Articles published in 2010 (authors from ProQinase are emphasized)
Egert-Schmidt AM, Dreher J, Dunkel U, Kohfeld S, Preu L, Weber H, Ehlert JE, Mutschler B, Totzke F, Schaechtele C, Kubbutat MHG, Baumann K, Kunick C (2010): Identification of 2-Anilino-9-methoxy-5,7-dihydro-6H-pyrimido[5,4-d ][1] benzazepin-6-ones as Dual PLK1/VEGF-R2 Kinase Inhibitor Chemotypes by Structure-Based Lead Generation. Journal of Medicinal Chemistry 53, 2433-2442
Elsadek B, Graeser R, Warnecke A, Unger C, Saleem T, El-Melegy N, Madkor H, Kratz F (2010): Optimization of an Albumin-Bindng Prodrug of Doxorubicin That Is Cleaved by Prostate-Specific Antigen. ACS Medicinal Chemistry Letters 1, 234-238
Fichtner I, Claffey J, Deally A, Gleeson B, Hogan M, Markelova MR, Mueller-Bunz H., Weber H, Tacke M (2010): Antitumor activity of vanadocene Y and its selenocyanate derivative in xenografted caki-1 tumors in mice. Journal of Organometallic Chemistry 695, 1175-1181Fürst R, Zirrgiebel U, Totzke F, Zahler S, Vollmar AM, Koch E (2010): The Crataegus extract WS® 1442 inhibits balloon catheter-induced intimal hyperplasia in the rat carotid artery by directly influencing PDGFR-b. Atherosclerosis 211, 409-417Graeser R, Esser N (2010): Bioluminescence in vivo imaging of orthotopically implanted tumor cells in the preclinical drug discovery. In: 3D Imaging: Theory, Technology and Applications. Nova Science Publishers, Inc. Chapter 5
Graeser R, Fiedler U, Esser N, Klotzbuecher A, Weber H, Schaechtele C(2010): The Potency of Refined Mouse Models: Implications for Clinical Trials. Current Cancer Therapy Reviews 6, 62-80
Metzger E, Imhof A, Patel D, Kahl P, Hoffmeyer K, Friedrichs N, Müller MJ, Greschik H, Kirfel J, Ji S, Kunowska N, Beisenherz-Huss C, Günther T, Buettner R, Schüle R (2010): Phosphorylation of histone H3T6 by PKCbI controls demethylation at histone H3K4. nature [Advanced online publication]
Piersma SR, Fiedler U, Span S, Lingnau A, Pham T, Hoffmann S, Kubbutat MHG, Jimenez C (2010): Workflow comparison for in-depth, quantitative secretome proteomics for cancer biomarker discovery: Method evaluation, differential analysis and verification in serum. Journal of Proteome Research 9, 1913-1922
Shi C, Xu MJ, Bayer M, Deng ZW, Kubbutat MHG, Waejen W, Proksch P, Lin WH (2010): Phenolic compounds and their anti-oxidative properties and protein kinase inhibition from the Chinese mangrove plant Laguncularia racemosa Phytochemistry 71, 435-442
Sroka IM, Heiss EH, Havlicek L, Totzke F, Aristei Y, Pechan P, Kubbutat MHG, Strnad M, Dirsch VM(2010): A Novel Roscovitine Derivative Potently Induces G1-Phase Arrest in Platelet-Derived Growth Factor-BB-Activated Vascular Smooth Muscle Cells. Molecular Pharmacology 77, 255-261
Thomas M, Felcht M, Kruse K, Kretschmer S, Deppermann C, Biesdorf A, Rohr K, Benest AV, Fiedler U, Augustin HG (2010): Angiopoietin-2 stimulation of endothelial cells induces avb3 integrin internalization and degradation. Journal of Biological Chemistry [Epub ahead of print June 2]
Articles published in 2009 (authors from ProQinase are emphasized)
Ajaj AK, Graeser R, Fichtner I, Kratz F (2009): In vitro and in vivo study of an albumin-binding prodrug of doxorubicin that is cleaved by cathepsin B. Cancer Chemother Pharmacol, Feb 20 [Epub ahead of print]
Caballero M, Scheele J, Zirrgiebel U, Esser N, Schaechtele C, Soltau J, Rentschler J, Diergarten K, Drevs J (2009): Anti-tumor effects of AMT in the renal cell carcinoma model. Oncology Reports 23, 205-210
Calderón M, Graeser R, Kratz F, Haag R (2009): Development of enzymatically cleavable prodrugs derived from dendritic polyglycerol. Bioorganic & Medicinal Chemistry Letters 19, 3725-3728
