Publications (Articles and Posters)
List of Posters
Articles
Articles published in 2008 (authors from ProQinase are emphasized)
Alajati A, Laib AM, Weber H, Boos AM, Bartol A, Ikenberg K, Korff T, Zentgraf H, Obodozie C, Graeser R, Christian S, Finkenzeller G, Stark GB, Héroult M, Augustin H (2008): Spheroid-based engineering of a human vasculature in mice.
Nature Methods 5, 439-445
Aly AH, Edrada-Ebel R, Indriani ID, Wray V, Mueller WE, Totzke F, Zirrgiebel U, Schaechtele C, Kubbutat MH, Lin WH, Proksch P, Ebel R (2008): Cytotoxic Metabolites from the Fungal Endophyte Alternaria sp. and Their Subsequent Detection in Its Host Plant Polygonum senegalense.
Journal of Natural Products 71, 972-980
Bornmann C, Graeser R, Esser N, Ziroli V, Jantscheff P, Keck T, Unger C, Hopt UT, Adam U, Schaechtele C, Massing U, von Dobschuetz E (2008): A new liposomal formulation of Gemcitabine is active in an orthotopic mouse model of pancreatic cancer accessible to bioluminescence imaging.
Cancer Chemother Pharmacol. 61, 395-405
Fichtner I, Claffey J, Gleeson B, Hogan M, Wallis D, Weber H, Tacke M (2008): Antitumor Activity of Oxali-Titanocene Y in Xenografted Caki-1 Tumors in Mice.
Letters in Drug Design & Discovery 5, 489-493
Graeser R, Chung DE, Esser N, Moor S, Schaechtele C, Unger C, Kratz F (2008): Synthesis and biological evaluation of an albumin-binding prodrug of doxorubicin that is cleaved by prostate-specific antigen (PSA) in a PSA-positive orthotopic prostate carcinoma model (LNCaP).
Int J Cancer 122, 1145-54
Kloepper J, Lindenmaier W, Fiedler U, Mehlhorn A, Stark GB, Finkenzeller G (2008): High efficient adenoviral-mediated VEGF and Ang-1 gene delivery into osteogenically differentiated human mesenchymal stem cells.
Microvasc Res. 75, 83-90
Oehmig A, Klotzbuecher A, Thomas M, Weise F, Hagner U, Brundiers R, Waldherr D, Lingnau A, Knappik A, Kubbutat MHG, Joos T, Volkmer H (2008): A novel reverse transduction adenoviral array for the functional analysis of shRNA libraries.
BMC Genomics 9, 44l
Peifer C, Selig R, Kinkel K, Ott D, Totzke F, Schaechtele C, Heidenreich R, Roecken M, Schollmeyer D, Laufer S (2008): Design, Synthesis and Biological Evaluation of Novel 3-Aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as Vascular Endothelial Growth Factor Recceptor (VEGF-R) Inhibitors.
J. Med. Chem 51, 3814-24
Pieh C, Agostini H, Buschbeck C, Krueger M, Schulte-Moenting J, Zirrgiebel U, Drevs J, Lagrèze WA (2008): VEGF-A, VEGFR-1, VEGFR-2 and Tie2 levels in plasma of premature infants: Relationship to retinopathy of prematurity.
British Journal of Ophthalmology 92, 689-693
Puttini M, Redaelli S, Moretti, L, Gunby R, Mologni L, Marchisi E, Cleris L, Donella-Deana A, Drueckes P, Sala E, Lucchini V, Kubbutat MHG, Formelli F, Zambon A, Scapozza L, Gambarcorti-Passerini C (2008): Characterisation of CMP-584, an Abl-inhibitor with lasting effects.
Haematologica 93, 653-661
Soltau J, Zirrgiebel U, Esser N, Schaechtele C, Totzke F, Unger C, Merefort I, Drevs J (2008): Antitumoral and Antiangiogenic Efficacy of Bisphosphonates In Vitro and in Murine RENCA Model.
