Sebastian Pomplun
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View article: Barcode-free hit discovery from massive libraries enabled by automated small molecule structure annotation
Barcode-free hit discovery from massive libraries enabled by automated small molecule structure annotation Open
Affinity-selection platforms are powerful tools in early drug discovery, but current technologies – most notably DNA-encoded libraries (DELs) – are limited by synthesis complexity and incompatibility with nucleic acid-binding targets. We p…
View article: AlphaFold‐Guided Discovery of an Overlapping MYC/Miz‐1 Interface Enables Peptidomimetic Disruption of MYC/MAX
AlphaFold‐Guided Discovery of an Overlapping MYC/Miz‐1 Interface Enables Peptidomimetic Disruption of MYC/MAX Open
Intrinsically disordered proteins (IDPs) lack stable structure and classical binding pockets, making them remarkably difficult to drug. However, upon interacting with partner proteins, IDPs can form transient yet specific and defined inter…
View article: Generative Design of High-Affinity Peptides Using BindCraft
Generative Design of High-Affinity Peptides Using BindCraft Open
Discovering high-affinity ligands directly from protein structures remains a key challenge in drug discovery. We applied BindCraft, a structure-guided generative modeling platform, to de novo design of peptide ligands for protein interface…
View article: Barcode-free hit discovery from massive libraries enabled by automated small molecule structure annotation
Barcode-free hit discovery from massive libraries enabled by automated small molecule structure annotation Open
Affinity-selection platforms are powerful tools in early drug discovery, but current technologies – most notably DNA-encoded libraries (DELs) – are limited by synthesis complexity and incompatibility with nucleic acid-binding targets. We p…
View article: Development of DuoMYC: a synthetic cell penetrant miniprotein that efficiently inhibits the oncogenic transcription factor MYC
Development of DuoMYC: a synthetic cell penetrant miniprotein that efficiently inhibits the oncogenic transcription factor MYC Open
The master regulator transcription factor MYC is implicated in numerous human cancers, and its targeting is a long‐standing challenge in drug development. MYC is a typical ‘undruggable’ target, with no binding pockets on its DNA binding do…
View article: Synthetic Peptides: Promising Modalities for the Targeting of Disease‐Related Nucleic Acids
Synthetic Peptides: Promising Modalities for the Targeting of Disease‐Related Nucleic Acids Open
DNA and RNA play pivotal roles in life processes by storing and transferring genetic information, modulating gene expression, and contributing to essential cellular machinery such as ribosomes. Dysregulation and mutations in nucleic acid‐r…
View article: Development of DuoMYC: a synthetic cell penetrant miniprotein that efficiently inhibits the oncogenic transcription factor MYC
Development of DuoMYC: a synthetic cell penetrant miniprotein that efficiently inhibits the oncogenic transcription factor MYC Open
The master regulator transcription factor MYC is implicated in numerous human cancers, and its targeting is a long-standing challenge in drug development. MYC is a typical ‘undruggable’ target, with no binding pockets on its DNA binding do…
View article: Automated Flow Peptide Synthesis Enables Engineering of Proteins with Stabilized Transient Binding Pockets
Automated Flow Peptide Synthesis Enables Engineering of Proteins with Stabilized Transient Binding Pockets Open
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 by genetic approaches, which have been extremely powerful but only allow for mi…
View article: Advances in Ultrahigh Throughput Hit Discovery with Tandem Mass Spectrometry Encoded Libraries
Advances in Ultrahigh Throughput Hit Discovery with Tandem Mass Spectrometry Encoded Libraries Open
Discovering new bioactive molecules is crucial for drug development. Finding a hit compound for a new drug target usually requires screening of millions of molecules. Affinity selection based technologies have revolutionized early hit disc…
View article: Trendbericht Biochemie 2022: Bioaktive Substanzen entdecken: von Display‐Methoden zu selbstkodierten Substanzbibliotheken
Trendbericht Biochemie 2022: Bioaktive Substanzen entdecken: von Display‐Methoden zu selbstkodierten Substanzbibliotheken Open
Über spezialisierte Enzyme, Affinitätsselektionsmethoden, um bioaktive Substanzen zu entdecken, hochauflösende Strukturanalyse von Proteinkomplexen und die Kombination von Bio‐ und Photokatalyse.