Debbab A, Aly AH, Edrada-Ebel R, Wray V, Mueller WE, Totzke F, Zirrgiebel U, Schaechtele C, Kubbutat MHG, Lin WH, Mosaddak M, Hakiki A, Proksch P, Ebel R (2009): Bioactive Metabolites the Endophytic Fungus Stemphylium globuliferum Isolated from Mentha pulegium. Journal of Natural Products, [Epub ahead of print]
Fiedler W, Mesters R, Heuser M, Ehninger G, Berdel WE, Zirrgiebel U, Robertson JD, Puchalski TA, Collins B, Juergensmeier JM, Serve (2009): An open-label, Phase I study of cediranib (RECENTINTM) in patients with acute myeloid leukemia. Leukemia Research, [Epub ahead of print]
Graeser R, Esser N, Unger H, Fichtner I, Zhu A, Unger C, Kratz F (2009): INNO-206, the (6-maleimidocaproyl hydrazone derivative of doxorubicin), shows superior antitumor efficacy compared to doxorubicin in different tumor xenograft models and in an orthotopic pancreas carcinoma model. Invest New Drugs, Jan 8 [Epub ahead of print]
Graeser R, Bornmann C, Esser N, Ziroli V, Jantscheff P, Unger C, Hopt UT, Schaechtele C, von Dobschuetz E, Massing U (2009): Antimetastatic Effects of Liposomal Gemcitabine and Empty Liposomes in an Orthotopic Mouse Model of Pancreatic Cancer. Pancreas, Jan 11 [Epub ahead of print]
Jantscheff P, Ziroli V, Esser N, Graeser R, Kluth J, Sukolinskays A, Taylor LA, Unger C, Massing U (2009): Anti-metastatic effects of liposomal gemcitabine in a human orthotopic LNCaP prostate cancer xenograft model. Clinical & Experimental Metastasis 26, 984-992
Kalén M, Wallgard E, Asker N, Nasevicius A, Athley E, Billgren E, Larson JD, Wadman SA, Norseng E, Clark KJ, He L, Karlsson-Lindahl L, Häge A-K, Weber H, Augustin HG, Samuelsson T, Kemmet CK, Utesch CM, Essner JJ, Hackett PB, Hellström M (2009): Combination of Reverse and Chemical Genetic Screens Reveals Angiogenesis Inhibitors and Targets. Chemistry & Biology 16, 432-441
Nasarre P, Thomas M, Kruse K, Helfrich I, Wolter V, Deppermann C, Schadendorf D, Thurston G, Fiedler U, Augustin HG (2009): Host-Derived Angiopoietin-2 Affects Early Stages of Tumor Development and Vessel Maturation but Is Dispensable for Later Stages of Tumor Growth. Cancer Research 69, 1324-1333
Peifer C, Buehler S, Hauser D, Kinkel K, Totzke F, Schachetele C, Laufer S (2009): Design, synthesis and characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors. Eur J Med Chem. 44, 1788-1793
Shi C, Xu MJ, Bayer M, Deng ZW, Kubbutat MHG, Wätjen W, Proksch P, Lin WH (2009): Phenolic compounds and their anti-oxidative properties and protein kinase inhibition from the Chinese mangrove plant Laguncularia racemosa. Phytochemistry, Dec 17 [Epub ahead of print]
Tasler S, Mueller O, Wieber T, Herz T, Pegoraro S, Saeb W, Lang M, Krauss R, Totzke F, Zirrgiebel U, Ehlert JE, Kubbutat MHG, Schaechtele C(2009): Substituted 2-arylbenzothiazoles as kinase inhibitors: Hit-to-lead optimization. Bioorganic & Medicinal Chemistry Letters 17, 6728-6737 Tasler S, Mueller O, Wieber T, Herz T, Krauss R, Totzke F, Kubbutat MHG, Schaechtele C(2009): N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: Hit identification and scaffold hopping. Bioorganic & Medicinal Chemistry Letters 19, 1349-1356 Wätjen W, Putz A, Chovolou Y, Kampkötter A, Totzke F, Kubbutat MHG, Proksch P, Konuklugil B (2009): Hexa-, hepta- and nonaprenylhydroquinones isolated from marine sponges Sarcotragus muscarum and Ircinia fasciculata inhibit NF-kB signalling in H4IIE cells. Journal of Pharmacy and Pharmacology 61, 919-924