Anticancer Research 28, 933-942
Voigt B, Krug M, Schaechtele C, Totzke F, Hilgeroth A (2008): Probing Novel 1-Aza-9-oxafluorenes as Selective GSK-3beta Inhibitors.
ChemMedChem 3, 120-126
Xu S, Luo Y, Graeser R, Warnecke A, Kratz F, Hauff P, Licha K, Haag R (2008): Development of pH-responsive core-shell nanocarriers for delivery of therapeutic and diagnostic agents.
Biorg. Med. Chem. Lett., in press
Articles published in 2007 (authors from ProQinase are emphasized)
Augustin HG, Fiedler U (2007): Regulation of angiogenesis and vascular homeostasis through the Angiopoietin/Tie system. In: Marmé D, Fusenig N (eds): Tumor Angiogenesis – Basic Mechanism and Cancer Therapy. Springer Verlag, Berlin, pp 109-120
Bettayeb K, Tirado OM, Marionneau-Lambot S, Ferandin Y, Lozach O, Morris JC, Mateo-Lozano S, Drueckes P, Schaechtele C, Kubbutat MHG, Liger F, Marquet B, Joseph B, Echalier A, Endicott JA, Notario V, Meijer L (2007): Meriolins, a new class of cell death inducing kinase inhibitors with enhanced selectivity for cyclin-dependent kinases.
Cancer Res. 1, 8325-34
Dakas PY, Barluenga S, Totzke F, Zirrgiebel U, Winssinger N (2007): Modular synthesis of radicicol A and related resorcylic acid lactones, potent kinase inhibitors.
Angew Chem Int Ed Engl. 46, 6899-902
Drevs J, Siegert P, Medinger M, Mross K, Strecker R, Zirrgiebel U, Harder J, Blum H, Robertson J, Jürgensmeier JM, Puchalski TA, Young H, Saunders O, Unger C (2007): Phase I clinical study of AZD2171, an oral vascular endothelial growth factor signaling inhibitor, in patients with advanced solid tumors.
J Clin Oncol. 25, 3045-54 Fiedler U (2007): Die Bedeutung des Tie / Angiopoietin-1 und -2 Rezeptor / Ligand Systems
in der Angiogenese. In: Mross K (ed): Angiogeneseforschung in der Medizin.
UniMed Verlag, Bremen, pp 35-44
Kohfeld S, Jones PG, Totzke F, Schaechtele C, Kubbutat MHG, Kunick C (2007): 1-Aryl-4,6-dihydropyrazolo[4,3-d][1]benzazepin-5(1H)-ones: A new class of antiproliferative agents with selectivity for human leukemia and breast cancer cell lines.
Eur J Med Chem. 42, 1317-1324
Zirrgiebel U, Schaechtele C (2007): Surrogatmarker. In: Drevs J (ed): Tumorangiogenese - Grundlagen und therapeutische Ansätze. Uni-Med Verlag, Bremen, pp 30-49
Weber H, Claffey J, Hogan M, Pampillón C, Tacke M (2007): Analyses of Titanocenes in the spheroid-based cellular angiogenesis assay.
Toxicol In Vitro. 29
Zahler S, Tietze S, Totzke F, Kubbutat MHG, Meijer L, Vollmar AM, Apostolakis J (2007): Inverse in silico screening for identification of kinase inhibitor targets.
Chemistry & Biology 14, 1207-14
Articles published in 2006 (authors from ProQinase are emphasized)
Fiedler U, Christian S, Koidl S, Kerjaschki D, Emmett MS, Bates DO, Christofori G, Augustin HG (2006): The sialomucin CD34 is a marker of lymphatic endothelial cells in human tumors.
Am J Pathol. 168, 1045-53
Fiedler U, Reiss Y, Scharpfenecker M, Grunow V, Koidl S, Thurston G, Gale NW, Witzenrath M, Rosseau S, Suttorp N, Sobke A, Herrmann M, Preissner KT, Vajkoczy P, Augustin HG (2006): Angiopoietin-2 sensitizes endothelial cells to TNF-alpha and has a crucial role in the induction of inflammation.
