Search Results - "Savarese, Fabio"

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor by Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen

“…Activating mutations in KRAS are the most frequent oncogenic alterations in cancer. The oncogenic hotspot position 12, located at the lip of the switch II…”
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A chromosomal memory triggered by Xist regulates histone methylation in X inactivation by Kohlmaier, Alexander, Savarese, Fabio, Lachner, Monika, Martens, Joost, Jenuwein, Thomas, Wutz, Anton

“…We have elucidated the kinetics of histone methylation during X inactivation using an inducible Xist expression system in mouse embryonic stem (ES) cells…”
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Satb1 and Satb2 regulate embryonic stem cell differentiation and Nanog expression by Savarese, Fabio, Dávila, Amparo, Nechanitzky, Robert, De La Rosa-Velazquez, Inti, Pereira, Carlos F, Engelke, Rudolf, Takahashi, Keiko, Jenuwein, Thomas, Kohwi-Shigematsu, Terumi, Fisher, Amanda G, Grosschedl, Rudolf

“…Satb1 and the closely related Satb2 proteins regulate gene expression and higher-order chromatin structure of multigene clusters in vivo. In examining the role…”
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Hematopoietic Precursor Cells Transiently Reestablish Permissiveness for X Inactivation by Savarese, Fabio, Flahndorfer, Katja, Jaenisch, Rudolf, Busslinger, Meinrad, Wutz, Anton

“…Article Usage Stats Services MCB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Efficacy and mechanism of action of volasertib, a potent and selective inhibitor of Polo-like kinases, in preclinical models of acute myeloid leukemia by Rudolph, Dorothea, Impagnatiello, Maria Antonietta, Blaukopf, Claudia, Sommer, Christoph, Gerlich, Daniel W, Roth, Mareike, Tontsch-Grunt, Ulrike, Wernitznig, Andreas, Savarese, Fabio, Hofmann, Marco H, Albrecht, Christoph, Geiselmann, Lena, Reschke, Markus, Garin-Chesa, Pilar, Zuber, Johannes, Moll, Jürgen, Adolf, Günther R, Kraut, Norbert

“…Polo-like kinase 1 (Plk1), a member of the Polo-like kinase family of serine/threonine kinases, is a key regulator of multiple steps in mitosis. Here we report…”
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Satb1 and Satb2 Are Dispensable for X Chromosome Inactivation in Mice by Nechanitzky, Robert, Dávila, Amparo, Savarese, Fabio, Fietze, Stefanie, Grosschedl, Rudolf

“…Satb1 and Satb2 have been recently described as regulators of embryonic stem (ES) cell pluripotency and as silencing factors in X chromosome inactivation. The…”
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BETter together: exploiting BRD4-functions in transcription to inform rational combinations by Savarese, Fabio, Kraut, Norbert

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The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML by 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

“…Bromodomain and extra-terminal (BET) protein inhibitors have been reported as treatment options for acute myeloid leukemia (AML) in preclinical models and are…”
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Synergistic activity of BET inhibitor BI 894999 with PLK inhibitor volasertib in AML in vitro and in vivo by Tontsch-Grunt, Ulrike, Rudolph, Dorothea, Waizenegger, Irene, Baum, Anke, Gerlach, Daniel, Engelhardt, Harald, Wurm, Melanie, Savarese, Fabio, Schweifer, Norbert, Kraut, Norbert

“…Interactions between a new potent Bromodomain and extraterminal domain (BET) inhibitor BI 894999 and the polo-like kinase (PLK) inhibitor volasertib were…”
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Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis by 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, Garavel, Géraldine, Scherbantin, Yvonne, Mitzner, Sophie, Fett, Thomas N, Scholz, Guido, Bruchhaus, Jens, Burkard, Michelle, Kousek, Roland, Ciftci, Tuncay, Sharps, Bernadette, Schrenk, Andreas, Harrer, Christoph, Haering, Daniela, Wolkerstorfer, Bernhard, Zhang, Xuechun, Lv, Xiaobing, Du, Alicia, Li, Dongyang, Li, Yali, Quant, Jens, Pearson, Mark, McConnell, Darryl B

“…Phosphoglycerate dehydrogenase (PHGDH) is known to be the rate-limiting enzyme in the serine synthesis pathway in humans. It converts glycolysis-derived…”
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Abstract 5194: Epigenomic and transcriptional profiling of CRC cell lines with distinct response patterns to the BET inhibitor BI 894999 by Savarese, Fabio, Gerlach, Daniel, Koller, Larissa, Straubinger, Susy, Träxler, Paula Elena, Kaya, Onur, Schweifer, Norbert, Tontsch-Grunt, Ulrike, Kraut, Norbert

“…Abstract The bromodomain and extra-terminal (BET) protein BRD4 is a “reader” of epigenetic information and binds to acetylated chromatin. BRD4 acts as key…”
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Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS G12C Inhibitor by Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen

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Abstract A030: Evaluation of phosphoprotein- and transcript-based pharmacodynamic biomarkers in pre-clinical studies of the novel SOS1::KRAS inhibitor BI-3406 by Gerlach, Daniel, Savarese, Fabio, Hofmann, Marco H, Trapani, Francesca, Gmachl, Michael, Botesteanu, Dana-Adriana, Ramharter, Jürgen, Arnhof, Heribert, Schweifer, Norbert, McConnell, Darryl B, Kraut, Norbert