Wätjen W, Debbab A, Hohfeld A, Chovolou Y, Kampkoetter A, Edrada RA, Ebel R, Hakiki A, Mosaddak M, Totzke F, Kubbutat MHG, Proksch P (2009): Enniatins A1, B and B1 from an endophytic strain of Fusarium tricinctum induce apoptotic cell death in H4IIE hepatoma cells accompanied by inhibition of ERK phosphorylation. Molecular Nutrition & Food Research 53, 431-440 Xu S, Luo Y, Graeser R, Warnecke A, Kratz F, Hauff P, Licha K, Haag R (2009): Development of pH-responsive core-shell nanocarriers for delivery of therapeutic and diagnostic agents. Bioorganic & Medicinal Chemistry Letters 19, 1030-1034. Epub 2008 Jan 18.
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. J Nat Prod. 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
Danilenko VN, Simonov AY, Lakatosh SA, Kubbutat MHG, Totzke F, Schaechtele C, Elizarov SM, Bekker OB, Printsevskaya SS, Luzikov YN, Reznikova MI, Shtil AA, Preobrazhenskaya (2008): Search for Inhibitors of Bacterial and Human Protein kInases among Derivatives of Diazepines[1,4] Annelated with Maleimide and Indole Cycles J Med Chem. 51, 7731-7736
Doehn C, Esser N, Pauels HG, Kießig ST, Stelljes M, Grossmann A, Jocham D, Drevs J (2008): Mode-of-Action, Efficacy, and Safety of a Homologous Multi-Epitope Vaccine in a Murine Model for Adjuvant Treatment of Renal Cell Carcinoma. European Urology , Jun 4. [Epub ahead of print]
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
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 published in 2010 (authors from ProQinase are emphasized)
Lingnau A, Feger D, Hoffmann S, Umber S, Kubbutat MHG(2010): A novel human AML bone marrow engraftment mouse model using luciferase expressing MOLM13 cells 5th Annual Cell-Based Assays Conference, June 8-9, Cologne, Germany View Poster (pdf)
Graeser R, Birkle M, Rentzsch C, Schaechtele C(2010): A combined IHC/Western method to measure phosphorylated histone H3 in skin biopsies as potential biomarker for anticancer drug action 101st Annual Meeting of AACR, April 17-21, Washington, USA View Poster (pdf)
Posters published in 2009 (authors from ProQinase are emphasized)
DetermannR, Totzke F, Schaechtele C, Kubbutat MHG, Preu L, Kunick C (2009): 2-ANILINO-4-(BENZIMIDAZOL-2-YL)PYRIMIDINES: A SERIES OF NOVEL MULTIKINASE INHIBITORS DPhG Jahrestagung, September 29-October 1, Jena, Germany View Poster (pdf)Ehlert J, Mutschler B, Mueller M, Feger D, Umber S, Weber H, Ziegler D, Schaechtele C, Kubbutat MHG(2009): Profiling of kinase inhibitors Lapatinib, Tozasertib, Sorafenib, Sunitinib, Erlotinib, Gefitinib and Vatalanib in cellular phosphorylation assays. 100th Annual Meeting of AACR, April 18-22, Denver, USA View Poster (pdf)
Esser N, Graeser R, Fiedler U, Yu T, Mueller I, Schaechtele C(2009): Impressive Antitumoral, Antimetastatic and Antiangiogenic activity of the Thrombin Inhibitor Revasc in an orthotopic mouse model of pancreatic cancer. AACR-NCI-EORTC, November 15-19, Boston, USA View Poster (pdf)
Esser N, Fiedler U, Graeser R, Yu T, Mueller I, Schaechtele C(2009): Antitumor efficacy of PEG-Hirudin (LU 87981), administered three times weekly, in an orthotopic AsPC-1 pancreas carcinoma model. AACR-NCI-EORTC, November 15-19, Boston, USA View Poster (pdf)
Fiedler U, Lingnau A, Hoffmann S, Piersma SR, Knol JC, Jasper A, Jimenez CR, Kubbutat MHG (2009): Identification of protein kinase signaling dependent biomarkers. Biomarker World Congress, Mai 27-29, Philadelphia, USA View Poster (pdf)
Frost A, Karrasch M, Lilla C, Klinkhardt U, Buechert M, Arends J, Fiedler U, Marmé D, Mross K, Fasol U (2009): Dynamic Contrast-Enhanced Magnetic Resonance Imaging (DCE-MRI) as a diagnostic tool for early response to antiangiogenic treatment with cationic liposomal paclitaxel (EndoTAGTM-1) in patients suffering from secondary liver tumors. 100th Annual Meeting of AACR, April 18-22, Denver USA View Poster (pdf)