Nat Med. 12, 235-9
Fiedler U, Augustin HG (2006): Angiopoietins: a link between angiogenesis and inflammation.
Trends Immunol. 27, 552-8
Kunick C, Bleeker C, Prühs C, Totzke F, Schaechtele C, Kubbutat MHG, Link A (2006): Matrix compare analysis discriminates subtle structural differences in a family of novel antiproliferative agents,diaryl-3-hydroxy-2,3,3a,10a-tetrahydrobenzo[b]cycylopenta[e]azepine-4,10(1H,5H)-diones.
Bioorganic & MedicinalChemistry Letters 16, 2148-53
Moulin E, Barluenga S, Totzke F, Winssinger N (2006): Diversity-oriented synthesis of pochonins and biological evaluation against a panel of kinases.
Chemistry 12, 8819-34
Peifer C, Krasowski A, Hämmerle N, Kohlbacher O, Dannhardt G, Totzke F, Schaechtele C, Laufer S (2006): Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.
J Med Chem. 49, 7549-53
Peifer C, Stoiber T, Unger E, Totzke F, Schaechtele C, Marme D, Brenk R, Klebe G, Schollmeyer D, Dannhardt G (2006): Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors.
J Med Chem. 49, 1271-81
Pfaff D, Fiedler U, Augustin HG (2006): Emerging roles of the Angiopoietin-Tie and the ephrin-Eph systems as regulators of cell trafficking.
J Leukoc Biol. 80, 719-26
Ribas J, Bettayeb K, Ferandin Y, Knockaert M, Garrofe-Ochoa X, Totzke F, Schaechtele C, Mester J, Polychronopoulos P, Magiatis P, Skaltsounis AL, Boix J, Meijer L (2006): 7‑Bromoindirubin-3'-oxime induces caspase-independent cell death.
Oncogene 25, 6304-18
Articles published in 2005 (authors from ProQinase are emphasized)
Agostini H, Boden K, Unsöld A, Martin G, Hansen L, Fiedler U, Esser N, Marmé D (2005): A single local injection of recombinant VEGF receptor 2 but not of Tie2 inhibits retinal neovascularization in the mouse.
Curr Eye Res. 30, 249-57
Bach S, Knockaert M, Reinhardt J, Lozach O, Schmitt S, Baratte B, Koken M, Coburn SP, Tang L, Jiang T, Liang DC, Galons H, Dierick JF, Pinna LA, Meggio F, Totzke F, Schaechtele C, Lerman AS, Carnero A, Wan Y, Gray N, Meijer L (2005): Roscovitine targets, protein kinases and pyridoxal kinase.
J Biol Chem. 280, 31208-31219
Drevs J, Zirrgiebel U, Schmidt-Gersbach CI, Mross K, Medinger M, Lee L, Pinheiro J, Wood J, Thomas AL, Unger C, Henry A, Steward WP, Laurent D, Lebwohl D, Dugan M, Marmé D (2005): Soluble markers for the assessment of biological activity with PTK787/ZK 222584 (PTK/ZK), a vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitor in patients with advanced colorectal cancer from two phase I trials.
Ann Oncol. 4, 558-65
Kunick C, Zeng Z, Gussio R, Zaharevitz D, Leost M, Totzke F, Schaechtele C, Kubbutat MHG, Meijer L, Lemcke T (2005): Structure-aided optimization of kinase inhibitor derived from Alsterpaullone.
ChemBioChem. 6, 1-9
Scharpfenecker M, Fiedler U, Reiss Y, Augustin HG (2005): The Tie-2 ligand angiopoietin-2 destabilizes quiescent endothelium through an internal autocrine loop mechanism.
J Cell Sci. 118, 771-80
Voigt B, Meijer L, Lozach O, Schaechtele C, Totzke F, Hilgeroth A (2005): Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.
