Search Results - "Pellé, Xavier"

Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1 by Schoepfer, Joseph, Jahnke, Wolfgang, Berellini, Giuliano, Buonamici, Silvia, Cotesta, Simona, Cowan-Jacob, Sandra W, Dodd, Stephanie, Drueckes, Peter, Fabbro, Doriano, Gabriel, Tobias, Groell, Jean-Marc, Grotzfeld, Robert M, Hassan, A. Quamrul, Henry, Chrystèle, Iyer, Varsha, Jones, Darryl, Lombardo, Franco, Loo, Alice, Manley, Paul W, Pellé, Xavier, Rummel, Gabriele, Salem, Bahaa, Warmuth, Markus, Wylie, Andrew A, Zoller, Thomas, Marzinzik, Andreas L, Furet, Pascal

“…Chronic myelogenous leukemia (CML) arises from the constitutive activity of the BCR-ABL1 oncoprotein. Tyrosine kinase inhibitors (TKIs) that target the…”
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An Amphiphilic Polymer-Supported Strategy Enables Chemical Transformations under Anhydrous Conditions for DNA-Encoded Library Synthesis by Ruff, Yves, Martinez, Roberto, Pellé, Xavier, Nimsgern, Pierre, Fille, Pascale, Ratnikov, Maxim, Berst, Frédéric

“…The use of DNA-encoded libraries has emerged as a powerful hit generation technology. Combining the power of combinatorial chemistry to enumerate large…”
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Binding or Bending: Distinction of Allosteric Abl Kinase Agonists from Antagonists by an NMR-Based Conformational Assay by Jahnke, Wolfgang, Grotzfeld, Robert M, Pellé, Xavier, Strauss, André, Fendrich, Gabriele, Cowan-Jacob, Sandra W, Cotesta, Simona, Fabbro, Doriano, Furet, Pascal, Mestan, Jürgen, Marzinzik, Andreas L

“…Allosteric inhibitors of Bcr-Abl have emerged as a novel therapeutic option for the treatment of CML. Using fragment-based screening, a search for novel Abl…”
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Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery by Jahnke, Wolfgang, Rondeau, Jean-Michel, Cotesta, Simona, Marzinzik, Andreas, Pellé, Xavier, Geiser, Martin, Strauss, André, Götte, Marjo, Bitsch, Francis, Hemmig, René, Henry, Chrystèle, Lehmann, Sylvie, Glickman, J Fraser, Roddy, Thomas P, Stout, Steven J, Green, Jonathan R

“…Although FPPS is a potential anti-cancer target, the high bone affinity of nitrogen-containing bisphosphonates, FPPS inhibitors used clinically to treat bone…”
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A General Strategy for Targeting Drugs to Bone by Jahnke, Wolfgang, Bold, Guido, Marzinzik, Andreas L., Ofner, Silvio, Pellé, Xavier, Cotesta, Simona, Bourgier, Emmanuelle, Lehmann, Sylvie, Henry, Chrystelle, Hemmig, René, Stauffer, Frédéric, Hartwieg, J. Constanze D., Green, Jonathan R., Rondeau, Jean-Michel

“…Targeting drugs to their desired site of action can increase their safety and efficacy. Bisphosphonates are prototypical examples of drugs targeted to bone…”
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Discovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead Finding by Marzinzik, Andreas L., Amstutz, René, Bold, Guido, Bourgier, Emmanuelle, Cotesta, Simona, Glickman, J. Fraser, Götte, Marjo, Henry, Christelle, Lehmann, Sylvie, Hartwieg, J. Constanze D., Ofner, Silvio, Pellé, Xavier, Roddy, Thomas P., Rondeau, Jean-Michel, Stauffer, Frédéric, Stout, Steven J., Widmer, Armin, Zimmermann, Johann, Zoller, Thomas, Jahnke, Wolfgang

“…Farnesyl pyrophosphate synthase (FPPS) is an established target for the treatment of bone diseases, but also shows promise as an anticancer and anti‐infective…”
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Gezielte Anreicherung von Wirkstoffen am Knochen am Beispiel von allosterischen FPPS-Inhibitoren by Jahnke, Wolfgang, Bold, Guido, Marzinzik, Andreas L., Ofner, Silvio, Pellé, Xavier, Cotesta, Simona, Bourgier, Emmanuelle, Lehmann, Sylvie, Henry, Chrystelle, Hemmig, René, Stauffer, Frédéric, Hartwieg, J. Constanze D., Green, Jonathan R., Rondeau, Jean-Michel

“…Abstract Die Wirksamkeit und Verträglichkeit eines Medikaments kann verbessert werden, indem dieses gezielt an den gewünschten Wirkungsort gebracht wird…”
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The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1 by Wylie, Andrew A., Schoepfer, Joseph, Jahnke, Wolfgang, Cowan-Jacob, Sandra W., Loo, Alice, Furet, Pascal, Marzinzik, Andreas L., Pelle, Xavier, Donovan, Jerry, Zhu, Wenjing, Buonamici, Silvia, Hassan, A. Quamrul, Lombardo, Franco, Iyer, Varsha, Palmer, Michael, Berellini, Giuliano, Dodd, Stephanie, Thohan, Sanjeev, Bitter, Hans, Branford, Susan, Ross, David M., Hughes, Timothy P., Petruzzelli, Lilli, Vanasse, K. Gary, Warmuth, Markus, Hofmann, Francesco, Keen, Nicholas J., Sellers, William R.

