Laboratoire de Toxicologie

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Laboratoire de Toxicologie
Quelques publications représentatives pour la période 1986 – 2004.
Kiss R, Paridaens R, Heuson JC, Danguy A. Effect of progesterone on cell proliferation in the MXT mouse
hormone sensitive mammary neoplasm. J Natl Cancer Inst 77:173-178, 1986.
Kiss R, de Launoit Y, L'Hermite-Balériaux M, L'Hermite M, Paridaens R, Danguy A, Pasteels JL. Effect of
prolactin and estradiol administrations on cell proliferation in the uterus and the MXT mouse mammary
neoplasm. J Natl Cancer Inst 78:993-998, 1987.
Kiss R, de Launoit Y, Danguy A, Paridaens R, Pasteels JL. Influence of pituitary grafts or prolactin
administrations on the hormone sensitivity of "ovarian-independent" mouse mammary MXT tumors. Cancer
Res 49:2945-2951, 1989.
Camby I, Salmon I, Danguy A, Pasteels JL, Brotchi J, Martinez J, Kiss R. Influence of gastrin on human
astrocytic tumor cell proliferation. J Natl Cancer Inst 88:594-600, 1996.
Lesueur-Ginot L, Demarquay D, Kiss R, Kasprzyck PG, Dassonneville L, Bailly C, Camara J, Lavergne O,
Bigg DCH. Homocamptothecin, an E-ring modified camptothecin with enhanced lactone stability, retains
topoisomerase I-targeted activity and antitumor properties. Cancer Res 59:2939-2943, 1999.
Philippart P, Harper L, Chaboteaux C, Decaestecker C, Bronckart Y, Gordower L, Lesueur-Ginot L,
Malonne H, Lavergne O, Bigg DCH, Mendes Da Costa P, Kiss R. Homocampothecin, an E-Ring-modified
camptothecin, exerts more potent antiproliferative activity than other topoisomerase I inhibitors in human
colon cancers obtained from surgery and maintained in vitro under histotypical culture conditions. Clin
Cancer Res 6:1557-1562, 2000.
Malonne H, Farinelle S, Decaestecker C, Gordower L, Fontaine J, Chaminade F, Saucier JM, Atassi G,
Kiss R. In vitro and in vivo pharmacological characterizations of the antitumor properties of two new
olivacine derivatives, S16020-2 and S30972-1. Clin Cancer Res 6:3774-3782, 2000.
Camby I, Belot N, Rorive S, Lefranc F, Maurage CA, Lahm H, Kaltner H, Hadari Y, Ruchoux MM, Brotchi J,
Zick Y, Salmon I, Gabius HJ, Kiss R. Galectins are differentially expressed in supratentorial pilocytic
astrocytomas, astrocytomas, anaplastic astrocytomas and glioblastomas, and significantly modulate tumor
astrocyte migration. Brain Pathol 11:12-26, 2001.
Lefranc F, Mijatovic T, Mathieu V, Rorive S, Decaestecker C, Debeir O, Brotchi J, Van Ham P, Salmon I,
Kiss R. Characterization of gastrin-induced proangiogenic effects in vivo in orthotopic U373 experimental
human glioblastomas and in vitro in human umbilical vein endothelial cells. Clin Cancer Res 10:8250-8265,
2004.
Platek A, Mettlen M, Camby I, Kiss R, Amyere M, Courtoy PJ. v-Src accelerates spontaneous motility via
phosphoinositide 3-kinase, phospholipase C and phospholipase D, but abrogates chemotaxis in Rat-1 and
MDCK cells. J Cell Sci 117:4849-4861, 2004.
Liste des publications scientifiques depuis 2005.
Lefranc F, Brotchi J, Kiss R. Possible future issues in the treatment of glioblastomas, with a special
emphasis on cell migration and the resistance of migrating glioblastoma cells to apoptosis. J Clin Oncol
23:2411-2422, 2005.
Lefranc F, Mijatovic T, Decaestecker C, Kaltner H, Andre S, Brotchi J, Salmon I, Gabius HJ, Kiss R.
Monitoring the expression profiles of integrins and adhesion / growth regulatory galectins in
adamantinomatous craniopharyngiomas: their ability to regulate tumor adhesiveness to surrounding tissue
and their contribution to prognosis. Neurosurgery 56 :763-776, 2005.