Bioorg Med Chem Lett. 15, 823-5
Posters
List of Articles
Posters published in 2008 (authors from ProQinase are emphasized)
Egert-Schmidt AM, Preu L, Totzke F, Schaechtele C, Kubbutat MHG, Kunick C (2008): PYRIMIDO[5',4':5,6]PYRIDIO[3,2-d][1]-BENZAZEPINE-6,9,11-TRIONES: A new type of biologically active heterocycles.
Jahrestagung der Deutschen Pharmazeutischen Gesellschaft, October 8-10, Bonn, Germany
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Ehlert J, Mutschler B, Mueller M, Lingnau A, Hoffmann S, Kubbutat MHG (2008): A test system for assaying inhibitors of the kinase activity of B-Raf V600E in cells and in vivo.
3rd Protein Kinases in Drug Discovery (GTCBIO), May 5-6, San Diego, USA
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Feger D, Umber S, Totzke F, Zirrgiebel U, Lingnau A, Schaechtele C, Kubbutat MHG (2008): Cellular phosphorylation assays - important tools for the characterization of protein kinase inhibitors.
7th Annual Protein Kinase Congress, March 11-12, Berlin, Germany
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Fiedler U, Lingnau A, Hoffmann S, Piersma S, Knoll JC, Jasper A, Jimenez CR, Kubbutat MHG (2008): A novel system to identify target-specific biomarkers.
Biomarkers Europe 2008, November 10-11, Vienna, Austria
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Fiedler U, Lingnau A, Hoffmann S, Jasper A, Totzke F, Zirrgiebel U, Schaechtele C, Kubbutat MHG (2008): Identification of target specific biomarkers to monitor efficient anti-cancer therapies.
Keystone Symposia Conference, February 3-8, Tahoe City, USA
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Graeser R, Esser N, Schillert A, Zeiser R, Jantscheff P, Hildenbrand B, Unger C, Schaechtele C (2008): Development of an orthotopic colon tumor model using HT29 cells with an endogenous population of CD133/CD44 positive cells.
99th Annual Meeting of AACR, April 12-16, San Diego, USA
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Luik S, Goetter M, Graeser R, Schaechtele C, Laufer S (2008): Development of two microplate or microbead beased assay to screen p38δ MAPK inhibitors.
20th Intern. Symposium on Medicinal Chemistry EFMC-ISMC, Aug. 31 - Sept. 04, Vienna, Austria
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Weber W, Weidensteiner C, Reichardt W, von Elverfeldt D, Siedentopf O, Schaechtele C (2008): Blood flow analysis by magnetic resonance imaging in a human endothelial cell derived in vivo angiogenesis model in mice.
Discovery on Target, October 20-23, Boston USA
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Posters published in 2007 (authors from ProQinase are emphasized)
Chamrad DC, Bailey S, Wattenberg A, Beisenherz-Huss C, Graeser R, Müller D, Blüggel M (2007): Systematic PTM Analysis of Protein Kinases Using LC-MS/MS data.
ABRF Conference Creating the Biological Roadmap, March 31 - April 3, Tampa, USAView Poster (PDF)
Egert AM, Kohfeld S, Kubbutat MHG, Schaechtele C, Totzke F, Zaharevitz DW, Kunick C (2007): 2-Anilino-pyrimido [5,4-d][1]Benzazepin-6-ones: Novel inhibitors of cancer-related protein kinases.
Jahrestagung der Deutschen Pharmazeutischen Gesellschaft, October 10-13, Erlangen, Germany
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Ehlert JE, Mutschler B, Weber H, Totzke F, Zirrgiebel U, Krauss R, Lang M, Tasler S, Schaechtele C, Kubbutat MHG (2007): A cellular test system for assaying inhibitors of the focal adhesion kinase (FAK).
