Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS
Hodges, Timothy R, Abbott, Jason R, Little, Andrew J, Sarkar, Dhruba, Salovich, James M, Howes, Jennifer E, Akan, Denis T, Sai, Jiqing, Arnold, Allison L, Browning, Carrie, Burns, Michael C, Sobolik, Tammy, Sun, Qi, Beesetty, Yugandhar, Coker, Jesse A, Scharn, Dirk, Stadtmueller, Heinz, Rossanese, Olivia W, Phan, Jason, Waterson, Alex G, McConnell, Darryl B, Fesik, Stephen W
Published in Journal of medicinal chemistry (11.10.2018)
Published in Journal of medicinal chemistry (11.10.2018)
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Journal Article
Endovascular Treatment of Occlusive Lesions in the Aortic Bifurcation with Kissing Polytetrafluoroethylene-Covered Stents
Grimme, Frederike A.B., MD, Spithoven, J. Hans, MD, Zeebregts, Clark J., MD, PhD, Scharn, Dirk M., MD, PhD, Reijnen, Michel M.P.J., MD, PhD
Published in Journal of vascular and interventional radiology (01.09.2015)
Published in Journal of vascular and interventional radiology (01.09.2015)
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Journal Article
Thrombogenicity and Related Biological Properties of Heparin Bonded Collagen Coated Polyester and Human Umbilical Vein Prosthetic Vascular Grafts
Scharn, Dirk M., Oyen, Wim J.G., Klemm, Peter L., Verhofstad, Albert A.J., van der Vliet, J. Adam
Published in The Journal of surgical research (01.08.2006)
Published in The Journal of surgical research (01.08.2006)
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Journal Article
The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML
Gerlach, Daniel, Tontsch-Grunt, Ulrike, Baum, Anke, Popow, Johannes, Scharn, Dirk, Hofmann, Marco H, Engelhardt, Harald, Kaya, Onur, Beck, Janina, Schweifer, Norbert, Gerstberger, Thomas, Zuber, Johannes, Savarese, Fabio, Kraut, Norbert
Published in Oncogene (01.05.2018)
Published in Oncogene (01.05.2018)
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Journal Article
Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors
Engelhardt, Harald, Böse, Dietrich, Petronczki, Mark, Scharn, Dirk, Bader, Gerd, Baum, Anke, Bergner, Andreas, Chong, Eugene, Döbel, Sandra, Egger, Georg, Engelhardt, Christian, Ettmayer, Peter, Fuchs, Julian E, Gerstberger, Thomas, Gonnella, Nina, Grimm, Andreas, Grondal, Elisabeth, Haddad, Nizar, Hopfgartner, Barbara, Kousek, Roland, Krawiec, Mariusz, Kriz, Monika, Lamarre, Lyne, Leung, Joyce, Mayer, Moriz, Patel, Nitinchandra D, Simov, Biljana Peric, Reeves, Jonathan T, Schnitzer, Renate, Schrenk, Andreas, Sharps, Bernadette, Solca, Flavio, Stadtmüller, Heinz, Tan, Zhulin, Wunberg, Tobias, Zoephel, Andreas, McConnell, Darryl B
Published in Journal of medicinal chemistry (27.11.2019)
Published in Journal of medicinal chemistry (27.11.2019)
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Journal Article
Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance
Hofmann, Marco H, Mani, Rajeswaran, Engelhardt, Harald, Impagnatiello, Maria A, Carotta, Sebastian, Kerenyi, Marc, Lorenzo-Herrero, Seila, Böttcher, Jark, Scharn, Dirk, Arnhof, Heribert, Zoephel, Andreas, Schnitzer, Renate, Gerstberger, Thomas, Sanderson, Michael P, Rajgolikar, Girish, Goswami, Swagata, Vasu, Sumithira, Ettmayer, Peter, Gonzalez, Segundo, Pearson, Mark, McConnell, Darryl B, Kraut, Norbert, Muthusamy, Natarajan, Moll, Jürgen
Published in Molecular cancer therapeutics (01.04.2020)
Published in Molecular cancer therapeutics (01.04.2020)
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Journal Article
Abstract 1472: Novel EGFR WT sparing, HER2 selective inhibitors for the treatment of HER2 exon 20 insertion driven tumors address a clear unmet medical need
Neumüller, Ralph A., Wilding, Birgit, Scharn, Dirk, Böse, Dietrich, Santoro, Valeria, Gerlach, Daniel, Ettmayer, Peter, Gerstberger, Thomas, Fuchs, Julian, Treu, Matthias, Zahn, Stephan, Baum, Anke, Chetta, Paolo, Pearson, Mark, McConnell, Darryl B., Kraut, Norbert, Solca, Flavio
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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Journal Article
Zongertinib (BI 1810631), an irreversible HER2 TKI, spares EGFR signaling and improves therapeutic response in preclinical models and patients with HER2-driven cancers
Wilding, Birgit, Woelflingseder, Lydia, Baum, Anke, Chylinski, Krzysztof, Vainorius, Gintautas, Gibson, Neil, Waizenegger, Irene C., Gerlach, Daniel, Augsten, Martin, Spreitzer, Fiona, Shirai, Yukina, Ikegami, Masachika, Tilandyova, Sylvia, Scharn, Dirk, Pearson, Mark A., Popow, Johannes, Obenauf, Anna C., Yamamoto, Noboru, Kondo, Shunsuke, Opdam, Frans L., Bruining, Annemarie, Kohsaka, Shinji, Kraut, Norbert, Heymach, John V., Solca, Flavio, Neumuller, Ralph A.
