Search Results - "Holzer, Philipp"

Discovery of Potent and Selective p53-MDM2 Protein-Protein Interaction Inhibitors as Anticancer Drugs by Holzer, Philipp

“…As a result of our persistent efforts to discover novel inhibitors of the p53-MDM2 protein-protein interaction useful for the treatment of cancer, the potent…”
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p53 dynamics vary between tissues and are linked with radiation sensitivity by Stewart-Ornstein, Jacob, Iwamoto, Yoshiko, Miller, Miles A., Prytyskach, Mark A., Ferretti, Stephane, Holzer, Philipp, Kallen, Joerg, Furet, Pascal, Jambhekar, Ashwini, Forrester, William C., Weissleder, Ralph, Lahav, Galit

“…Radiation sensitivity varies greatly between tissues. The transcription factor p53 mediates the response to radiation; however, the abundance of p53 protein…”
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Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors by Holzer, Philipp, Masuya, Keiichi, Furet, Pascal, Kallen, Joerg, Valat-Stachyra, Therese, Ferretti, Stéphane, Berghausen, Joerg, Bouisset-Leonard, Michèle, Buschmann, Nicole, Pissot-Soldermann, Carole, Rynn, Caroline, Ruetz, Stephan, Stutz, Stefan, Chène, Patrick, Jeay, Sébastien, Gessier, Francois

“…As a result of our efforts to discover novel p53:MDM2 protein–protein interaction inhibitors useful for treating cancer, the potent and selective MDM2…”
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Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201 by Jeay, Sébastien, Ferretti, Stéphane, Holzer, Philipp, Fuchs, Jeanette, Chapeau, Emilie A, Wartmann, Markus, Sterker, Dario, Romanet, Vincent, Murakami, Masato, Kerr, Grainne, Durand, Eric Y, Gaulis, Swann, Cortes-Cros, Marta, Ruetz, Stephan, Stachyra, Therese-Marie, Kallen, Joerg, Furet, Pascal, Würthner, Jens, Guerreiro, Nelson, Halilovic, Ensar, Jullion, Astrid, Kauffmann, Audrey, Kuriakose, Emil, Wiesmann, Marion, Jensen, Michael R, Hofmann, Francesco, Sellers, William R

“…Activation of p53 by inhibitors of the p53-MDM2 interaction is being pursued as a therapeutic strategy in p53 wild-type cancers. Here, we report distinct…”
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A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097 by Jeay, Sébastien, Gaulis, Swann, Ferretti, Stéphane, Bitter, Hans, Ito, Moriko, Valat, Thérèse, Murakami, Masato, Ruetz, Stephan, Guthy, Daniel A, Rynn, Caroline, Jensen, Michael R, Wiesmann, Marion, Kallen, Joerg, Furet, Pascal, Gessier, François, Holzer, Philipp, Masuya, Keiichi, Würthner, Jens, Halilovic, Ensar, Hofmann, Francesco, Sellers, William R, Graus Porta, Diana

“…Biomarkers for patient selection are essential for the successful and rapid development of emerging targeted anti-cancer therapeutics. In this study, we report…”
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Structural States of Hdm2 and HdmX: X‐ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes by Kallen, Joerg, Izaac, Aude, Chau, Suzanne, Wirth, Emmanuelle, Schoepfer, Joseph, Mah, Robert, Schlapbach, Achim, Stutz, Stefan, Vaupel, Andrea, Guagnano, Vito, Masuya, Keiichi, Stachyra, Therese‐Marie, Salem, Bahaa, Chene, Patrick, Gessier, Francois, Holzer, Philipp, Furet, Pascal

“…Hdm2 (human MDM2, human double minute 2 homologue) counteracts p53 function by direct binding to p53 and by ubiquitin‐dependent p53 protein degradation…”
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The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis by Martiny-Baron, Georg, Holzer, Philipp, Billy, Eric, Schnell, Christian, Brueggen, Joseph, Ferretti, Mireille, Schmiedeberg, Niko, Wood, Jeanette M., Furet, Pascal, Imbach, Patricia

