S Liekens

Summary

Affiliation: Katholieke Universiteit Leuven
Country: Belgium

Publications

  1. ncbi request reprint The nucleotide analog cidofovir suppresses basic fibroblast growth factor (FGF2) expression and signaling and induces apoptosis in FGF2-overexpressing endothelial cells
    Sandra Liekens
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Leuven, Belgium
    Mol Pharmacol 71:695-703. 2007
  2. doi request reprint The thymidine phosphorylase inhibitor 5'-O-tritylinosine (KIN59) is an antiangiogenic multitarget fibroblast growth factor-2 antagonist
    Sandra Liekens
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Mol Cancer Ther 11:817-29. 2012
  3. ncbi request reprint Thymidine phosphorylase is noncompetitively inhibited by 5'-O-trityl-inosine (KIN59) and related compounds
    S Liekens
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Nucleosides Nucleotides Nucleic Acids 25:975-80. 2006
  4. ncbi request reprint Targeting platelet-derived endothelial cell growth factor/thymidine phosphorylase for cancer therapy
    Sandra Liekens
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem Pharmacol 74:1555-67. 2007
  5. ncbi request reprint CXCL12-CXCR4 axis in angiogenesis, metastasis and stem cell mobilization
    S Liekens
    Rega Institute for Medical Research, Department of Microbiology and Immunology, K U Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium
    Curr Pharm Des 16:3903-20. 2010
  6. ncbi request reprint 5'-O-tritylated nucleoside derivatives: inhibition of thymidine phosphorylase and angiogenesis
    Sandra Liekens
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Mol Pharmacol 70:501-9. 2006
  7. ncbi request reprint A novel animal model for hemangiomas: inhibition of hemangioma development by the angiogenesis inhibitor TNP-470
    S Liekens
    Rega Institute for Medical Research, University Hospitals, Leuven, Belgium
    Cancer Res 59:2376-83. 1999
  8. ncbi request reprint Inhibition of fibroblast growth factor-2-induced vascular tumor formation by the acyclic nucleoside phosphonate cidofovir
    S Liekens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Cancer Res 61:5057-64. 2001
  9. ncbi request reprint Potent inhibition of hemangioma formation in rats by the acyclic nucleoside phosphonate analogue cidofovir
    S Liekens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Cancer Res 58:2562-7. 1998
  10. ncbi request reprint Potent inhibition of hemangiosarcoma development in mice by cidofovir
    S Liekens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroederstraat 10, B 3000 Leuven, Belgium
    Int J Cancer 92:161-7. 2001