Published in Cancer discovery (09.09.2024)
Published in Cancer discovery (09.09.2024)
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Journal Article
Abstract 1951: SMAC mimetic and BET inhibitor - a promising combination for solid cancer treatment
Traexler, Paula-Elena, Arnold, Dominik, Ebner, Florian, Slavic-Obradovic, Ksenija, Jacob, Robin, Thanh, Ha Pham Thi, Aichinger, Martin, Baum, Anke, Wernitznig, Andreas, Gerlach, Daniel, Impagnatiello, Maria-Antonietta, Santoro, Valeria, Olt, Sabine, Scharn, Dirk, Ruzicka, Regina, House, Reniqua P., Murphy, Mary Y., Reiser, Ulrich, Engelhardt, Harald, Zinzalla, Vittoria, Laux, Thorsten, Solca, Flavio, Tontsch-Grunt, Ulrike
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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Journal Article
[1,3]DIAZINO[5,4-D]PYRIMIDINE AS HER2 INHIBITOR
SCHARN DIRK, BIRGIT WILDING, HARALD ENGELHARDT, JULIAN FUCHS, MARK PETRONCZKI, DIETRICH BOESE, RALPH NEUMUELLER, MATTHIAS TREU
Year of Publication 20.06.2023
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Year of Publication 20.06.2023
Patent
HER2 억제제로서의 [1,3]디아지노[5,4-d]피리미딘
WILDING BIRGIT, SCHARN DIRK, TREU MATTHIAS, PETRONCZKI MARK, FUCHS JULIAN, NEUMUELLER RALPH, BOESE DIETRICH, ENGELHARDT HARALD
Year of Publication 09.01.2023
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Year of Publication 09.01.2023
Patent
Abstract 6221: Targeting IAP in cancer: BI 891065 a potent small molecule SMAC mimetic that synergizes with immune checkpoint inhibition
Aichinger, Martin, Santoro, Valeria, Slavic-Obradovic, Ksenija, Ruhland, Stefanie, Wernitznig, Andreas, Neudolt, Andrea, Schaefer, Markus, Kallenda, Sabine, Zach, Daniel, Olt, Sabine, Salomon, Carina, Rieser, Sarah, Weissenboeck, Martina, Ebner, Florian, Schlattl, Andreas, De Almeida, Melanie Talata, Langlois, Rebecca, Sykora, Martina, Reschke, Markus, Zichner, Thomas, Gerlach, Daniel, Jude, Julian, Fellner, Michaela, Scharn, Dirk, Kraut, Norbert, Moll, Juergen, Zuber, Johannes, Carotta, Sebastian, Impagnatiello, Maria Antonietta, Tontsch-Grunt, Ulrike
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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Journal Article
Abstract 510: Selective and potent CDK8 inhibitors enhance NK cell activity and promote tumor surveillance
Hofmann, Marco H., Mani, Rajeswaran, Engelhardt, Harald, Impagnatiello, Maria A., Carotta, Sebastian, Kerenyi, Marc A., Lorenzo-Herrero, Seila, Boettcher, Jark, Scharn, Dirk, Arnhof, Heribert, Zoephel, Andreas, Schnitzer, Renate, Gerstberger, Thomas, Rajgolikar, Girish, Goswami, Swagata, Vasu, Sumithira, Ettmayer, Peter, Gonzalez, Segundo R., Pearson, Mark, McConnell, Darryl B., Kraut, Norbert, Muthusamy, Natarajan, Moll, Juergen
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Abstract 2330: BI5: a novel SMAC mimetic that triggers tumor cell death and potentiates PD-1 mediated cancer therapy
Reschke, Markus, Impagnatiello, Maria Antonietta, Reiser, Ulrich, Scharn, Dirk, Spevak, Walter, Savchenko, Alexander, Wernitznig, Andreas, Sykora, Martina, Langlois, Rebecca, Zier, Elisabeth, Zach, Daniel, Kallenda, Sabine, Garin-Chesa, Pilar, Quant, Jens, Pearson, Mark, McConnell, Darryl, Kraut, Norbert, Moll, Juergen
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Journal Article