CHI's 5th Protein Kinase Targets Meeting, June 4-6, Boston, USA
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Fiedler W, Mesters R, Heuser M, Ehninger G, Ottman OG, Berdel WE, Zirrgiebel U, Robertson J, Puchalski TA, Brave SR, Jürgensmeier JM, Serve H (2007): An open, Phase I study of cediranib (RECENTINTM, AZD2171) in patients with acute myeloid leukemia (AML).
49th Annual Meeting and Exposition of the ASH, December 8-11, Atlanta, USA
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Graeser R, Bornmann C, Esser N, Jantscheff P, Ziroli V, Unger C, Hopt UT, von Dobschuetz E, Schaechtele C, Massing U (2007): Anti-metastatic activity of liposomes demonstrated on an orthotopic mouse model of pancreatic cancer.
98th Annual Meeting of AACR, April 14-18, Los Angeles, USA
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Rohrer S, Dreher J, Kubbutat MHG, Schaechtele C, Totzke F, Kunick C, Baumann K (2007): QSAR modelling of kinases inhibition for several structurally divers compound classes.
3rd Pharmaceutical Sciences World Congress, April 22-25, Amsterdam, The Netherlands
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van Herpen CML, Drevs J, van Cruijsen H, Voest EE, Punt CJ, Robertson J, Saunders O,
Zirrgiebel U, Unger C, Giaccone G (2007): Evaluation of AZD2171, an oral, highly potent and selective VEGFR signaling inhibitor, in renal cell carcinoma (RCC): combined results from two Phase I studies.
43rd ASCO Annual Meeting, June 1-5, Chicago, USA
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Weber H, Hellström M, Kalen M, Korff T, Esser N, and Augustin HG (2007): Large scale screening to identify novel pro- and antiangiogenic compounds using a spheroid based angiogenesis assay.
98th Annual Meeting of AACR, April 14-18, Los Angeles, USA
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Posters published in 2006 (authors from ProQinase are emphasized)
Berger B, Kubbutat MHG, Schaechtele C, Totzke F, Lemcke T, Kunick C (2006): 7-(2-Anilino-4-pyrimidinyl)-1,3,4,5-tetra-hydro-2H-1-benzazepin-2-ones: A new series of aurora A inhibitors.
18th Helsinki Drug Research Meeting, June 1-2, Helsinki, Finland
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Chamrad DC, Bailey S, Wattenberg A, Beisenherz-Huss C, Graeser R, Müller D, Blüggel M (2006): Systematic PTM analysis of a set of recombinant protein kinases using LC-MS/MS data.
54th ASMS Conference on Mass Spectrometry, May 28 - June 1, Seattle, USA
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Dunkel U, Kubbutat MHG, Schaechtele C, Totzke F, Kunick C (2006): Synthesis and kinase inhibitory activity of 7-alkynyl-substituted 1-benzazepin-2(1H)-ones.
18th Helsinki Drug Research Meeting, June 1-2, Helsinki, Finland
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Ehlert JE, Mutschler B, Müller M, Kubbutat MHG (2006): A cellular test system for assaying inhibitors of the kinases activity of B-Raf VE600.
Targeting the Kinome Meeting, December 4-6, Basel, SwitzerlandView Poster (PDF)
Esser N, Chung Da-Eun, Graeser R, Moor S, Jantscheff P, Schaechtele C, Kratz F (2006): An albumin-binding prodrug of doxorubicin that is cleaved by prostate-specific antigen: Development and biological evaluation in an orthotopic mouse model.
18th EORTC-NCI-AACR Symposium, November 7-10, Prague, Czech Republic
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Esser N, Graeser R, Bronmann C, Ziroli V, Unger C, Hopt UT, von Dobschuetz E, Schaechtele C, Massing U (2006): A new liposomal formulation of gemcitabine is active in an orthotopic mouse model of pancreatic cancer (treatment).
97th Annual Meeting of AACR, April 1-5, Washington, USA
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Feger D, Umber S, Kubbutat MHG (2006): Development of a novel cellular test system for the characterisation of inhibitors of the receptor tyrosine kinase FLT3.