Lefranc F, James S, Camby I, Gaussin JF, Darro F, Brotchi J, Gabius HJ, Kiss R. Combined cimetidine and
temozolomide, compared with temozolomide alone: significant increases in survival in nude mice bearing
U373 human glioblastoma multiforme orthotopic xenograft. J Neurosurg 102:706-714, 2005.

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Camby I, Decaestecker C, Lefranc F, Kaltner H, Gabius HJ, Kiss R. Galectin-1 knocking down in human
U87 glioblastoma cells alters their gene expression pattern. Biochem Biophys Res Commun 335:27-35,
2005.
Darro F, Decaestecker C, Gaussin JF, Mortier S, Van Ginckel R, Kiss R. Are syngeneoic mouse tumor
models still valuable experimental models in the field of anti-cancer drug discovery ? Int J Oncol 27:607-
616, 2005.
Mathieu V, Mijatovic T, Van Damme M, Kiss R. Gastrin exerts pleitropic effects on human melanoma cell
biology. Neoplasia 7:930-943, 2005.
Saussez S, Nonclercq D, Laurent G, Wattiez R, André S, Kaltner H, Gabius HJ, Kiss R, Toubeau G.
Toward functional glycomics by localization of tissue lectins: immunohistochemical galectin fingerprinting
during diethylstilbestrol-induced kidney tumorigenesis in male Syrian hamster. Histochem Cell Biol 123:29-
41, 2005.
Remmelink M, Mijatovic T, Gustin A, Mathieu A, Rombaut K, Kiss R, Salmon I, Decaestecker C.
Identification by means of cDNA microarray analyses of gene expression modifications in squamous non-
small cell lung cancers as compared to normal bronchial epithelial tissue. Int J Oncol 26:247-258, 2005.
Van Quaquebeke E, Simon G, Andre A, Dewelle J, Yazidi ME, Bruyneel F, Tuti J, Nacoulma O, Guissou P,
Decaestecker C, Braekman JC, Kiss R, Darro F. Identification of a novel cardenolide (2’’-oxovorusharin)
from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor
activities and high in vivo tolerance: Structure-activity relationship analyses. J Med Chem 48:849-856, 2005.
Debeir O, Van Ham Ph, Kiss R, Decaestecker C. Tracking of migrating cells under phase-contrast video
microscopy with combined mean-shift processes. IEEE Trans Med Imaging 24:697-711, 2005.
Mathieu A, Saal I, Vukovic A, Ransy V, Vereerstraten P, Kaltner H, Gabius HJ, Kiss R, Decaestecker C,
Salmon I, Remmelink M. Nuclear galectin-3 expression is an independent predictive factor of recurrence for
adenocarcinoma and squamous cell carcinoma of the lung. Mod Pathol 18:1264-1271, 2005.
Lefranc F, Decaestecker R, Brotchi J, Heizmann CW, DeWitte O, Kiss R, Mijatovic T. Co-expression/co-
location of S100 proteins (S100B, S100A1 and S100A2) and protein kinase C (PKC-β, -η and –ζ) in a rat
model of cerebral basilar artery vasospasm. Neuropathol Appl Neurobiol 31:649-660, 2005.
Saal I, Nagy N, Lensch M, Lohr M, Manning JC, Decaestecker C, Andre S, Kiss R, Salmon I, Gabius HJ.
Human galectin-2: expression profiling by RT-PCR/immunohistochemistry and its introduction as a
histochemical tool for ligand localization. Histol Histopathol 20:1191-1208, 2005.
Saussez S, Kiss R. Galectin-7 (Review). Cell Mol Life Sci 63:686-697, 2006.
Mijatovic T, Op De Beeck A, Van Quaquebeke E, Dewelle J, Darro F, de Launoit Y, Kiss R. The cardenolide
UNBS1450 is able to deactivate NF-kappaB-mediated cytoprotective effects in human non-small-cell-lung
cancer (NSCLC) cells. Mol Cancer Ther 5:1-9, 2006.
Lefranc F, Yeaton P, Brotchi J, Kiss R. Cimetidine, an unexpected anti-tumor agent, and its potential for the
treatment of glioblastoma (Review). Int J Oncol 28:1021-1030, 2006.
