Search Results - "Zécri, Frédéric J"

Medicinal Chemistry Profiling of Monocyclic 1,2‐Azaborines by Zhao, Peng, Nettleton, David O., Karki, Rajeshri G., Zécri, Frédéric J., Liu, Shih‐Yuan

“…The first examples of biologically active monocyclic 1,2‐azaborines have been synthesized and demonstrated to exhibit not only improved in vitro aqueous…”
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Water-Compatible Cycloadditions of Oligonucleotide-Conjugated Strained Allenes for DNA-Encoded Library Synthesis by Westphal, Matthias V, Hudson, Liam, Mason, Jeremy W, Pradeilles, Johan A, Zécri, Frédéric J, Briner, Karin, Schreiber, Stuart L

“…DNA-encoded libraries of small molecules are being explored extensively for the identification of binders in early drug-discovery efforts. Combinatorial…”
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From Natural Product to the First Oral Treatment for Multiple Sclerosis: The Discovery of FTY720 (Gilenya™)? by Zécri, Frédéric J

“…[Display omitted] •Derivatization of natural product Myriocin led to the discovery of FTY720.•FTY720 is a strong immune-modulator with a unique mode of…”
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Modular Synthesis of Cyclopropane‐Fused N‐Heterocycles Enabled by Underexplored Diazo Reagents by Richter, Matthieu J. R., Zécri, Frédéric J., Briner, Karin, Schreiber, Stuart L.

“…Cyclopropane‐fused N‐heterocycles are featured in various biologically active compounds and represent attractive scaffolds in medicinal chemistry. However,…”
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Rational Screening for Cooperativity in Small-Molecule Inducers of Protein–Protein Associations by Liu, Shuang, Tong, Bingqi, Mason, Jeremy W., Ostrem, Jonathan M., Tutter, Antonin, Hua, Bruce K., Tang, Sunny A., Bonazzi, Simone, Briner, Karin, Berst, Frédéric, Zécri, Frédéric J., Schreiber, Stuart L.

“…The hallmark of a molecular glue is its ability to induce cooperative protein–protein interactions, leading to the formation of a ternary complex, despite…”
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DNA-encoded library-enabled discovery of proximity-inducing small molecules by Mason, Jeremy W., Chow, Yuen Ting, Hudson, Liam, Tutter, Antonin, Michaud, Gregory, Westphal, Matthias V., Shu, Wei, Ma, Xiaolei, Tan, Zher Yin, Coley, Connor W., Clemons, Paul A., Bonazzi, Simone, Berst, Frédéric, Briner, Karin, Liu, Shuang, Zécri, Frédéric J., Schreiber, Stuart L.

“…Small molecules that induce protein–protein associations represent powerful tools to modulate cell circuitry. We sought to develop a platform for the direct…”
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Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy by Bonazzi, Simone, d'Hennezel, Eva, Beckwith, Rohan E J, Xu, Lei, Fazal, Aleem, Magracheva, Anna, Ramesh, Radha, Cernijenko, Artiom, Antonakos, Brandon, Bhang, Hyo-Eun C, Caro, Roxana García, Cobb, Jennifer S, Ornelas, Elizabeth, Ma, Xiaolei, Wartchow, Charles A, Clifton, Matthew C, Forseth, Ry R, Fortnam, Bethany Hughes, Lu, Hongbo, Csibi, Alfredo, Tullai, Jennifer, Carbonneau, Seth, Thomsen, Noel M, Larrow, Jay, Chie-Leon, Barbara, Hainzl, Dominik, Gu, Yi, Lu, Darlene, Meyer, Matthew J, Alexander, Dylan, Kinyamu-Akunda, Jacqueline, Sabatos-Peyton, Catherine A, Dales, Natalie A, Zécri, Frédéric J, Jain, Rishi K, Shulok, Janine, Wang, Y Karen, Briner, Karin, Porter, Jeffery A, Tallarico, John A, Engelman, Jeffrey A, Dranoff, Glenn, Bradner, James E, Visser, Michael, Solomon, Jonathan M