Collaborators

Detail Information

Publications37

  1. ncbi request reprint The nucleotide analog cidofovir suppresses basic fibroblast growth factor (FGF2) expression and signaling and induces apoptosis in FGF2-overexpressing endothelial cells
    Sandra Liekens
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Leuven, Belgium
    Mol Pharmacol 71:695-703. 2007
    ..These findings suggest that the clinical use of cidofovir might be expanded to tumors that are not induced by oncogenic viruses...
  2. doi request reprint The thymidine phosphorylase inhibitor 5'-O-tritylinosine (KIN59) is an antiangiogenic multitarget fibroblast growth factor-2 antagonist
    Sandra Liekens
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Mol Cancer Ther 11:817-29. 2012
    ....
  3. ncbi request reprint Thymidine phosphorylase is noncompetitively inhibited by 5'-O-trityl-inosine (KIN59) and related compounds
    S Liekens
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Nucleosides Nucleotides Nucleic Acids 25:975-80. 2006
    ..Our observations indicate that allosteric sites in TPase may regulate its biological activity...
  4. ncbi request reprint Targeting platelet-derived endothelial cell growth factor/thymidine phosphorylase for cancer therapy
    Sandra Liekens
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem Pharmacol 74:1555-67. 2007
    ..This review will focus on the different biological activities of PD-ECGF/TP and their implications for cancer progression and treatment...
  5. ncbi request reprint CXCL12-CXCR4 axis in angiogenesis, metastasis and stem cell mobilization
    S Liekens
    Rega Institute for Medical Research, Department of Microbiology and Immunology, K U Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium
    Curr Pharm Des 16:3903-20. 2010
    ..Here, we discuss the different aspects of CXCL12/CXCR4 biology as well as the development and anti-cancer/stem cell mobilizing activity of CXCR4 antagonists...
  6. ncbi request reprint 5'-O-tritylated nucleoside derivatives: inhibition of thymidine phosphorylase and angiogenesis
    Sandra Liekens
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Mol Pharmacol 70:501-9. 2006
    ..Thus, 5'-O-trityl nucleoside derivatives combine antiangiogenic and vascular-targeting activities, which opens perspectives for their potential use as anticancer agents...
  7. ncbi request reprint A novel animal model for hemangiomas: inhibition of hemangioma development by the angiogenesis inhibitor TNP-470
    S Liekens
    Rega Institute for Medical Research, University Hospitals, Leuven, Belgium
    Cancer Res 59:2376-83. 1999
    ..i. The model described here may be useful for investigating (a) the angiogenic mechanism(s) underlying hemangioma progression; and (b) the effect of anti-angiogenic compounds on vascular tumor growth...
  8. ncbi request reprint Inhibition of fibroblast growth factor-2-induced vascular tumor formation by the acyclic nucleoside phosphonate cidofovir
    S Liekens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Cancer Res 61:5057-64. 2001
    ..In conclusion, cidofovir appears to inhibit the growth of endothelium-derived tumors via induction of apoptosis without exerting a direct antiangiogenic activity...
  9. ncbi request reprint Potent inhibition of hemangioma formation in rats by the acyclic nucleoside phosphonate analogue cidofovir
    S Liekens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Cancer Res 58:2562-7. 1998
    ..Cidofovir may thus be further explored for the treatment of vascular tumors and, in particular, life-threatening juvenile hemangiomas...
  10. ncbi request reprint Potent inhibition of hemangiosarcoma development in mice by cidofovir
    S Liekens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroederstraat 10, B 3000 Leuven, Belgium
    Int J Cancer 92:161-7. 2001
    ..Cidofovir should be further explored for its potential in the treatment of fast-growing vascular tumors, like hemangiomas and hemangiosarcomas...
  11. ncbi request reprint The sulfonic acid polymers PAMPS [poly(2-acrylamido-2-methyl-1-propanesulfonic acid)] and related analogues are highly potent inhibitors of angiogenesis
    S Liekens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Oncol Res 9:173-81. 1997
    ..These results suggest that sulfonic acid polymers, and in particular PAMPS, may be considered as specific, nontoxic angiogenesis inhibitors...
  12. ncbi request reprint The A167Y mutation converts the herpes simplex virus type 1 thymidine kinase into a guanosine analogue kinase
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochemistry 41:6517-24. 2002
    ..Therefore, the single A167Y mutation converts the wild-type HSV-1 TK from a predominantly pyrimidine nucleos(t)ide kinase into a virtually exclusive purine (guanine) nucleoside analogue kinase...
  13. doi request reprint Identification of aspartic acid-203 in human thymidine phosphorylase as an important residue for both catalysis and non-competitive inhibition by the small molecule "crystallization chaperone" 5'-O-tritylinosine (KIN59)
    A Bronckaers
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem Pharmacol 78:231-40. 2009