“…The selective allosteric ABL1 inhibitor ABL001 (asciminib) represents a new inhibitory mechanism for BCR–ABL1-driven malignancies, and its efficacy and…”
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Gezielte Anreicherung von Wirkstoffen am Knochen am Beispiel von allosterischen FPPS‐Inhibitoren by Jahnke, Wolfgang, Bold, Guido, Marzinzik, Andreas L., Ofner, Silvio, Pellé, Xavier, Cotesta, Simona, Bourgier, Emmanuelle, Lehmann, Sylvie, Henry, Chrystelle, Hemmig, René, Stauffer, Frédéric, Hartwieg, J. Constanze D., Green, Jonathan R., Rondeau, Jean‐Michel

“…Die Wirksamkeit und Verträglichkeit eines Medikaments kann verbessert werden, indem dieses gezielt an den gewünschten Wirkungsort gebracht wird. Bisphosphonate…”
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Identification of a PCSK9-LDLR disruptor peptide with in vivo function by Brousseau, Margaret E, Clairmont, Kevin B, Spraggon, Glen, Flyer, Alec N, Golosov, Andrei A, Grosche, Philipp, Amin, Jakal, Andre, Jerome, Burdick, Debra, Caplan, Shari, Chen, Guanjing, Chopra, Raj, Ames, Lisa, Dubiel, Diana, Fan, Li, Gattlen, Raphael, Kelly-Sullivan, Dawn, Koch, Alexander W, Lewis, Ian, Li, Jingzhou, Liu, Eugene, Lubicka, Danuta, Marzinzik, Andreas, Nakajima, Katsumasa, Nettleton, David, Ottl, Johannes, Pan, Meihui, Patel, Tajesh, Perry, Lauren, Pickett, Stephanie, Poirier, Jennifer, Reid, Patrick C, Pelle, Xavier, Seepersaud, Mohindra, Subramanian, Vanitha, Vera, Victoria, Xu, Mei, Yang, Lihua, Yang, Qing, Yu, Jinghua, Zhu, Guoming, Monovich, Lauren G

“…Proprotein convertase subtilisin/kexin type 9 (PCSK9) regulates plasma low-density lipoprotein cholesterol (LDL-C) levels by promoting hepatic LDL receptor…”
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Abstract 10516: Identification of a PCSK9-LDLR Disruptor Macrocycle with in vivo Function by Brousseau, Margaret E, Clairmont, Kevin B, Spraggon, Glen, Flyer, Alec N, Golosov, Andrei A, Grosche, Philipp, André, Jérôme, Caplan, Shari, Chen, Guanjing, Fan, Li, Gattlen, Raphael, Koch, Alexander, Lewis, Ian, Li, Jingzhou, Liu, Eugene, Lubicka, Danuta, Marzinzik, Andreas, Nakajima, Katsumasa, Nettleton, David, Ottl, Johannes, Pan, Meihui, Patel, Tajesh, Pickett, Stephanie, Poirier, Jennifer, Reid, Patrick C, Pelle, Xavier, Subramanian, Vanitha, Vera, Victoria, Xu, Mei, Yang, Lihua, Yang, Qing, yu, jinghua, Zhu, Guoming, Monovich, Lauren G

“…Elevated LDL-C is a major risk factor for atherosclerotic cardiovascular disease, the leading cause of death worldwide. Proprotein convertase subtilisin/kexin…”
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The allosteric inhibitor ABL001 enables dual targeting of BCRABL1 by Wylie, Andrew A, Schoepfer, Joseph, Jahnke, Wolfgang, Cowan-Jacob, Sandra W, Loo, Alice, Furet, Pascal, Marzinzik, Andreas L, Pelle, Xavier, Donovan, Jerry, Zhu, Wenjing, Buonamici, Silvia, Hassan, A. Quamrul, Lombardo, Franco, Iyer, Varsha, Palmer, Michael, Berellini, Giuliano, Dodd, Stephanie, Thohan, Sanjeev, Bitter, Hans, Branford, Susan, Ross, David M, Hughes, Timothy P, Petruzzelli, Lilli, Vanasse, K. Gary, Warmuth, Markus, Hofmann, Francesco, Keen, Nicholas J, Sellers, William R

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Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site by Fabbro, Doriano, Manley, Paul W., Jahnke, Wolfgang, Liebetanz, Janis, Szyttenholm, Alexandra, Fendrich, Gabriele, Strauss, Andre, Zhang, Jianming, Gray, Nathanael S., Adrian, Francisco, Warmuth, Markus, Pelle, Xavier, Grotzfeld, Robert, Berst, Frederic, Marzinzik, Andreas, Cowan-Jacob, Sandra W., Furet, Pascal, Mestan, Jürgen

“…The ATP-competitive inhibitors dasatinib and nilotinib, which bind to catalytically different conformations of the Abl kinase domain, have recently been…”
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ABL001, a Potent Allosteric Inhibitor of BCR-ABL, Prevents Emergence of Resistant Disease When Administered in Combination with Nilotinib in an in Vivo Murine Model of Chronic Myeloid Leukemia by Wylie, Andrew, Schoepfer, Joseph, Berellini, Giuliano, Cai, Hongbo, Caravatti, Giorgio, Cotesta, Simona, Dodd, Stephanie, Donovan, Jerry, Erb, Bernhard, Furet, Pascal, Gangal, Geeti, Grotzfeld, Robert, Hassan, Quamrul, Hood, Tami, Iyer, Varsha, Jacob, Sandra, Jahnke, Wolfgang, Lombardo, Franco, Loo, Alice, Manley, Paul W., Marzinzik, Andreas, Palmer, Michael, Pelle, Xavier, Salem, Bahaa, Sharma, Sreenath, Thohan, Sanjeev, Zhu, Suzanne, Keen, Nicholas, Petruzzelli, Lilli, Vanasse, K. Gary, Sellers, William R

“…Background: Chronic myelogenous leukemia (CML) and a subset of acute lymphoblastic leukemia (ALL) are caused by the t(9;22)(q34;q11.2) chromosome…”
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