Sven Ullrich
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View article: Shaping the future of constrained peptides and compact proteins in drug discovery
Shaping the future of constrained peptides and compact proteins in drug discovery Open
Constrained peptides and compact proteins are potent alternatives to conventional drug modalities in academia and industry. Located in the chemical space between small molecules and classical biologics, these drug formats feature highly mo…
View article: Assembling Branched and Macrocyclic Peptides on Proteins
Assembling Branched and Macrocyclic Peptides on Proteins Open
A two-step, biocompatible strategy enables site-specific generation of branched and macrocyclic peptide–protein conjugates. Surface-exposed cysteines on proteins are modified by a small bifunctional reagent at near-physiological pH, follow…
View article: Synthesis and stability studies of constrained peptide–antimony bicycles
Synthesis and stability studies of constrained peptide–antimony bicycles Open
Peptide therapeutics play an increasingly important role in modern drug discovery. Improving the pharmacokinetic profile of bioactive peptides has been effectively achieved with chemical modifications, especially macrocyclisation reactions…
View article: Phage-encoded bismuth bicycles enable instant access to targeted bioactive peptides
Phage-encoded bismuth bicycles enable instant access to targeted bioactive peptides Open
Genetically encoded libraries play a crucial role in discovering structurally rigid, high-affinity macrocyclic peptide ligands for therapeutic applications. Bicyclic peptides with metal centres like bismuth were recently developed as a new…
View article: Exploiting Hydrophobic Amino Acid Scanning to Develop Cyclic Peptide Inhibitors of the SARS‐CoV‐2 Main Protease with Antiviral Activity
Exploiting Hydrophobic Amino Acid Scanning to Develop Cyclic Peptide Inhibitors of the SARS‐CoV‐2 Main Protease with Antiviral Activity Open
The development of novel antivirals is crucial not only for managing current COVID‐19 infections but for addressing potential future zoonotic outbreaks. SARS‐CoV‐2 main protease (M pro ) is vital for viral replication and viability and the…
View article: Phage-Encoded Bismuth Bicycles: Instant Access to Targeted Bioactive Peptides
Phage-Encoded Bismuth Bicycles: Instant Access to Targeted Bioactive Peptides Open
Genetically encoded libraries play a crucial role in discovering structurally rigid, high-affinity macrocyclic peptide ligands for therapeutic applications. This study represents the first genetic encoding of peptide-bismuth and peptide-ar…
View article: A RaPID Response to SARS‐CoV‐2
A RaPID Response to SARS‐CoV‐2 Open
Genetically encoded peptide libraries are at the forefront of de novo drug discovery. The RaPID (Random Nonstandard Peptides Integrated Discovery) platform stands out due to the unique combination of flexible in vitro translation (FIT) and…
View article: Bicyclic peptides: Paving the road for therapeutics of the future
Bicyclic peptides: Paving the road for therapeutics of the future Open
Bicyclic peptides have emerged as one of the driving forces within the constrained peptide family. Due to their unique pharmaceutical attributes, peptide bicycles have garnered a reputation as promising therapeutics of the future. Combinin…
View article: Probing Ligand Binding Sites on Large Proteins by Nuclear Magnetic Resonance Spectroscopy of Genetically Encoded Non-Canonical Amino Acids
Probing Ligand Binding Sites on Large Proteins by Nuclear Magnetic Resonance Spectroscopy of Genetically Encoded Non-Canonical Amino Acids Open
N6-(((trimethylsilyl)-methoxy)carbonyl)-l-lysine (TMSK) and N6-trifluoroacetyl-l-lysine (TFAK) are non-canonical amino acids, which can be installed in proteins by genetic encoding. In addition, we descr…
View article: Predicting Antiviral Resistance Mutations in SARS-CoV-2 Main Protease with Computational and Experimental Screening
Predicting Antiviral Resistance Mutations in SARS-CoV-2 Main Protease with Computational and Experimental Screening Open
