biochem 267:2516-24. 2000
    ..No intermediates could be identified in the unfolding equilibrium by combining fluorescence and CD measurements. Study of a stable monomeric triose phosphate isomerase variant confirmed that the phenomenon persists in the monomer...
  34. doi request reprint ECM1 interacts with fibulin-3 and the beta 3 chain of laminin 332 through its serum albumin subdomain-like 2 domain
    S Sercu
    Laboratory of Molecular Biotechnology, Department of Biomedical Sciences, University of Antwerp, Wilrijk, Belgium
    Matrix Biol 28:160-9. 2009
    ..Hence, disruption of the ECM1 function may cause the failure of multi-communication among the surrounding skin interstitial molecules, as seen in lipoid proteinosis pathology...
  35. ncbi request reprint Purification and characterization of dipeptidyl peptidase IV-like enzymes from bovine testes
    Veronique Dubois
    Laboratory of Medical Biochemistry, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk, Belgium
    Front Biosci 13:3558-68. 2008
    ..We can conclude that the natural DPP9-like enzyme and the DPP enriched peak 3 are closely related to the recombinant forms of human DPP9 and DPP8...
  36. ncbi request reprint Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties
    Jurgen Joossens
    Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    J Med Chem 50:6638-46. 2007
    ..We report in this paper a preclinical proof of concept that selective, irreversible uPA inhibitors could be valuable in antimetastatic therapy...
  37. ncbi request reprint Presence and release of SR-17 (chromogranin B(586-602)) in the porcine splenic nerve and its enzymatic degradation by CD26/dipeptidyl peptidase IV
    Jan Depreitere
    Laboratory of Neurobiology and Neuropharmacology, University of Antwerp, UIA, Universiteitsplein 1, B 2610 Wilrijk, Antwerp, Belgium
    Regul Pept 106:71-9. 2002
    ..In addition, we show that the new CgB-peptide can serve as a substrate for the lymphocyte surface glycoprotein CD26, also known as dipeptidyl peptidase IV (DPP IV), generating a new peptide ER-15 (CgB(588-602))...
  38. ncbi request reprint Search for substrates for prolyl oligopeptidase in porcine brain
    Inger Brandt
    Laboratory of Medical Biochemistry, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk, Belgium
    Peptides 26:2536-46. 2005
    ..Using MSMS peptide sequencing techniques, we identified several fragments of intracellular proteins as potential substrates, which opens new perspectives for finding the function of PO in the intracellular space...
  39. ncbi request reprint Dipeptidyl peptidase II and leukocyte cell death
    Marie Berthe Maes
    Laboratory of Medical Biochemistry, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk, Belgium
    Biochem Pharmacol 72:70-9. 2006
    ..These data are of importance for a more precise interpretation of the in vitro and in vivo effects of other dipeptidyl peptidase inhibitors...
  40. doi request reprint Prolyl oligopeptidase stimulates the aggregation of alpha-synuclein
    Inger Brandt
    Laboratory for Medical Biochemistry, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk, Belgium
    Peptides 29:1472-8. 2008
    ..If PO displays this activity also in vivo, PO inhibitors might have an effect on neurodegenerative disorders through a decrease in the aggregation of alpha-synuclein...
  41. ncbi request reprint Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity
    Gunther Bal
    Department of Medicinal Chemistry, University of Antwerp, Belgium
    Bioorg Med Chem Lett 13:2875-8. 2003
    ..These compounds are potent inhibitors of human and trypanosomal prolyloligopeptidase. They were shown to inhibit Trypanosoma cruzi and Trypanosoma b. brucei in in vitro systems with ED(50)'s in the lower microM range...
  42. ncbi request reprint The catalytic cycle of biosynthetic thiolase: a conformational journey of an acetyl group through four binding modes and two oxyanion holes
    Petri Kursula
    Department of Biochemistry and Biocenter Oulu, P O Box 3000, FIN 90014 University of Oulu, Oulu, Finland
    Biochemistry 41:15543-56. 2002
    ..The reactivity of the active site may be modulated by hydrogen bonding networks extending from the active site toward the back of the molecule...
  43. doi request reprint Carboxypeptidase M expressed by human bone marrow cells cleaves the C-terminal lysine of stromal cell-derived factor-1alpha: another player in hematopoietic stem/progenitor cell mobilization?
    Leah Marquez-Curtis
    Research and Development, Canadian Blood Services, Edmonton, Alberta, Canada
    Stem Cells 26:1211-20. 2008
    ..We suggest that cleavage of the C-terminal lysine residue of SDF-1alpha by CPM leads to attenuated chemotactic responses and could facilitate G-CSF-induced mobilization of HSPC from BM to peripheral blood...
  44. ncbi request reprint Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 2: substitution of the glycine part
    Katie Amssoms
    Department of Medicinal Chemistry, University of Antwerp UIA, Belgium
    Bioorg Med Chem Lett 12:2703-5. 2002
    ..Compounds with basic side chains such as diaminopropionic acid were found to be good inhibitors (K(i): 7.2 microM). Substitution of the glycine part abolished the GspS substrate properties of the tripeptide...
  45. ncbi request reprint Efficient conversion of tetrapeptide-based TSAO prodrugs to the parent drug by dipeptidyl-peptidase IV (DPPIV/CD26)
    Carlos García-Aparicio
    Instituto de Química Médica C S I C, Juan de la Cierva 3, E 28006 Madrid, Spain
    Antiviral Res 76:130-9. 2007
    ..The antiviral activity of the prototype NAP-TSAO could also be modulated by introducing different tetrapeptide moieties on the molecule resulting, in some cases, in a superior antiviral potential in cell culture than the parent drug...
  46. ncbi request reprint Functional role of the conserved active site proline of triosephosphate isomerase
    Marco G Casteleijn
    Department of Process and Environmental Engineering and Bioprocess Engineering Laboratory, University of Oulu, P O Box 3000, FIN 90014 Oulu, Finland
    Biochemistry 45:15483-94. 2006
    ..Apparently, the rotation of 90 degrees of the Gly211-Gly212 peptide plane of loop 7 plays a key role in this concerted movement...