Ingrassia L, Nshimyumukiza P, Dewelle J, Lefranc F, Wlodarczak L, Thomas S, Dielie G, Chiron C, Zedde
C, Tisnès P, van Soest R, Braeckman JC, Darro F, Kiss R. A lactosylated steroid contributes in vivo
therapeutic benefits in experimental models of mouse lymphoma and human glioblastoma. J Med Chem
49:1800-1807, 2006.
Saussez S, Raluca Cucu D, Decaestecker C, Chevalier D, Kaltner H, André S, Wacreniez A, Toubeau G,
Camby I, Gabius HJ, Kiss R. Galectin-7 (p53-induced gene-1): A new prognostic predictor of recurrence
and survival in stage IV hypopharyngeal cancer. Ann Surg Oncol 13:999-1009, 2006.
Mijatovic T, Mathieu V, Gaussin JF, De Neve N, Ribaucour F, Van Quaquebeke E, Dumont P, Darro F, Kiss
R. Cardenolide-induced lysosomal membrane permeabilization contributes therapeutic benefits in
experimental human non-small-cell-lung cancers. Neoplasia 8:402-412, 2006.

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Lefranc F, Kiss R. Autophagy, the Trojan horse to combat glioblastomas. Neurosurg Focus 20:e7, 2006.
Lefranc F, Sadeghi N, Camby I, Metens T, Dewitte O, Kiss R. Present and potential futur issues in
glioblastoma treatment. Expert Rev Anticancer Ther 6:719-732, 2006.
Camby I, Le Mercier M, Lefranc F, Kiss R. Galectin-1: A small protein with major functions. Glycobiology
16:137R-157R, 2006.
Ingrassia L, Camby I, Lefranc F, Mathieu V, Nshimyumukiza P, Darro F, Kiss R. Anti-galectin compounds
as potential anti-cancer drugs. Curr Med Chem 13:3513-3527, 2006.
Saussez S, Lorfevre F, Nonclercq D, Laurent G, André S, Journé F, Kiss R, Toubeau G, Gabius HJ.
Towards functional glycomics by localization of binding sites for tissue lectins : lectin histochemical reactivity
for galectins during diethylstilbestrol-induced kidney tumorigenesis in male Syrian hamster. Histochem Cell
Biol 25:1-13, 2006.
Hayot C, Debeir O, Van Ham P, Van Damme M, Kiss R, Decaestecker C. Characterization of the activities
of actin-affecting drugs on tumor cell migration. Toxicol Appl Pharmacol 211:30-40, 2006.
Servotte S, Camby I, Debeir O, Deroanne C, Lambert CA, Lapière CM, Kiss R, Nusgens B, Decaestecker
C. The in vitro influences of neurotensin on the motility characteristics of human U373 glioblastoma cells.
Neuropathol Appl Neurobiol 32:575-584, 2006.
Dubois F, Yourassowsky C, Monnom O, Legros JC, Debeir O, Van Ham P, Kiss R, Decaestecker C. Digital
holographic microscopy for the three-dimensional dynamic analysis of in vitro cancer cell migration. J
Biomedical Optics 11:054032, 2007.
Saussez S, Camby I, Toubeau G, Kiss R. Galectins as modulators of tumor progression in head and neck
squamous cell carcinomas (HNSCCs). Head & Neck 29:874-884, 2007.
Decaestecker C, Debeir O, Van Ham P, Kiss R. Can anti-migratory drugs be screened in vitro? A review of
2D and 3D assays for the quantitative analysis of cell migration (Review). Med Res Rev 27:149-176, 2007.
Saussez S, Decaestecker C, Lorfevre F, Cucu DR, Mortuaire G, Chevalier D, Wacreniez A, Kaltner H,
André S, Toubeau G, Camby I, Gabius HJ, Kiss R. High level of galectin-1 is a negative prognostic predictor
of recurrence in laryngeal squamous cell carcinomas. Int J Oncol 30:1109-1117, 2007.
Salmoun M, Braekman JC, Ranarivelo Y, Rasamoelisendra R, Ralambomanana D, Dewelle J, Darro F,
Kiss R. New calamene sesquiterpenes from Tarena madagascarensis. Nat Prod Res 21:111-120, 2007.
