Search Results - "Pomplun, Sebastian"

Advances in Ultrahigh Throughput Hit Discovery with Tandem Mass Spectrometry Encoded Libraries by Mata, J. Miguel, van der Nol, Edith, Pomplun, Sebastian J.

“…Discovering new bioactive molecules is crucial for drug development. Finding a hit compound for a new drug target usually requires screening of millions of…”
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Synthetic Peptides: Promising Modalities for the Targeting of Disease‐Related Nucleic Acids by Ellenbroek, Brecht D., Kahler, Jan Pascal, Evers, Sophie R., Pomplun, Sebastian J.

“…DNA and RNA play pivotal roles in life processes by storing and transferring genetic information, modulating gene expression, and contributing to essential…”
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Development of DuoMYC: a synthetic cell penetrant miniprotein that efficiently inhibits the oncogenic transcription factor MYC by Ellenbroek, Brecht D, Kahler, Jan Pascal, Arella, Damiano, Lin, Cherina, Jespers, Willem, Züger, Eliane Ann-Katrin, Drukker, Micha, Pomplun, Sebastian J

“…The master regulator transcription factor MYC is implicated in numerous human cancers, and its targeting is a long-standing challenge in drug development. MYC…”
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De Novo Discovery of High-Affinity Peptide Binders for the SARS-CoV‑2 Spike Protein by Pomplun, Sebastian, Jbara, Muhammad, Quartararo, Anthony J, Zhang, Genwei, Brown, Joseph S, Lee, Yen-Chun, Ye, Xiyun, Hanna, Stephanie, Pentelute, Bradley L

“…The β-coronavirus SARS-CoV-2 has caused a global pandemic. Affinity reagents targeting the SARS-CoV-2 spike protein are of interest for the development of…”
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Synthetic Peptides: Promising Modalities for the Targeting of Disease‐Related Nucleic Acids by Ellenbroek, Brecht D., Kahler, Jan Pascal, Evers, Sophie R., Pomplun, Sebastian J.

“…DNA and RNA play pivotal roles in life processes by storing and transferring genetic information, modulating gene expression, and contributing to essential…”
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Recent Progress in FKBP Ligand Development by Feng, Xixi, Pomplun, Sebastian, Hausch, Felix

“…FK506-binding proteins have been implicated in numerous human diseases suggesting novel therapeutic opportunities. In particular, the large FKBP51 has emerged…”
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Automated Flow Peptide Synthesis Enables Engineering of Proteins with Stabilized Transient Binding Pockets by Charalampidou, Anna, Nehls, Thomas, Meyners, Christian, Gandhesiri, Satish, Pomplun, Sebastian, Pentelute, Bradley L., Lermyte, Frederik, Hausch, Felix

“…Engineering at the amino acid level is key to enhancing the properties of existing proteins in a desired manner. So far, protein engineering has been dominated…”
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Parallel Automated Flow Synthesis of Covalent Protein Complexes That Can Inhibit MYC-Driven Transcription by Pomplun, Sebastian, Jbara, Muhammad, Schissel, Carly K, Wilson Hawken, Susana, Boija, Ann, Li, Charles, Klein, Isaac, Pentelute, Bradley L

“…Dysregulation of the transcription factor MYC is involved in many human cancers. The dimeric transcription factor complexes of MYC/MAX and MAX/MAX activate or…”
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Targeting the SARS-CoV-2-spike protein: from antibodies to miniproteins and peptides by Pomplun, Sebastian

“…Coronavirus disease-19, caused by the novel β-coronavirus SARS-CoV-2, has created a global pandemic unseen in a century. Rapid worldwide efforts have enabled…”
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Use of DNA forceps to measure receptor-ligand dissociation equilibrium constants in a single-molecule competition assay by Stransky, François, Kostrz, Dorota, Follenfant, Maryne, Pomplun, Sebastian, Meyners, Christian, Strick, Terence, Hausch, Felix, Gosse, Charlie

“…The ability of biophysicists to decipher the behavior of individual biomolecules has steadily improved over the past thirty years. However, it still remains…”
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Discovery of Nucleic Acid Binding Molecules from Combinatorial Biohybrid Nucleobase Peptide Libraries by Pomplun, Sebastian, Gates, Zachary P, Zhang, Genwei, Quartararo, Anthony J, Pentelute, Bradley L

“…Nature has three biopolymers: oligonucleotides, polypeptides, and oligosaccharides. Each biopolymer has independent functions, but when needed, they form mixed…”
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Efficient Pictet–Spengler Bioconjugation with N‐Substituted Pyrrolyl Alanine Derivatives by Pomplun, Sebastian, Mohamed, Mohamed Y. H., Oelschlaegel, Tobias, Wellner, Christian, Bergmann, Frank

