MST and TRIC Technology to Reliably Study PROTAC Binary and Ternary Binding in Drug Development

Authors: Bartoschik, Tanja, Zoephel, Andreas, Rumpel, Klaus, Ciulli, Alessio, Heffern, Charles

Source: Methods in molecular biology. 2365:115-134

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REPLY TO TRAN ET AL. : Dimeric KRAS protein–protein interaction stabilizers

Authors: Kessler, Dirk, Gollner, Andreas, Gmachl, Michael, Mantoulidis, Andreas, Martin, Laetitia J., Zoephel, Andreas, Mayer, Moriz, Covini, David, Fischer, Silke, Gerstberger, Thomas, Gmaschitz, Teresa, Goodwin, Craig, Greb, Peter, Häring, Daniela, Hela, Wolfgang, Hoffmann, Johann, Karolyi-Oezguer, Jale, Knesl, Petr, Kornigg, Stefan, Koegl, Manfred, Kousek, Roland, Lamarre, Lyne, Moser, Franziska, Munico-Martinez, Silvia, Peinsipp, Christoph, Phan, Jason, Rinnenthal, Jörg, Sai, Jiqing, Salamon, Christian, Scherbantin, Yvonne, Schipany, Katharina, Schnitzer, Renate, Schrenk, Andreas, Sharps, Bernadette, Siszler, Gabriella, Sun, Qi, Waterson, Alex, Wolkerstorfer, Bernhard, Zeeb, Markus, Pearson, Mark, Fesik, Stephen W., McConnell, Darryl B.

Source: Proceedings of the National Academy of Sciences of the United States of America, 2020 Feb . 117(7), 3365-3367.

Access URL: https://www.jstor.org/stable/26928963

Drugging an undruggable pocket on KRAS

Authors: Kesslera, Dirk, Gmachla, Michael, Mantoulidisa, Andreas, Martin, Laetitia J., Zoephel, Andreas, Mayer, Moriz, Gollner, Andreas, Covini, David, Fischer, Silke, Gerstberger, Thomas, Gmaschitz, Teresa, Goodwin, Craig, Greb, Peter, Häring, Daniela, Hela, Wolfgang, Hoffmann, Johann, Karolyi-Oezguer, Jale, Knesl, Petr, Kornigg, Stefan, Koegl, Manfred, Kousek, Roland, Lamarre, Lyne, Moser, Franziska, Munico-Martinez, Silvia, Peinsipp, Christoph, Phan, Jason, Rinnenthal, Jörg, Sai, Jiqing, Salamon, Christian, Scherbantin, Yvonne, Schipany, Katharina, Schnitzer, Renate, Schrenk, Andreas, Sharps, Bernadette, Siszler, Gabriella, Sun, Qi, Waterson, Alex, Wolkerstorfer, Bernhard, Zeeb, Markus, Pearson, Mark, Fesik, Stephen W., McConnell, Darryl B.

Source: Proceedings of the National Academy of Sciences of the United States of America, 2019 Aug 01. 116(32), 15823-15829.

Access URL: https://www.jstor.org/stable/26848431

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3

Authors: Böttcher, Jark, Dilworth, David, Reiser, Ulrich, Neumüller, Ralph, Schleicher, Michael, Petronczki, Mark, Zeeb, Markus, Mischerikow, Nikolai, Allali-Hassani, Abdellah, Szewczyk, Magdalena, Li, Fengling, Kennedy, Steven, Vedadi, Masoud, Barsyte-Lovejoy, Dalia, Brown, Peter, Huber, Kilian, Rogers, Catherine, Wells, Carrow, Fedorov, Oleg, Rumpel, Klaus, Zoephel, Andreas, Mayer, Moriz, Wunberg, Tobias, Böse, Dietrich, Zahn, Stephan, Arnhof, Heribert, Berger, Helmut, Reiser, Christoph, Hörmann, Alexandra, Krammer, Teresa, Corcokovic, Maja, Sharps, Bernadette, Winkler, Sandra, Häring, Daniela, Cockcroft, Xiao-Ling, Fuchs, Julian, Müllauer, Barbara, Weiss-Puxbaum, Alexander, Gerstberger, Thomas, Boehmelt, Guido, Vakoc, Christopher, Arrowsmith, Cheryl, Pearson, Mark, McConnell, Darryl