View article: Parallel Automated Flow Synthesis of Covalent Protein Complexes That Can Inhibit MYC-Driven Transcription
Parallel Automated Flow Synthesis of Covalent Protein Complexes That Can Inhibit MYC-Driven Transcription Open
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 inhibit, respectively, gene transcription upon binding to the same enhancer box …
View article: Targeting the SARS-CoV-2-spike protein: from antibodies to miniproteins and peptides
Targeting the SARS-CoV-2-spike protein: from antibodies to miniproteins and peptides Open
Fighting COVID-19 with high affinity reagents: this review article summarizes the discovery of several classes of (bio) molecules targeting the SARS-CoV-2 spike protein.
View article: Picomolar FKBP inhibitors enabled by a single water-displacing methyl group in bicyclic [4.3.1] aza-amides
Picomolar FKBP inhibitors enabled by a single water-displacing methyl group in bicyclic [4.3.1] aza-amides Open
Enhancement by displacement. A single methyl group displaces a water molecule from the binding site of FKBPs, resulting in the most potent binders known, outperforming the natural products FK506 and rapamycin in biochemical and cellular as…
View article: <i>De Novo</i> Discovery of High-Affinity Peptide Binders for the SARS-CoV-2 Spike Protein
<i>De Novo</i> Discovery of High-Affinity Peptide Binders for the SARS-CoV-2 Spike Protein Open
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 therapeutics and diagnostics. We used affinity selection-mass spectrometry for the r…
View article: Targeting the SARS-CoV-2-spike protein: from antibodies to miniproteins and peptides
Targeting the SARS-CoV-2-spike protein: from antibodies to miniproteins and peptides Open
Fighting COVID-19 with high affinity reagents: this review article summarizes the discovery of several classes of (bio) molecules targeting the SARS-CoV-2 spike protein.
View article: Discovery of Nucleic Acid Binding Molecules from Combinatorial Biohybrid Nucleobase Peptide Libraries
Discovery of Nucleic Acid Binding Molecules from Combinatorial Biohybrid Nucleobase Peptide Libraries Open
Nature has three biopolymers: oligonucleotides, polypeptides, and oligosaccharides. Each biopolymer has independent functions, but when needed, they form mixed assemblies for higher-order purposes, as in the case of ribosomal protein synth…
View article: <i>De Novo</i>Discovery of High Affinity Peptide Binders for the SARS-CoV-2 Spike Protein
<i>De Novo</i>Discovery of High Affinity Peptide Binders for the SARS-CoV-2 Spike Protein Open
The β-coronavirus SARS-CoV-2 has caused a global pandemic. Affinity reagents targeting the SARS-CoV-2 spike protein, the most exposed surface structure of the virus, are of interest for the development of therapeutics and diagnostics. We u…
View article: Secondary Amino Alcohols: Traceless Cleavable Linkers for Use in Affinity Capture and Release
Secondary Amino Alcohols: Traceless Cleavable Linkers for Use in Affinity Capture and Release Open
Capture and release of peptides is often a critical operation in the pathway to discovering materials with novel functions. However, the best methods for efficient capture impede facile release. To overcome this challenge, we report linker…
View article: Investigation of ACE2 N-terminal fragments binding to SARS-CoV-2 Spike RBD
Investigation of ACE2 N-terminal fragments binding to SARS-CoV-2 Spike RBD Open
Coronavirus disease 19 (COVID-19) is an emerging global health crisis. With over 7 million confirmed cases to date, this pandemic continues to expand, spurring research to discover vaccines and therapies. SARS-CoV-2 is the novel coronaviru…
View article: Chemogenomic Profiling of Human and Microbial FK506-Binding Proteins
Chemogenomic Profiling of Human and Microbial FK506-Binding Proteins Open
FK506-binding proteins (FKBPs) are evolutionarily conserved proteins that display peptidyl-prolyl isomerase activities and act as coreceptors for immunosuppressants. Microbial macrophage-infectivity-potentiator (Mip)-type FKBPs can enhance…