“…EphB4 and its cognitive ligand ephrinB2 play an important role in embryonic vessel development and vascular remodeling. In addition, several reports suggest…”
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Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach by Chen, Chao, Zhu, Hugh, Stauffer, Frédéric, Caravatti, Giorgio, Vollmer, Susanne, Machauer, Rainer, Holzer, Philipp, Möbitz, Henrik, Scheufler, Clemens, Klumpp, Martin, Tiedt, Ralph, Beyer, Kim S, Calkins, Keith, Guthy, Daniel, Kiffe, Michael, Zhang, Jeff, Gaul, Christoph

“…Oncogenic MLL fusion proteins aberrantly recruit Dot1L, a histone methyltransferase, to ectopic loci, leading to local hypermethylation of H3K79 and…”
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Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach by Möbitz, Henrik, Machauer, Rainer, Holzer, Philipp, Vaupel, Andrea, Stauffer, Frédéric, Ragot, Christian, Caravatti, Giorgio, Scheufler, Clemens, Fernandez, Cesar, Hommel, Ulrich, Tiedt, Ralph, Beyer, Kim S, Chen, Chao, Zhu, Hugh, Gaul, Christoph

“…Misdirected catalytic activity of histone methyltransferase Dot1L is believed to be causative for a subset of highly aggressive acute leukemias. Targeting the…”
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Abstract 1239: NVP-HDM201: Biochemical and biophysical profile of a novel highly potent and selective PPI inhibitor of p53-Mdm2 by Stachyra-Valat, Thérèse, Baysang, Frédéric, D’Alessandro, Anne-Cécile, Dirk, Erdmann, Furet, Pascal, Guagnano, Vito, Kallen, Joerg, Leder, Lukas, Mah, Robert, Masuya, Keiichi, Stutz, Stefan, Vaupel, Andrea, Hofmann, Francesco, Chène, Patrick, Jeay, Sébastien, Holzer, Philipp

“…Abstract An effective strategy to restore p53 activity in cancer cells containing wild type p53 is to inhibit the Mdm2-p53 protein-protein interaction (PPI)…”
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Correction: A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097 by Jeay, Sébastien, Gaulis, Swann, Ferretti, Stéphane, Bitter, Hans, Ito, Moriko, Valat, Thérèse, Murakami, Masato, Ruetz, Stephan, Guthy, Daniel A, Rynn, Caroline, Jensen, Michael R, Wiesmann, Marion, Kallen, Joerg, Furet, Pascal, Gessier, François, Holzer, Philipp, Masuya, Keiichi, Würthner, Jens, Halilovic, Ensar, Hofmann, Francesco, Sellers, William R, Graus Porta, Diana

“…Sonkin’s approach would require multiple technologies to measure p53 gene expression and p53 copy number in addition to sequencing the full-length of p53 for…”
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Theory of photoionization-induced blueshift of ultrashort solitons in gas-filled hollow-core photonic crystal fibers by Saleh, Mohammed F, Chang, Wonkeun, Hölzer, Philipp, Nazarkin, Alexander, Travers, John C, Joly, Nicolas Y, Russell, Philip St J, Biancalana, Fabio

“…We show theoretically that the photoionization process in a hollow-core photonic crystal fiber filled with a Raman-inactive noble gas leads to a constant…”
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Click chemistry in materials synthesis. 1. Adhesive polymers from copper-catalyzed azide-alkyne cycloaddition by Díaz, David D., Punna, Sreenivas, Holzer, Philipp, McPherson, Andrew K., Sharpless, K. Barry, Fokin, Valery V., Finn, M. G.

“…The copper(I)‐catalyzed cycloaddition reaction between azides and alkynes has been employed to make metal‐adhesive materials. Copper and brass surfaces supply…”
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Heavy-ion-induced desorption yields of cryogenic surfaces bombarded with 1.4     MeV / u xenon ions by Holzer, Donat Philipp, Mahner, Edgar, Kollmus, Holger, Bender, Markus, Severin, Daniel, Wengenroth, Marc