18th Helsinki Drug Research Meeting, June 1-2, Helsinki, Finland
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Graeser R, Esser N, Bornmann C, Jantscheff P, Hopt UT, von Dobschuetz E, Massing U, Schaechtele C (2006): Development of metastasizing orthotopic tumor models accesible to in vivo bioluminescence imaging.
97th Annual Meeting of AACR, April 1-5, Washington, USAView Poster (PDF)
Möllenbeck J, Totzke F, Schaechtele C, Kubbutat MHG, Grünert R, Bednarski P, Kunick C (2006): Library of N-(Aryloxyalkyl)-phthalimide kinase inhibitors by parallel synthesis in liquid phase.
18th Helsinki Drug Research Meeting, June 1-2, Helsinki, Finland
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Rouleau N, Fafard C, Flament J, Weber T, Padrós J, Drückes P, Illy C, Bossé R, Parent S (2006): Using AlphaScreen® to Detect GST-Protein Substrate Phosphorylation.
12th Annual Conference and Exhibition of SBS, September 17-21, Seattle, USA
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Posters published in 2005 (authors from ProQinase are emphasized)
Berger B, Kubbutat MHG, Schaechtele C, Totzke F, Bednarski P, Kunick C (2005): Synthesis and kinase inhibitory activity of phenylpropenoylbenzazepinones.
Jahrestagung der Deutschen Pharmazeutischen Gesellschaft, October 5-8, Mainz, Germany
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Dunkel U, Kubbutat MHG, Schaechtele C, Totzke F, Bednarski P, Kunick C (2005): 7-ethyl-1-benzazepine-2,5-diones: Sonogashira synthesis and kinase inhibition profile.
Jahrestagung der Deutschen Pharmazeutischen Gesellschaft, October 5-8, Mainz, Germany
View Poster (PDF) Ehlert J, Mutschler B, Kubbutat MHG (2005): Analyses of protein kinases PKB/Akt1 function and its inhibition using different inducible cellular systems.
CHI's 3rd Annual Protein Kinase Targets Meeting, June 6-7, Boston, USA
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Feger D, Umber S, Birkle A, Schaechtele C, Kubbutat MHG (2005): Development of a novel cellular test system for the characterization of inhibitors of the receptor tyrosine kinase EphB4.
96th Annual Meeting of AACR, April 16-20, Anaheim, USA
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Graeser R, Schaffner F, Esser N, Schaechtele C, Augustin H (2005): Luciferase-based detection of minimal size metastases.
96th Annual Meeting of AACR, April 16-20, Anaheim, USA
View Poster (PDF) Graeser R, Umber S, Zirrgiebel U, Esser N, Kubbutat MHG (2005): Generation of a conditionally transformed MEF cell line using a tetracycline-regulatable IGF1-R allele.
21st Annual Meeting OAO/GTOR/AOR, January 14-15, Freiburg, Germany
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Krauss R, Lang M, Herz T, Saeb W, Tasler S, Totzke F, Ehlert J, Zirrgiebel U, Kubbutat MHG, Vitt D, Schaechtele C (2005): New inhibitors of cancer relevant protein kinases.
Joint Meeting on Medicinal Chemistry, June 20-23, Vienna, Austria
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Lingnau A, Jasper A, Stettner P, Schmitt-Graeff A, Eggstein S, Jungraithmayr W, Steinert MR, Kubbutat MHG (2005): Protein kinase mRNA expression profiling of gastrointestinal and lung cancer by analysis of biopsie “matched pair” tissue samples using Affymetrix microarray technology.
AACR Oncogenomics Meeting, February 2-6, San Diego, USA
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Zirrgiebel U, Ziegler D, Schaechtele C (2005): Multiplexed Biomarker Determination.
21st Annual Meeting OAO/GTOR/AOR, January 14-15, Freiburg, GermanyView Poster (PDF)
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