Source: Nature chemical biology. 15(8):822-829

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100185512840.0x000001&indx=1&recIds=ETOCvdc_100185512840.0x000001

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

Authors: Farnaby, William, Koegl, Manfred, Roy, Michael, Whitworth, Claire, Diers, Emelyne, Trainor, Nicole, Zollman, David, Steurer, Steffen, Karolyi-Oezguer, Jale, Riedmueller, Carina, Gmaschitz, Teresa, Wachter, Johannes, Dank, Christian, Galant, Michael, Sharps, Bernadette, Rumpel, Klaus, Traxler, Elisabeth, Gerstberger, Thomas, Schnitzer, Renate, Petermann, Oliver, Greb, Peter, Weinstabl, Harald, Bader, Gerd, Zoephel, Andreas, Weiss-Puxbaum, Alexander, Ehrenhöfer-Wölfer, Katharina, Wöhrle, Simon, Boehmelt, Guido, Rinnenthal, Joerg, Arnhof, Heribert, Wiechens, Nicola, Wu, Meng-Ying, Owen-Hughes, Tom, Ettmayer, Peter, Pearson, Mark, McConnell, Darryl, Ciulli, Alessio

Source: Nature chemical biology. 15(7):672-680

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100184141562.0x000001&indx=1&recIds=ETOCvdc_100184141562.0x000001

Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6

Authors: Kerres, Nina, Steurer, Steffen, Schlager, Stefanie, Bader, Gerd, Berger, Helmut, Caligiuri, Maureen, Dank, Christian, Engen, John R., Ettmayer, Peter, Fischerauer, Bernhard, Flotzinger, Gerlinde, Gerlach, Daniel, Gerstberger, Thomas, Gmaschitz, Teresa, Greb, Peter, Han, Bingsong, Heyes, Elizabeth, Iacob, Roxana E., Kessler, Dirk, Kölle, Heike, Lamarre, Lyne, Lancia, David R., Lucas, Simon, Mayer, Moriz, Mayr, Katharina, Mischerikow, Nikolai, Mück, Katja, Peinsipp, Christoph, Petermann, Oliver, Reiser, Ulrich, Rudolph, Dorothea, Rumpel, Klaus, Salomon, Carina, Scharn, Dirk, Schnitzer, Renate, Schrenk, Andreas, Schweifer, Norbert, Thompson, Diane, Traxler, Elisabeth, Varecka, Roland, Voss, Tilman, Weiss-Puxbaum, Alexander, Winkler, Sandra, Zheng, Xiaozhang, Zoephel, Andreas, Kraut, Norbert, McConnell, Darryl, Pearson, Mark, Koegl, Manfred

Source: In Cell Reports 19 September 2017 20(12):2860-2875

Efficacy of the highly selective focal adhesion kinase inhibitor BI 853520 in adenocarcinoma xenograft models is linked to a mesenchymal tumor phenotype

Authors: Hirt, Ulrich, Waizenegger, Irene, Schweifer, Norbert, Haslinger, Christian, Gerlach, Daniel, Braunger, Jürgen, Weyer-Czernilofsky, Ulrike, Stadtmüller, Heinz, Sapountzis, Ioannis, Bader, Gerd, Zoephel, Andreas, Bister, Bojan, Baum, Anke, Quant, Jens, Kraut, Norbert, Garin-Chesa, Pilar, Adolf, Günther

Source: Oncogenesis. 7(2):1-11

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100117611492.0x000001&indx=1&recIds=ETOCvdc_100117611492.0x000001

Target Binding Properties and Cellular Activity of Afatinib (BIBW 2992), an Irreversible ErbB Family Blocker

Authors: Solca, Flavio ^*, Dahl, Goeran ¹, Zoephel, Andreas, Bader, Gerd, Sanderson, Michael, Klein, Christian, Kraemer, Oliver, Himmelsbach, Frank, Haaksma, Eric, Adolf, Guenther R.