Graeser R, Esser N, Obodozie C, Schaechtele C(2009): Characterization of a novel orthotopic hepatocarcinoma mouse model using luciferase-transduced Alexander cells. 100th Annual Meeting of AACR, April 18-22, Denver, USA View Poster (pdf)
Graeser R, Esser N, Unger H, Unger C, Kratz F (2009): INNO-206 shows superior antitumor efficacy compared to doxorubicin in an orthotopic pancreas carcinoma model. 100th Annual Meeting of AACR, April 18-22, Denver, USA View Poster (pdf)
Krauss R, Lang M, Herz T, Tasler S, Henry C, Totzke F, Ehlert J, Zirrgiebel U, Klotzbücher A, Feger D, Weber H, Kubbutat MHG, Schaechtele C(2009): 4SC-203, a Novel multi-Target Kinase Inhibitor. PROTEIN KINASE 2009: Signalling Success, 3rd SCI-RSC Symposium on Kinase Inhibitor Design, May 18-19, AstraZeneca, Cheshire, UK View Poster (pdf)
Lingnau A, Feger D, Hoffmann S, Umber S, Graeser R, Esser N, Schaechtele C, Kubbutat MHG(2009): A novel orthotopic AML mouse using intravenously transplanted luciferase expressing human MOLM-13 cells. AACR Special Conference "Mouse Models of Cancer, January 12-15, San Francisco, USA View Poster (pdf)
Schmidt S, Totzke F, Schaechtele C, Kubbutat MHG, Lemcke T, Preu L, Kunick C (2009): Development of novel dual SRC/IGF-1R inhibitors. DPhG Jahrestagung, September 29-October 1, Jena, Germany View Poster (pdf)
Schmidt S, Totzke F, Schaechtele C, Kubbutat MHG, Lemcke T, Preu L, Kunick C (2009): Dual SRC/IGF-1R inhibitors based on 2-(1H-indol-3-yl)-2-oxoacetohydrazide scaffold. Frontiers in Medicinal Chemistry Conference, October 4-6, Barcelona, Spain View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf) 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 View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf)
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, USA View 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 View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf) 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 View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf) 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 View Poster (pdf)
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. 18thHelsinki Drug Research Meeting, June 1-2, Helsinki, Finland View Poster (pdf)
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 View Poster (pdf)
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. 18thHelsinki Drug Research Meeting, June 1-2, Helsinki, Finland View Poster (pdf)
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, Switzerland View 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 View Poster (pdf)
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 View Poster (pdf)
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. 18thHelsinki Drug Research Meeting, June 1-2, Helsinki, Finland View Poster (pdf)
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, USA View 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. 18thHelsinki Drug Research Meeting, June 1-2, Helsinki, Finland View Poster (pdf)
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. 12thAnnual Conference and Exhibition of SBS, September 17-21, Seattle, USA View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf)
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 View Poster (pdf)
Zirrgiebel U, Ziegler D, Schaechtele C(2005): Multiplexed Biomarker Determination. 21st Annual Meeting OAO/GTOR/AOR, January 14-15, Freiburg, Germany View Poster (pdf)