Mijatovic T, Roland I, Van Quaquebeke E, Nilsson B, Mathieu A, Van Vynckt F, Darro F, Blanco G, Facchini
V, Kiss R. The alpha-1 subunit of the sodium pump could represent a novel target to combat non-small cell
lung cancers. J Pathol 212:170-179, 2007.
Mijatovic T, Van Quaquebeke E, Delest B, Debeir O, Darro F, Kiss R. Cardiotonic steroids on the road to
anti-cancer therapy. BBA Rev Cancer 1776:32-57, 2007.
Van Quaquebeke E, Mahieu T, Dumont P, Dewelle J, Ribaucour F, Simon G, Sauvage S, Gaussin JF, Tuti
J, El Yazidi M, Van Vynckt F, Mijatovic T, Lefranc F, Darro F, Kiss R. 2,2,2-Trichloro-N-({2-[2-
(dimethylamino)ethyl]-1,3-dihydro-1H-benzo[de]isoquinolin-5yl}carbamoyl)acetamide (UNBS3157), a novel
non-hematotoxic naphthalimide derivative with potent anti-tumor activity. J Med Chem 50:4122-4134, 2007.
Mathieu V, Le Mercier M, De Neve N, Sauvage S, Gras T, Roland I, Lefranc F, Kiss R. Galectin-1
knockdown increases sensitvity to temozolomide in a B16F10 mouse metastatic melanoma model. J Invest
Dermatol 127:2399-2410, 2007.
Dumont P, Ingrassia L, Rouzeau S, Ribaucour F, Thomas S, Roland I, Darro F, Lefranc F, Kiss R. The
Amaryllidaceae isocarbostyril narciclasine induces apoptosis by activation of the Death Receptor and/or the
mitochondrial pathways in cancer cells but not in normal fibroblasts. Neoplasia 9:766-776, 2007.
Mijatovic T, Lefranc F, Van Quaquebeke E, Van Vynckt F, Darro F, Kiss R. UNBS1450: A new hemi-
synthetic cardenolide with promising anti-cancer activity. Drug Dev Res 68:1-10, 2007.

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Lefranc F, Facchini V, Kiss R. Pro-autophagic drugs: A novel means to combat apoptosis-resistant cancers,
with a special emphasis on glioblastomas. The Oncologist 12:1395-1403, 2007.
Salmoun M, Braekman JC, Dewelle J, Darro F, Kiss R, De Voogd NJ, Van Soest RW. New terpenoids from
two Indonesian marine sponges. Nat Prod Res 21:149-155, 2007.
Pilette C, Colinet B, Kiss R, Andre S, Kaltner H, Gabius HJ, Delos M, Vaerman JP, Decramer M, Sibille Y.
Increased galectin-3 expression and intraepithelial neutrophils in small airways in severe chronic obstructive
pulmonary disease. Eur Respir J 29 :914-922, 2007.
Mégalizzi V, Mathieu V, Mijatovic T, Gailly P, Debeir O, De Neve N, Van Damme M, Bontempi G, Haibe-
Kains B, Decaestecker C, Kondo Y, Kiss R, Lefranc F. 4-IBP : A sigma-1 receptor agonist decreases the
migration of human cancer cells including glioblastoma cells in vitro and sensitizes them in vitro and in vivo
to the cytotoxic insults of pro-apoptotic and pro-autophagic drugs. Neoplasia 9:358-369, 2007.
Hoog PD, Boldron C, Gamez P, Sliedregt-Bol K, Roland I, Pitie M, Kiss R, Meunier B, Reedijk J. New
approach for the preparation of efficient DNA cleaving agents: Ditopic copper-platinum complexes based on
3-clip-phen and cisplatin. J Med Chem 50:3148-3152, 2007.
Mijatovic T, Gailly P, Mathieu V, De Neve N, Yeaton P, Kiss R, Decaestecker C. Neurotensin is a versatile
modulator of in vitro human pancreatic ductal adenocarcinomas cell (PDAC) migration. Cell Oncol 29:315-
326, 2007.