“…Heavy-ion-induced desorption of two different cryogenic targets was studied with a new experimental setup installed at the GSI High Charge State Injector. One…”
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Discovery of a novel class of highly potent inhibitors of the p53–MDM2 interaction by structure-based design starting from a conformational argument by Furet, Pascal, Masuya, Keiichi, Kallen, Joerg, Stachyra-Valat, Thérèse, Ruetz, Stephan, Guagnano, Vito, Holzer, Philipp, Mah, Robert, Stutz, Stefan, Vaupel, Andrea, Chène, Patrick, Jeay, Sébastien, Schlapbach, Achim

“…[Display omitted] The p53–MDM2 interaction is an anticancer drug target under investigation in the clinic. Our compound NVP-CGM097 is one of the small molecule…”
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Synthesis of the Potent, Selective, and Efficacious β‑Secretase (BACE1) Inhibitor NB-360 by Rueeger, Heinrich, Lueoend, Rainer, Machauer, Rainer, Veenstra, Siem J, Holzer, Philipp, Hurth, Konstanze, Voegtle, Markus, Frederiksen, Mathias, Rondeau, Jean-Michel, Tintelnot-Blomley, Marina, Jacobson, Laura H, Staufenbiel, Matthias, Laue, Grit, Neumann, Ulf

“…Starting from lead compound 4, the 1,4-oxazine headgroup was optimized to improve potency and brain penetration. Focusing at the 6-position of the…”
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DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance by Schröder, Martin, Renatus, Martin, Liang, Xiaoyou, Meili, Fabian, Zoller, Thomas, Ferrand, Sandrine, Gauter, Francois, Li, Xiaoyan, Sigoillot, Frederic, Gleim, Scott, Stachyra, Therese-Marie, Thomas, Jason R., Begue, Damien, Khoshouei, Maryam, Lefeuvre, Peggy, Andraos-Rey, Rita, Chung, BoYee, Ma, Renate, Pinch, Benika, Hofmann, Andreas, Schirle, Markus, Schmiedeberg, Niko, Imbach, Patricia, Gorses, Delphine, Calkins, Keith, Bauer-Probst, Beatrice, Maschlej, Magdalena, Niederst, Matt, Maher, Rob, Henault, Martin, Alford, John, Ahrne, Erik, Tordella, Luca, Hollingworth, Greg, Thomä, Nicolas H., Vulpetti, Anna, Radimerski, Thomas, Holzer, Philipp, Carbonneau, Seth, Thoma, Claudio R.

“…Targeted protein degradation (TPD) mediates protein level through small molecule induced redirection of E3 ligases to ubiquitinate neo-substrates and mark them…”
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Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53–MDM2 interaction with a distinct binding mode by Gessier, François, Kallen, Joerg, Jacoby, Edgar, Chène, Patrick, Stachyra-Valat, Thérèse, Ruetz, Stephan, Jeay, Sébastien, Holzer, Philipp, Masuya, Keiichi, Furet, Pascal

“…[Display omitted] Blocking the interaction between the p53 tumor suppressor and its regulatory protein MDM2 is a promising therapeutic concept under current…”
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In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor by Vaupel, Andrea, Holzer, Philipp, Ferretti, Stephane, Guagnano, Vito, Kallen, Joerg, Mah, Robert, Masuya, Keiichi, Ruetz, Stephan, Rynn, Caroline, Schlapbach, Achim, Stachyra, Thérèse, Stutz, Stefan, Todorov, Milen, Jeay, Sébastien, Furet, Pascal

“…[Display omitted] •Novel rationally designed p53-MDM2 inhibitor scaffold.•Structural proof of concept by x-ray crystallography.•Optimization of metabolic…”
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Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field by Vulpetti, Anna, Holzer, Philipp, Schmiedeberg, Niko, Imbach-Weese, Patricia, Pissot-Soldermann, Carole, Hollingworth, Gregory J., Radimerski, Thomas, Thoma, Claudio R., Stachyra, Therese-Marie, Wojtynek, Matthias, Maschlej, Magdalena, Chau, Suzanne, Schuffenhauer, Ansgar, Fernández, César, Schröder, Martin, Renatus, Martin

“…In this study, we describe the rapid identification of potent binders for the WD40 repeat domain (WDR) of DCAF1. This was achieved by two rounds of iterative…”
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