“…Abstract KRAS is among the most frequently mutated oncogenes across all human cancers. Targeting KRAS-mutant cancers either directly or at the effector level…”
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Abstract 1271: In vitro and in vivo characterization of BI 1823911 - a novel KRASG12C selective small molecule inhibitor by Savarese, Fabio, Gollner, Andreas, Rudolph, Dorothea, Lipp, Jesse, Popow, Johannes, Hofmann, Marco H., Arnhof, Heribert, Rinnenthal, Jörg, Trapani, Francesca, Gmachl, Michael, Gerlach, Daniel, Broeker, Joachim, Ettmayer, Peter, Mantoulidis, Andreas, Phan, Jason, Smethurst, Christian A., Treu, Matthias, Waterson, Alex G., Lu, Hengyu, Machado, Annette, Daniele, Joseph, Fesik, Stephan W., Vellano, Christopher P., Heffernan, Timothy P., Marszalek, Joseph R., McConnell, Darryl B., Petronczki, Mark, Kraut, Norbert, Waizenegger, Irene C.

“…Abstract KRASG12C mutations are predominantly found in non-small cell lung cancer (NSCLC, 13%), in colorectal cancer (CRC, 3%), and with a lower prevalence in…”
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Blurring cis and trans in Gene Regulation by Savarese, Fabio, Grosschedl, Rudolf

“…In this issue of Cell, Axel and colleagues ( Lomvardas et al., 2006) report that a single enhancer of an odorant receptor (OR) gene cluster interacts with…”
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Abstract PL06-01: Discovery of BI-3406: A potent and selective SOS1::KRAS inhibitor opens a new approach for treating KRAS-driven tumors by Hofmann, Marco H, Gmachl, Michael, Ramharter, Jürgen, Savarese, Fabio, Gerlach, Daniel, Marszalek, Joseph R, Sanderson, Michael P, Trapani, Francesca, Kessler, Dirk, Rumpel, Klaus, Botesteanu, Dana-Adriana, Ettmayer, Peter, Arnhof, Heribert, Gerstberger, Thomas, Kofink, Christiane, Wunberg, Tobias, Fu, Szu-Chin, Teh, Jessica, Vellano, Christopher P., O’Connell, Jonathan C., Mendes, Rachel L, Moll, Juergen, Heffernan, Timothy P., Pearson, Mark, McConnell, Darryl B, Kraut, Norbert

“…Abstract KRAS is the most frequently mutated oncogene with high prevalence in pancreatic, colorectal, and non-small cell lung tumors. KRAS signaling is tightly…”
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Abstract C133: Effective targeting of KRAS-driven tumors by the first-in-class, orally bioavailable SOS1::KRAS inhibitor BI-3406 by Hofmann, Marco H, Gmachl, Michael, Ramharter, Jürgen, Savarese, Fabio, Sanderson, Michael P, Gerlach, Daniel, Trapani, Francesca, Botesteanu, Dana-Adriana, Kessler, Dirk, Ettmayer, Peter, Arnhof, Heribert, Gerstberger, Thomas, Schnitzer, Renate, Kofink, Christiane, Stadtmueller, Heinz, Wunberg, Tobias, O’Connell, Jonathan C., Mendes, Rachel L, Richard, David, Saldanha, Adrian S, Moll, Juergen, Pearson, Mark, McConnell, Darryl B, Kraut, Norbert

“…Abstract KRAS is the most frequently mutated oncogene with high prevalence in pancreatic, colorectal, and non-small cell lung cancers. KRAS signaling is…”
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FOXtrot and RAGtime in B cells by Savarese, Fabio, Grosschedl, Rudolf

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Concurrent SOS1 and MEK suppression inhibits signaling and growth of NF1-null melanoma by Marasco, Michelangelo, Kumar, Dinesh, Seale, Tessa, Borrego, Santiago Garcia, Kaplun, Esther, Aricescu, Ilinca, Cole, Soren, Qeriqi, Besnik, Qiu, Juan, Chen, Xiaoping, Bahr, Amber, Fidele, Deborah, Hofmann, Marco H., Gerlach, Daniel, Savarese, Fabio, Merghoub, Taha, Wolchok, Jedd D., Yao, Zhan, de Stanchina, Elisa, Solit, David, Misale, Sandra, Rosen, Neal

“…Neurofibromin (NF1) is a negative regulator of RAS signaling, frequently mutated in cancer. NF1-mutant melanoma is a highly malignant tumor for which targeted…”
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Abstract B79: BI 894999, a novel BET inhibitor: Treatment of hematological malignancies by repression of super-enhancer driven oncogenes by Tontsch-Grunt, Ulrike, Savarese, Fabio, Gerlach, Daniel, Gianni, Davide, Baum, Anke, Scharn, Dirk, Engelhardt, Harald, Kaya, Onur, Schweifer, Norbert, Gerstberger, Thomas, Kraut, Norbert

“…Abstract Background: Bromodomain and extra-terminal (BET) protein inhibitors comprising the family members BRD2, 3, 4 and T are being extensively studied as…”
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