Source: In The Journal of Pharmacology and Experimental Therapeutics November 2012 343(2):342-350

4-heterocycloalkylpyri(mi)dines, process for the preparation thereof and their use as medicaments

Thiazolyl-dihydro-indazoles

THIAZOLYL-DIHYDRO-INDAZOLES

4-HETEROCYCLOALKYLPYRI(MI)DINES, PROCESS FOR THE PREPARATION THEREOF AND THEIR USE AS MEDICAMENTS

Cytokine involved in epithelial-mesenchymal transition

Thiazolyl-dihydro-indazole

Crystal Structure of Bisphosphorylated IGF-1 Receptor Kinase: Insight into Domain Movements upon Kinase Activation

Authors: Pautsch, Alexander ^*, Zoephel, Andreas, Ahorn, Horst, Spevak, Walter, Hauptmann, Rudolf, Nar, Herbert

Source: In Structure 2001 9(10):955-965

Publisher Correction: BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

Authors: Farnaby, William, Koegl, Manfred, Roy, Michael, Whitworth, Claire, Diers, Emelyne, Trainor, Nicole, Zollman, David, Steurer, Steffen, Karolyi-Oezguer, Jale, Riedmueller, Carina, Gmaschitz, Teresa, Wachter, Johannes, Dank, Christian, Galant, Michael, Sharps, Bernadette, Rumpel, Klaus, Traxler, Elisabeth, Gerstberger, Thomas, Schnitzer, Renate, Petermann, Oliver, Greb, Peter, Weinstabl, Harald, Bader, Gerd, Zoephel, Andreas, Weiss-Puxbaum, Alexander, Ehrenhöfer-Wölfer, Katharina, Wöhrle, Simon, Boehmelt, Guido, Rinnenthal, Joerg, Arnhof, Heribert, Wiechens, Nicola, Wu, Meng-Ying, Owen-Hughes, Tom, Ettmayer, Peter, Pearson, Mark, McConnell, Darryl, Ciulli, Alessio

Source: Nature chemical biology. 15(8):846-846

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100185512779.0x000001&indx=1&recIds=ETOCvdc_100185512779.0x000001

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Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis.

Authors: Weinstabl, Harald, Treu, Matthias, Rinnenthal, Joerg, Zahn, Stephan K., Ettmayer, Peter, Bader, Gerd, Dahmann, Georg, Kessler, Dirk, Rumpel, Klaus, Mischerikow, Nikolai, Savarese, Fabio, Gerstberger, Thomas, Mayer, Moriz, Zoephel, Andreas, Schnitzer, Renate, Sommergruber, Wolfgang, Martinelli, Paola, Arnhof, Heribert, Peric-Simov, Biljana, Hofbauer, Karin S.

Source: Journal of Medicinal Chemistry; 9/12/2019, Vol. 62 Issue 17, p7976-7997, 22p

Drugging an undruggable pocket on KRAS.

Authors: Kessler, Dirk, Gmachl, Michael, Mantoulidis, Andreas, Martin, Laetitia J., Zoephel, Andreas, Mayer, Moriz, Gollner, Andreas, Covini, David, Fischer, Silke, Gerstberger, Thomas, Gmaschitz, Teresa, Goodwin, Craig, Greb, Peter, Häring, Daniela, Hela, Wolfgang, Hoffmann, Johann, Karolyi-Oezguer, Jale, Knesl, Petr, Kornigg, Stefan, Koegl, Manfred

Source: Proceedings of the National Academy of Sciences of the United States of America; 8/6/2019, Vol. 116 Issue 32, p15823-15829, 7p

Subject Terms: GENETIC mutation, RAS proteins, RAS oncogenes, DRUG design, MOLECULAR switches, HUMAN genes

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