“…Malignant tumors can evade destruction by the immune system by attracting immune-suppressive regulatory T cells (Treg) cells. The IKZF2 (Helios) transcription…”
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Diversity-oriented synthesis encoded by deoxyoligonucleotides by Hudson, Liam, Mason, Jeremy W., Westphal, Matthias V., Richter, Matthieu J. R., Thielman, Jonathan R., Hua, Bruce K., Gerry, Christopher J., Xia, Guoqin, Osswald, Heather L., Knapp, John M., Tan, Zher Yin, Kokkonda, Praveen, Tresco, Ben I. C., Liu, Shuang, Reidenbach, Andrew G., Lim, Katherine S., Poirier, Jennifer, Capece, John, Bonazzi, Simone, Gampe, Christian M., Smith, Nichola J., Bradner, James E., Coley, Connor W., Clemons, Paul A., Melillo, Bruno, Hon, C. Suk-Yee, Ottl, Johannes, Dumelin, Christoph E., Schaefer, Jonas V., Faust, Ann Marie E., Berst, Frédéric, Schreiber, Stuart L., Zécri, Frédéric J., Briner, Karin

“…Diversity-oriented synthesis (DOS) is a powerful strategy to prepare molecules with underrepresented features in commercial screening collections, resulting in…”
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Author Correction: Diversity-oriented synthesis encoded by deoxyoligonucleotides by Hudson, Liam, Mason, Jeremy W., Westphal, Matthias V., Richter, Matthieu J. R., Thielman, Jonathan R., Hua, Bruce K., Gerry, Christopher J., Xia, Guoqin, Osswald, Heather L., Knapp, John M., Tan, Zher Yin, Kokkonda, Praveen, Tresco, Ben I. C., Liu, Shuang, Reidenbach, Andrew G., Lim, Katherine S., Poirier, Jennifer, Capece, John, Bonazzi, Simone, Gampe, Christian M., Smith, Nichola J., Bradner, James E., Coley, Connor W., Clemons, Paul A., Melillo, Bruno, Hon, C. Suk-Yee, Ottl, Johannes, Dumelin, Christoph E., Schaefer, Jonas V., Faust, Ann Marie E., Berst, Frédéric, Schreiber, Stuart L., Zécri, Frédéric J., Briner, Karin

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Total Synthesis of Thiostrepton. Retrosynthetic Analysis and Construction of Key Building Blocks by Nicolaou, K. C, Safina, Brian S, Zak, Mark, Lee, Sang Hyup, Nevalainen, Marta, Bella, Marco, Estrada, Anthony A, Funke, Christian, Zécri, Frédéric J, Bulat, Stephan

“…The first phase of the total synthesis of thiostrepton (1), a highly complex thiopeptide antibiotic, is described. After a brief introduction to the target…”
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Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P 1) receptor agonists by Zécri, Frédéric J., Albert, Rainer, Landrum, Gregory, Hinterding, Klaus, Cooke, Nigel G., Guerini, Danilo, Streiff, Markus, Bruns, Christian, Nuesslein-Hildesheim, Barbara

“…High throughput screening and hit to lead optimization led to the identification of ‘carene’ as a promising scaffold showing selective S1P 1 receptor agonism…”
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Modular Synthesis of Cyclopropane‐Fused N‐Heterocycles Enabled by Underexplored Diazo Reagents by Richter, Matthieu J. R., Zécri, Frédéric J., Briner, Karin, Schreiber, Stuart L.

“…Cyclopropane‐fused N‐heterocycles are featured in various biologically active compounds and represent attractive scaffolds in medicinal chemistry. However,…”
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Stereocontrolled Synthesis of the Quinaldic Acid Macrocyclic System of Thiostrepton by Nicolaou, K. C., Safina, Brian S., Funke, Christian, Zak, Mark, Zécri, Frédéric J.