Abstract 4630: Development of selective and potent CDK8 inhibitors that increase NK cell activity, which translates in tumor surveillance
Hofmann, Marco H., Engelhardt, Harald, Carotta, Sebastian, Arnhof, Heribert, Scharn, Dirk, Kerenyi, Marc, Mayer, Moritz, Gmaschitz, Gerhard, Egger, Georg, Engelhardt, Christian, Sanderson, Michael, Impagnatiello, Maria A., Schnitzer, Renate, Pearson, Mark, McConnell, Darryl, Kraut, Norbert, Moll, Jürgen
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Journal Article
Abstract C140: BI 1810631 is a novel EGFR wild-type sparing, HER2-selective small molecule inhibitor that efficiently blocks HER2 mutant-driven lung cancer
Neumüller, Ralph A., Wilding, Birgit, Scharn, Dirk, Baum, Anke, Augsten, Martin, Waizenegger, Irene, Kohsaka, Shinji, Santoro, Valeria, Chetta, Paolo, Woelflingseder, Lydia, Popow, Johannes, Gerlach, Daniel, Ettmayer, Peter, Gerstberger, Thomas, Fuchs, Julian, Treu, Matthias, Zahn, Stephan, Pearson, Mark, Petronczki, Mark, McConnell, Darryl B., Kraut, Norbert, Solca, Flavio
Published in Molecular cancer therapeutics (01.12.2023)
Published in Molecular cancer therapeutics (01.12.2023)
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Journal Article
Abstract B79: BI 894999, a novel BET inhibitor: Treatment of hematological malignancies by repression of super-enhancer driven oncogenes
Tontsch-Grunt, Ulrike, Savarese, Fabio, Gerlach, Daniel, Gianni, Davide, Baum, Anke, Scharn, Dirk, Engelhardt, Harald, Kaya, Onur, Schweifer, Norbert, Gerstberger, Thomas, Kraut, Norbert
Published in Molecular cancer therapeutics (01.12.2015)
Published in Molecular cancer therapeutics (01.12.2015)
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Journal Article
Effects of the novel BET inhibitor BI 894999 on upregulation of HEXIM1 in cancer cells and on antitumor activity in xenograft tumor models
Tontsch-Grunt, Ulrike, Savarese, Fabio, Baum, Anke, Scharn, Dirk, Gerlach, Daniel, Hofmann, Marco H., Kaya, Onur, Schweifer, Norbert, Engelhardt, Harald, Musa, Hanny, Lee, Chooi Peng, Munzert, Gerd Michael, Kraut, Norbert
Published in Journal of clinical oncology (20.05.2016)
Published in Journal of clinical oncology (20.05.2016)
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Journal Article
Abstract 1525: Chemically induced degradation of the oncogenic transcription factor BCL6
Kerres, Nina, Steurer, Steffen, Schlager, Stefanie, Bader, Gerd, Berger, Helmut, Blake, Sophia, Caligiuri, Maureen, Engen, John, Ettmayer, Peter, Gerstberger, Thomas, Gerlach, Daniel, Jacob, Roxana, Lucas, Simon, Mayer, Moriz, Nikolai, Mischerikow, Klaus, Rumpel, Dirk, Scharn, Renate, Schnitzer, Voss, Tilman, Andreas, Zoephel, Kraut, Norbert, McConnell, Darryl, Mark, Pearson, Koegl, Manfred
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Journal Article
Bispyrimidines as Potent Histamine H-4 Receptor Ligands: Delineation of Structure-Activity Relationships and Detailed H-4 Receptor Binding Mode
Engelhardt, Harald, Schultes, Sabine, de Graaf, Chris, Nijmeijer, Saskia, Vischer, Henry F., Zuiderveld, Obbe P., Dobler, Julia, Stachurski, Katharina, Mayer, Moriz, Arnhof, Heribert, Scharn, Dirk, Haaksma, Eric E. J., de Esch, Iwan J. P., Leurs, Rob
Published in Journal of medicinal chemistry (13.06.2013)
Published in Journal of medicinal chemistry (13.06.2013)
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