Saussez S, Lorfevre F, Lequeux T, Laurent G, Chantrain G, Vertongen F, Toubeau G, Decaestecker C,
Kiss R. The determination of the levels of circulating galectin-1 and –3 in HNSCC patients could be used to
monitor tumor progression and/or responses to therapy. Oral Oncol 44:86-93, 2008.
Lefranc F, Mijatovic T, Kondo Y, Sauvage S, Roland I, Krstic D, Vasic V, Gailly P, Kondo S, Blanco G, Kiss
R. Targeting the alpha-1 subunit of the sodium pump (the Na
+
/K
+
-ATPase) to combat glioblastoma cells.
Neurosurgery 62:211-222, 2008.
Lefranc F, Mijatovic T, Kiss R. La pompe à sodium pourrait représenter une nouvelle cible pour le
traitement du glioblastome. Bul Cancer 95 :271-281, 2008.
Lefranc F, Kiss R. The sodium pump alpha-1 subunit as a potential target to combat apoptosis-resistant
glioblastomas. Neoplasia 10:198-206, 2008.
Ingrassia L, Lefranc F, Mathieu V, Darro F, Kiss R. Amaryllidaceae isocarbostyril alkaloids and their
derivatives as promising anti-tumor agents. Translational Oncology 1:1-13, 2008.
Mijatovic T, Mahieu T, Bruyère C, De Neve N, Dewelle J, Simon G, Dehoux M, Van Der Aar E, Haibe-Kains
B, Bontempi G, Decaestecker C, Van Quaquebeke E, Darro F, Kiss R. UNBS5162, a novel naphthalimide
that decreases CXCL chemokine expression in experimental prostate cancers. Neoplasia 10:573-586,
2008.
Mijatovic T, De Neve N, Gailly P, Mathieu V, Haibe-Kains B, Bontempi G, Lapeira J, Decaestecker C,
Facchini V, Kiss R. The nucleolus and cMyc: potential targets of cardenolide-mediated anti-tumor activity.
Mol Cancer Ther 7:1285-1296, 2008.
Lefranc F, Ingrassia L, Kiss R. Targeting autophagy: do patents reveal a therapeutic potential? Expert Opin
Ther Patents 18:1-7, 2008.
Mijatovic T, Ingrassia L, Facchini V, Kiss R. Na
+
/K
+
-ATPase alpha subunits as new targets in anti-cancer
therapy. Expert Opin Ther Targets 12:1403-1417, 2008.
Camby I, Le Mercier M, Mathieu V, Ingrassia L, Lefranc F, Kiss R. Galectin-1 as potential therapeutic target
for cancer progression. Drugs of the Future 33:1057-1069, 2008.
Gnoula C, Mégalizzi V, De Neve N, Sauvage S, Ribaucour F, Guissou P, Duez P, Dubois J, Ingrassia L,
Lefranc F, Kiss R, Mijatovic T. Balanitin-6 and –7: Diosgenyl saponins isolated from Balanites aegyptiaca
Del. Display significant anti-tumor activity in vitro and in vivo. Int J Oncol 32 :5-15, 2008.

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Le Mercier M, Lefranc F, Mijatovic T, Debeir O, Haibe-Kains B, Bontempi G, Decaestecker C, Kiss R,
Mathieu V. Evidence of galectin-1 involvement in glioma chemoresistance. Toxicol Appl Pharmacol
229:172-183, 2008.
Ozalp-Yaman S, de Hoog P, Amadei G, Pitié M, Gamez P, Dewelle J, Mijatovic T, Meunier B, Kiss R,
Reedijk J. Platinated copper(3-clip-phen) complexes as effective DNA-cleaving and cytotoxic agents.
Chemistry - Eur J 14:3418-3426, 2008.
de Hoog P, Pitié M, Amadei G, Gamez P, Meunier B, Kiss R, Reedijk J. DNA cleavage and binding
selectivity of a heterodinuclear Pt-Cu(3-clip-phen) complex. J Biol Inorg Chem 13:575-586, 2008.
Le Mercier M, Mathieu V, Haibe-Kains B, Bontempi G, Mijatovic T, Decaestecker C, Kiss R, Lefranc F.