“…An efficient construction of the quinaldic acid macrocycle (see picture) of the antibiotic thiostrepton is based on state‐of‐the‐art asymmetric synthesis. The…”
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Facile and purification free synthesis of Mosher amides utilizing a ROMPgel supported reagent by Arnauld, Thomas, Barrett, Anthony G.M, Hopkins, Brian T, Zécri, Frédéric J

“…A novel ROMPgel immobilized active ester for the purification free synthesis of Mosher amides is described. A novel ROMPgel immobilized active ester for the…”
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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors by Lorthiois, Edwige, Gerspacher, Marc, Beyer, Kim S., Vaupel, Andrea, Leblanc, Catherine, Stringer, Rowan, Weiss, Andreas, Wilcken, Rainer, Guthy, Daniel A., Lingel, Andreas, Bomio-Confaglia, Claudio, Machauer, Rainer, Rigollier, Pascal, Ottl, Johannes, Arz, Dorothee, Bernet, Pascal, Desjonqueres, Gaëlle, Dussauge, Solene, Kazic-Legueux, Malika, Lozac’h, Marie-Anne, Mura, Christophe, Sorge, Mickaël, Todorov, Milen, Warin, Nicolas, Zink, Florence, Voshol, Hans, Zecri, Frederic J., Sedrani, Richard C., Ostermann, Nils, Brachmann, Saskia M., Cotesta, Simona

“…Rapid emergence of tumor resistance via RAS pathway reactivation has been reported from clinical studies of covalent KRASG12C inhibitors. Thus, inhibitors with…”
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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS G12C for the Treatment of Solid Tumors by Lorthiois, Edwige, Gerspacher, Marc, Beyer, Kim S, Vaupel, Andrea, Leblanc, Catherine, Stringer, Rowan, Weiss, Andreas, Wilcken, Rainer, Guthy, Daniel A, Lingel, Andreas, Bomio-Confaglia, Claudio, Machauer, Rainer, Rigollier, Pascal, Ottl, Johannes, Arz, Dorothee, Bernet, Pascal, Desjonqueres, Gaëlle, Dussauge, Solene, Kazic-Legueux, Malika, Lozac'h, Marie-Anne, Mura, Christophe, Sorge, Mickaël, Todorov, Milen, Warin, Nicolas, Zink, Florence, Voshol, Hans, Zecri, Frederic J, Sedrani, Richard C, Ostermann, Nils, Brachmann, Saskia M, Cotesta, Simona

“…Rapid emergence of tumor resistance via RAS pathway reactivation has been reported from clinical studies of covalent KRAS inhibitors. Thus, inhibitors with…”
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The design and implementation of a generic lipopeptide scanning platform to enable the identification of ‘locally acting’ agonists for the apelin receptor by McKeown, Stephen C., Zecri, Frederic J., Fortier, Eric, Taggart, Andrew, Sviridenko, Lilya, Adams, Christopher M., McAllister, Kathryn H., Pin, Sokhom S.

“…This Letter describes methodology to enable the identification of tool or therapeutic lipopeptides which modulate the function of membrane bound proteins. The…”
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ROMPGEL Scavengers:  A High-Loading Supported Anhydride for Sequestering Amines and Hydrazines by Arnauld, Thomas, Barrett, Anthony G. M, Cramp, Susan M, Roberts, Richard S, Zécri, Frederic J

“…A versatile method for sequestering excess amines and hydrazines is reported using a high-loading ROMPGEL anhydride polymer…”
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Stereocontrolled Synthesis of the Quinaldic Acid Macrocyclic System of Thiostrepton We thank Drs. D. H. Huang and G. Suizdak for NMR spectroscopic and mass spectrometric assistance, respectively, as well as Mike Sertic (University of California, San Diego) for experimental assistance. Financial support for this work was provided by The Skaggs Institute for Chemical Biology, the National Institutes of Health (USA), fellowships from The Skaggs Institute for Research (to M.Z. and F.Z.), and grants by Nicolaou, K. C., Safina, Brian S., Funke, Christian, Zak, Mark, Zécri, Frédéric J.

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Horner−Emmons Synthesis with Minimal Purification Using ROMPGEL:  A Novel High-Loading Matrix for Supported Reagents by Barrett, Anthony G. M, Cramp, Susan M, Roberts, Richard S, Zecri, Frederic J

“…The synthesis and use of two novel high-loading Horner−Emmons ring-opening metathesis polymers are described. α,β-Unsaturated ethyl esters (E:Z > 99:1) and…”
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