    ..Our findings reveal the existence of a previously unrecognized site in TP that can be targeted by small molecules to inhibit the catalytic activity of TP...
  14. ncbi request reprint The nucleoside derivative 5'-O-trityl-inosine (KIN59) suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action
    Sandra Liekens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    J Biol Chem 279:29598-605. 2004
    ..Identification of these site(s) is important to obtain a better insight into the molecular role of TPase in the progression of cancer and angiogenic diseases...
  15. ncbi request reprint Angiogenesis: regulators and clinical applications
    S Liekens
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000, Leuven, Belgium
    Biochem Pharmacol 61:253-70. 2001
    ....
  16. ncbi request reprint Modulation of fibroblast growth factor-2 receptor binding, signaling, and mitogenic activity by heparin-mimicking polysulfonated compounds
    S Liekens
    Rega Institute for Medical Research, University Hospital, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 56:204-13. 1999
    ..In conclusion, sulfonic acid polymers bind FGF-2 by mimicking heparin interaction. These compounds may provide a tool to inhibit FGF-2-induced endothelial cell proliferation in angiogenesis and tumor growth...
  17. ncbi request reprint The role of growth factors, angiogenic enzymes and apoptosis in neovascularization and tumor growth-collected publications
    S Liekens
    Laboratory of Virology and Experimental Chemotherapy, Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven
    Verh K Acad Geneeskd Belg 64:197-224. 2002
    ..Our findings open new perspectives for the use of cidofovir as an anti-tumor agent in the therapy of hemangiomas and other tumors that are not associated with an oncogenic virus...
  18. ncbi request reprint Effect of TNP-470 (AGM-1470) on the growth of rat rhabdomyosarcoma tumors of different sizes
    W Landuyt
    University Hospital, K U Leuven, Belgium
    Cancer Invest 19:35-40. 2001
    ..The antivasculature therapy might also improve hypoxia/necrosis-related therapeutic approaches...
  19. doi request reprint Human mitochondrial thymidine kinase is selectively inhibited by 3'-thiourea derivatives of beta-thymidine: identification of residues crucial for both inhibition and catalytic activity
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 75:1127-36. 2009
    ....
  20. pmc Pradimicin S, a highly soluble nonpeptidic small-size carbohydrate-binding antibiotic, is an anti-HIV drug lead for both microbicidal and systemic use
    Jan Balzarini
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antimicrob Agents Chemother 54:1425-35. 2010
    ..It proved stable at high temperature and low pH. Therefore, PRM-S may qualify as a potential anti-HIV drug candidate for further (pre)clinical studies, including its microbicidal use...
  21. ncbi request reprint Stromal cell-derived factor 1 (CXCL12) binds to endothelial cells and signals through a receptor different from CXCR4
    Sigrid Hatse
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Biochem Biophys Res Commun 348:192-9. 2006
    ..Together, our data point to the existence of an additional receptor through which CXCL12 exerts its biological effects in endothelial cells...
  22. ncbi request reprint Engineering of a single conserved amino acid residue of herpes simplex virus type 1 thymidine kinase allows a predominant shift from pyrimidine to purine nucleoside phosphorylation
    Jan Balzarini
    Rega Institute for Medical Research, K U Leuven, B 3000 Leuven, Belgium
    J Biol Chem 281:19273-9. 2006
    ....
  23. ncbi request reprint Anti-angiogenic activity of a novel multi-substrate analogue inhibitor of thymidine phosphorylase
    Sandra Liekens
    Rega Institute for Medical Research, Minderbroedersstraat 10, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    FEBS Lett 510:83-8. 2002
    ....
  24. ncbi request reprint Fluorescent CXCL12AF647 as a novel probe for nonradioactive CXCL12/CXCR4 cellular interaction studies
    Sigrid Hatse
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Cytometry A 61:178-88. 2004
    ..Therefore, potent and specific CXCR4 antagonists may have therapeutic potential as anti-HIV, anti-cancer, and anti-inflammatory drugs...
  25. pmc Zebrafish bioassay-guided natural product discovery: isolation of angiogenesis inhibitors from East African medicinal plants
    Alexander D Crawford
    Department of Pharmaceutical Sciences, University of Leuven, Leuven, Belgium
    PLoS ONE 6:e14694. 2011
    ..These results suggest that the combination of zebrafish bioassays with analytical chromatography methods is an effective strategy for the rapid identification of bioactive natural products...
  26. ncbi request reprint Lack of susceptibility of bicyclic nucleoside analogs, highly potent inhibitors of varicella-zoster virus, to the catabolic action of thymidine phosphorylase and dihydropyrimidine dehydrogenase
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 61:1140-5. 2002
    ....
  27. doi request reprint The cytostatic activity of pyrimidine nucleosides is strongly modulated by Mycoplasma hyorhinis infection: Implications for cancer therapy
    Annelies Bronckaers
