Research Topics
| S LiekensSummaryAffiliation: Katholieke Universiteit Leuven Country: Belgium Publications
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Publications
The nucleotide analog cidofovir suppresses basic fibroblast growth factor (FGF2) expression and signaling and induces apoptosis in FGF2-overexpressing endothelial cellsSandra 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...
The thymidine phosphorylase inhibitor 5'-O-tritylinosine (KIN59) is an antiangiogenic multitarget fibroblast growth factor-2 antagonistSandra Liekens
Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
Mol Cancer Ther 11:817-29. 2012....- Thymidine phosphorylase is noncompetitively inhibited by 5'-O-trityl-inosine (KIN59) and related compoundsS 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... - 5'-O-tritylated nucleoside derivatives: inhibition of thymidine phosphorylase and angiogenesisSandra 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... - Targeting platelet-derived endothelial cell growth factor/thymidine phosphorylase for cancer therapySandra 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... - CXCL12-CXCR4 axis in angiogenesis, metastasis and stem cell mobilizationS 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... - A novel animal model for hemangiomas: inhibition of hemangioma development by the angiogenesis inhibitor TNP-470S 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... - Inhibition of fibroblast growth factor-2-induced vascular tumor formation by the acyclic nucleoside phosphonate cidofovirS 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... - Potent inhibition of hemangioma formation in rats by the acyclic nucleoside phosphonate analogue cidofovirS 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... - Potent inhibition of hemangiosarcoma development in mice by cidofovirS 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... - The sulfonic acid polymers PAMPS [poly(2-acrylamido-2-methyl-1-propanesulfonic acid)] and related analogues are highly potent inhibitors of angiogenesisS 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... - The A167Y mutation converts the herpes simplex virus type 1 thymidine kinase into a guanosine analogue kinaseJan 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... - 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... - The nucleoside derivative 5'-O-trityl-inosine (KIN59) suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of actionSandra 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... - Angiogenesis: regulators and clinical applicationsS Liekens
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000, Leuven, Belgium
Biochem Pharmacol 61:253-70. 2001.... - Modulation of fibroblast growth factor-2 receptor binding, signaling, and mitogenic activity by heparin-mimicking polysulfonated compoundsS 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... - The role of growth factors, angiogenic enzymes and apoptosis in neovascularization and tumor growth-collected publicationsS 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... - Effect of TNP-470 (AGM-1470) on the growth of rat rhabdomyosarcoma tumors of different sizesW Landuyt
University Hospital, K U Leuven, Belgium
Cancer Invest 19:35-40. 2001..The antivasculature therapy might also improve hypoxia/necrosis-related therapeutic approaches... - Anti-angiogenic activity of a novel multi-substrate analogue inhibitor of thymidine phosphorylaseSandra Liekens
Rega Institute for Medical Research, Minderbroedersstraat 10, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium
FEBS Lett 510:83-8. 2002.... - Fluorescent CXCL12AF647 as a novel probe for nonradioactive CXCL12/CXCR4 cellular interaction studiesSigrid 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... 
Pradimicin S, a highly soluble nonpeptidic small-size carbohydrate-binding antibiotic, is an anti-HIV drug lead for both microbicidal and systemic useJan 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...- Human mitochondrial thymidine kinase is selectively inhibited by 3'-thiourea derivatives of beta-thymidine: identification of residues crucial for both inhibition and catalytic activityJan Balzarini
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
Mol Pharmacol 75:1127-36. 2009.... - 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 phosphorylationJan Balzarini
Rega Institute for Medical Research, K U Leuven, B 3000 Leuven, Belgium
J Biol Chem 281:19273-9. 2006.... - Stromal cell-derived factor 1 (CXCL12) binds to endothelial cells and signals through a receptor different from CXCR4Sigrid 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... - Zebrafish bioassay-guided natural product discovery: isolation of angiogenesis inhibitors from East African medicinal plantsAlexander 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... - Lack of susceptibility of bicyclic nucleoside analogs, highly potent inhibitors of varicella-zoster virus, to the catabolic action of thymidine phosphorylase and dihydropyrimidine dehydrogenaseJan Balzarini
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
Mol Pharmacol 61:1140-5. 2002.... - The cytostatic activity of pyrimidine nucleosides is strongly modulated by Mycoplasma hyorhinis infection: Implications for cancer therapyAnnelies 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... - The dual role of thymidine phosphorylase in cancer development and chemotherapyAnnelies 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... - Amino-terminal truncation of CXCR3 agonists impairs receptor signaling and lymphocyte chemotaxis, while preserving antiangiogenic propertiesP 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... - The COOH-terminal peptide of platelet factor-4 variant (CXCL4L1/PF-4var47-70) strongly inhibits angiogenesis and suppresses B16 melanoma growth in vivoJo 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... - Improvement of purine and pyrimidine antimetabolite-based anticancer treatment by selective suppression of mycoplasma-encoded catabolic enzymesSandra 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... - Thymidine phosphorylase inhibitors: recent developments and potential therapeutic applicationsMaría 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... - 5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylaseElena Casanova
, 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)... - Mutations distal to the substrate site can affect varicella zoster virus thymidine kinase activity: implications for drug designKamel 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... - Structural basis for non-competitive product inhibition in human thymidine phosphorylase: implications for drug designKamel 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... - Heparin-mimicking sulfonic acid polymers as multitarget inhibitors of human immunodeficiency virus type 1 Tat and gp120 proteinsAntonella 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...