“…We discovered N‐pyrrolyl alanine derivatives as efficient reagents for the fast and selective Pictet–Spengler reaction with aldehyde‐containing biomolecules…”
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Engineering Bioactive Dimeric Transcription Factor Analogs via Palladium Rebound Reagents by Jbara, Muhammad, Pomplun, Sebastian, Schissel, Carly K, Hawken, Susana Wilson, Boija, Ann, Klein, Isaac, Rodriguez, Jacob, Buchwald, Stephen L, Pentelute, Bradley L

“…Transcription factors (TF), such as Myc, are proteins implicated in disease pathogenesis, with dysregulation of Myc expression in 50% of all human cancers…”
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Rational Design and Asymmetric Synthesis of Potent and Neurotrophic Ligands for FK506-Binding Proteins (FKBPs) by Pomplun, Sebastian, Wang, Yansong, Kirschner, Alexander, Kozany, Christian, Bracher, Andreas, Hausch, Felix

“…To create highly efficient inhibitors for FK506‐binding proteins, a new asymmetric synthesis for pro‐(S)‐C5‐branched [4.3.1] aza‐amide bicycles was developed…”
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Chemogenomic Profiling of Human and Microbial FK506-Binding Proteins by Pomplun, Sebastian, Sippel, Claudia, Hähle, Andreas, Tay, Donald, Shima, Kensuke, Klages, Alina, Ünal, Can Murat, Rieß, Benedikt, Toh, Hui Ting, Hansen, Guido, Yoon, Ho Sup, Bracher, Andreas, Preiser, Peter, Rupp, Jan, Steinert, Michael, Hausch, Felix

“…FK506-binding proteins (FKBPs) are evolutionarily conserved proteins that display peptidyl-prolyl isomerase activities and act as coreceptors for…”
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Picomolar FKBP inhibitors enabled by a single water-displacing methyl group in bicyclic [4.3.1] aza-amides by Kolos, Jürgen M, Pomplun, Sebastian, Jung, Sascha, Rieß, Benedikt, Purder, Patrick L, Voll, Andreas M, Merz, Stephanie, Gnatzy, Monika, Geiger, Thomas M, Quist-Løkken, Ingrid, Jatzlau, Jerome, Knaus, Petra, Holien, Toril, Bracher, Andreas, Meyners, Christian, Czodrowski, Paul, Krewald, Vera, Hausch, Felix

“…Methyl groups can have profound effects in drug discovery but the underlying mechanisms are diverse and incompletely understood. Here we report the…”
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Secondary Amino Alcohols: Traceless Cleavable Linkers for Use in Affinity Capture and Release by Pomplun, Sebastian, Shugrue, Christopher R., Schmitt, Adeline M., Schissel, Carly K., Farquhar, Charlotte E., Pentelute, Bradley L.

“…Capture and release of peptides is often a critical operation in the pathway to discovering materials with novel functions. However, the best methods for…”
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Development of DuoMYC: a synthetic cell penetrant miniprotein that efficiently inhibits the oncogenic transcription factor MYC by Ellenbroek, Brecht D., Kahler, Jan Pascal, Arella, Damiano, Lin, Cherina, Jespers, Willem, Züger, Eliane Ann‐Katrin, Drukker, Micha, Pomplun, Sebastian J.

“…The master regulator transcription factor MYC is implicated in numerous human cancers, and its targeting is a long‐standing challenge in drug development. MYC…”
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Loratadine and analogues: discovery and preliminary structure-activity relationship of inhibitors of the amino acid transporter B(0)AT2 by Cuboni, Serena, Devigny, Christian, Hoogeland, Bastiaan, Strasser, Andrea, Pomplun, Sebastian, Hauger, Barbara, Höfner, Georg, Wanner, Klaus T, Eder, Matthias, Buschauer, Armin, Holsboer, Florian, Hausch, Felix

“…B(0)AT2, encoded by the SLC6A15 gene, is a transporter for neutral amino acids that has recently been implicated in mood and metabolic disorders. It is…”
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Efficient Pictet–Spengler Bioconjugation with N‐Substituted Pyrrolyl Alanine Derivatives by Pomplun, Sebastian, Mohamed, Mohamed Y. H., Oelschlaegel, Tobias, Wellner, Christian, Bergmann, Frank

“…We discovered N‐pyrrolyl alanine derivatives as efficient reagents for the fast and selective Pictet–Spengler reaction with aldehyde‐containing biomolecules…”
Get full text