    Rega Institute for Medical Research, K U Leuven, B 3000 Leuven, Belgium
    Biochem Pharmacol 76:188-97. 2008
    ..Given the association of M. hyorhinis with several human cancers, our findings suggest that pyrimidine nucleoside-based but not 5FU-based anti-cancer therapy might be more effective when combined with a mycoplasmal TP inhibitor...
  28. doi request reprint The dual role of thymidine phosphorylase in cancer development and chemotherapy
    Annelies Bronckaers
    Rega Institute for Medical Research, KULeuven, Leuven, Belgium
    Med Res Rev 29:903-53. 2009
    ..This duality illustrates the complexity of the role of TP in tumor progression and in the clinical response to fluoropyrimidine-based chemotherapy...
  29. doi request reprint 2-aminothiophene-3-carboxylic acid ester derivatives as novel highly selective cytostatic agents
    J Balzarini
    Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, 3000, Leuven, Belgium
    Invest New Drugs 32:200-10. 2014
    ..Compound 3 was also shown to induce apoptosis in prostate cancer cells. The 2-aminothiophene-3-carboxylic acid ester derivatives represent novel candidate cytostatic agents to be further explored for their tumor-selective potential. ..
  30. ncbi request reprint Amino-terminal truncation of CXCR3 agonists impairs receptor signaling and lymphocyte chemotaxis, while preserving antiangiogenic properties
    P Proost
    Laboratory of Molecular Immunology, Rega Institute for Medical Research, Leuven, Belgium
    Blood 98:3554-61. 2001
    ..These data demonstrate a negative feedback regulation by CD26/DPP IV in CXCR3-mediated chemotaxis without affecting the angiostatic potential of the CXCR3 ligands IP-10 and Mig...
  31. doi request reprint The COOH-terminal peptide of platelet factor-4 variant (CXCL4L1/PF-4var47-70) strongly inhibits angiogenesis and suppresses B16 melanoma growth in vivo
    Jo Vandercappellen
    Laboratory of Molecular Immunology, Rega Institute for Medical Research, University of Leuven, Leuven, Belgium
    Mol Cancer Res 8:322-34. 2010
    ..In conclusion, CXCL4L1/PF-4var(47-70) is a potent antitumoral and antiangiogenic peptide. These results may represent the basis for the design of CXCL4L1/PF-4var COOH-terminal-derived peptidomimetic anticancer drugs...
  32. doi request reprint Improvement of purine and pyrimidine antimetabolite-based anticancer treatment by selective suppression of mycoplasma-encoded catabolic enzymes
    Sandra Liekens
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    Lancet Oncol 10:628-35. 2009
    ..We also suggest potential methods for improving future chemotherapy by suppressing mycoplasma-mediated catabolism of the anticancer nucleoside analogues...
  33. ncbi request reprint Thymidine phosphorylase inhibitors: recent developments and potential therapeutic applications
    María Jesús Pérez-Pérez
    Instituto de Quimica Medica CSIC, Juan de la Cierva 3, E 28006 Madrid, Spain
    Mini Rev Med Chem 5:1113-23. 2005
    ..Here we have summarized the most recent approaches in the search for novel TPase inhibitors together with the potential therapeutic applications of such inhibitors...
  34. ncbi request reprint Mutations distal to the substrate site can affect varicella zoster virus thymidine kinase activity: implications for drug design
    Kamel El Omari
    Division of Structural Biology, The Wellcome Trust Centre for Human Genetics, University of Oxford, Roosevelt Drive, Oxford, OX3 7BN, UK
    Mol Pharmacol 69:1891-6. 2006
    ..The work described here shows that distal mutations that affect the VZVTK active-site may help in the design of more selective substrates for gene suicide therapy or as anti-varicella zoster virus drugs...
  35. pmc Heparin-mimicking sulfonic acid polymers as multitarget inhibitors of human immunodeficiency virus type 1 Tat and gp120 proteins
    Antonella Bugatti
    General Pathology and Immunology, Department of Biomedical Sciences and Biotechnology, School of Medicine, University of Brescia, Brescia, Italy
    Antimicrob Agents Chemother 51:2337-45. 2007
    ..As these activities contribute to both AIDS progression and associated pathologies, SSAPs can be considered prototypic molecules for the development of multitarget drugs for the treatment of HIV infection and AIDS-associated pathologies...
  36. pmc Structural basis for non-competitive product inhibition in human thymidine phosphorylase: implications for drug design
    Kamel El Omari
    Division of Structural Biology, The Wellcome Trust Centre for Human Genetics, University of Oxford, Oxford OX3 7BN, UK
    Biochem J 399:199-204. 2006
    ..The present study will assist in the design of HTP inhibitors that could lead to drugs for anti-angiogenesis as well as for the potentiation of other nucleoside drugs...
  37. ncbi request reprint 5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase
    Elena Casanova
    Instituto de Química Médica C S I C, Juan de la Cierva 3, E 28006 Madrid, Spain
    J Med Chem 49:5562-70. 2006
    ..The here reported results further substantiate that 5'-O-trityl nucleosides represent a new class of TPase inhibitors that should be further explored in those biological systems where TPase plays an instrumental role (i.e. angiogenesis)...