Knocking down galectin-1 in human Hs683 glioblastoma cells impairs both angiogenesis through ORP150
depletion and endoplasmic reticulum stress responses. J Neuropathol Exp Neurol 67:456-469, 2008.
Debeir O, Mégalizzi V, Warzée N, Kiss R, Decaestecker C. Videomicroscopic extraction of specific
information on cell proliferation and migration in vitro. Exp Cell Res 314:2985-2998, 2008.
Mathieu V, De Neve N, Le Mercier M, Dewelle J, Gaussin JF, Dehoux M, Kiss R, Lefranc F. Combining
Bevacizumab with temozolomide increases the anti-tumor efficacy of temozolomide in human glioblastoma
orthotopic xenograft model. Neoplasia 10:1383-1392, 2008.
Delaine T, Cumpstey I, Ingrassia L, Le Mercier M, Okechukwu P, Leffler H, Kiss R, Nilsson UJ. Galectin-
inhibitory thiodigalactoside ester derivatives have anti-migratory effects in cultured lung and prostate cancer
cells. J Med Chem 51:8109-8114, 2008.
Ingrassia L, Lefranc F, Dewelle J, Pottier L, Mathieu V, Spiegl-Kreinecker S, Sauvage S, El Yazidi M,
Dehoux M, Berger W, Van Quaquebeke E, Kiss R. Structure-activity-relationship analysis of novel
derivatives of narciclasine (an Amaryllidaceae Isocarbostyril alkaloid) as potential anti-cancer agents. J Med
Chem 52:1100-1114, 2009.
Lefranc F, Rynkowski M, De Witte O, Kiss R. Present and potential future adjuvant issues in high-grade
astrocytic glioma treatment. Adv Tech Stand Neurosurg 34:3-35, 2009.
Le Mercier M, Fortin S, Mathieu V, Roland I, Spiegl-Kreinecker S, Haibe-Kains B, Bontempi G,
Decaestecker C, Berger W, Lefranc F, Kiss R. Galectin-1 proangiogenic and promigratory effects in the
Hs683 oligodendroglioma model are partly mediated through the control of BEX2 expression. Neoplasia
11:485-496, 2009.
Azéma J, Guidetti B, Dewelle J, Le Calvé B, Mijatovic T, Korolyov A, Vaysse J, Malet-Martino M, Martino R,
Kiss R. 7-((4-Substituted)piperazin-1-yl) derivatives of ciprofloxacin : Synthesis and in vitro biological
evaluation as potential antitumor agents. Bioorg Med Chem 17:5396-5407, 2009.
Lefranc F, Sauvage S, Van Goietsenoven G, Mégalizzi V, Lamoral-Theys D, Debeir O, Spiegl-Kreinecker S,
Berger W, Mathieu V, Decaestecker C, Kiss R. Narciclasine, a plant growth modulator, activates Rho and
stress fibers in glioblastoma cells. Mol Cancer Ther 8:1739-1750, 2009.
Mégalizzi V, Decaestecker C, Debeir O, Spiegl-Kreinecker S, Berger W, Lefranc F, Kast RE, Kiss R.
Sigma-1 receptors as potential targets to impair both cell proliferation and cell migration in human
glioblastomas. Eur J Cancer 45:2893-2905, 2009.
Frédérich M, Marcowycz A, Cieckiewicz E, Mégalizzi V, Angenot L, Kiss R. In vitro anticancer potential of
tree extracts from the Walloon Region Forrest. Planta Med 75:1634-1637, 2009.
Mathieu V, Pirker C, Martin de Lassalle E, Vernier M, Mijatovic T, DeNeve N, Gaussin JF, Dehoux M,
Lefranc F, Berger W, Kiss R. The sodium pump alpha-1 subunit: a disease progression-related target for
metastatic melanoma treatment. J Cell Mol Med 13 (9B):3960-3972, 2009.
Sivasankaran B, Degen M, Ghaffari A, Hegi ME, Hamou MF, Ionescu MCS, Zweifel C, Tolnay M, Wasner
M, Mergenthaler S, Miserez AR, Kiss R, Lino MM, Merlo A, Chiquet-Ehrismann, Boulay JL. Tenascin-C is a
novel RBPJk-induced target gene for Notch signaling in gliomas. Cancer Res 69:458-465, 2009.