The main protease (Mpro) of SARS-CoV-2 is essential for viral replication and has been the focus of many drug discovery efforts since the start of the COVID-19 pandemic. Nirmatrelvir (NTV) is an inhibitor of SARS-CoV-2 Mpro…
View article: Site-selective generation of lanthanoid binding sites on proteins using 4-fluoro-2,6-dicyanopyridine
Site-selective generation of lanthanoid binding sites on proteins using 4-fluoro-2,6-dicyanopyridine Open
The paramagnetism of a lanthanoid tag site-specifically installed on a protein provides a rich source of structural information accessible by nuclear magnetic resonance (NMR) and electron paramagnetic resonance (EPR) spectroscopy. Here we …
View article: Predicting antiviral resistance mutations in SARS-CoV-2 main protease with computational and experimental screening
Predicting antiviral resistance mutations in SARS-CoV-2 main protease with computational and experimental screening Open
The main protease (M pro ) of SARS-CoV-2 is essential for viral replication and has been the focus of many drug discovery efforts since the start of the COVID-19 pandemic. Nirmatrelvir (NTV) is an inhibitor of SARS-CoV-2 M pro that is used…
View article: SARS‐CoV‐2 Papain‐Like Protease: Structure, Function and Inhibition
SARS‐CoV‐2 Papain‐Like Protease: Structure, Function and Inhibition Open
Emerging variants of SARS‐CoV‐2 and potential novel epidemic coronaviruses underline the importance of investigating various viral proteins as potential drug targets. The papain‐like protease of coronaviruses has been less explored than ot…
View article: Biokompatible und selektive Generierung bizyklischer Peptide**
Biokompatible und selektive Generierung bizyklischer Peptide** Open
Bizyklische Peptide sind aufgrund ihrer überragenden Eigenschaften für die Arzneimittelforschung von hoher Bedeutung. Ihre chemische Darstellung ist jedoch kompliziert und zudem häufig weder biokompatibel noch orthogonal zu allen kanonisch…
View article: Biocompatible and Selective Generation of Bicyclic Peptides**
Biocompatible and Selective Generation of Bicyclic Peptides** Open
Bicyclic peptides possess superior properties for drug discovery; however, their chemical synthesis is not straightforward and often neither biocompatible nor fully orthogonal to all canonical amino acids. The selective reaction between 1,…
View article: Supplementary material to "Site-selective generation of lanthanoid binding sites on proteins using 4-fluoro-2,6-dicyanopyridine"
Supplementary material to "Site-selective generation of lanthanoid binding sites on proteins using 4-fluoro-2,6-dicyanopyridine" Open
View article: Site-selective generation of lanthanoid binding sites on proteins using 4-fluoro-2,6-dicyanopyridine
Site-selective generation of lanthanoid binding sites on proteins using 4-fluoro-2,6-dicyanopyridine Open
The paramagnetism of a lanthanoid tag site-specifically installed on a protein provides a rich source of structural information accessible by nuclear magnetic resonance (NMR) and electron paramagnetic resonance (EPR) spectroscopy. Here we …
View article: Biocompatible and selective generation of bicyclic peptides
Biocompatible and selective generation of bicyclic peptides Open
Bicyclic peptides possess superior properties for drug discovery; however, their chemical synthesis is not straightforward and often neither biocompatible nor fully orthogonal to all canonical amino acids. The selective reaction between 1,…
View article: Main protease mutants of SARS-CoV-2 variants remain susceptible to nirmatrelvir
Main protease mutants of SARS-CoV-2 variants remain susceptible to nirmatrelvir Open
View article: Antiviral cyclic peptides targeting the main protease of SARS-CoV-2
Antiviral cyclic peptides targeting the main protease of SARS-CoV-2 Open
RaPID mRNA display was used for the discovery of antiviral cyclic peptides that potently and selectively inhibit SARS-CoV-2 M pro . The most potent inhibitor exhibited a novel binding mode, interacting with residues across the homodimer in…
View article: Main protease mutants of SARS-CoV-2 variants remain susceptible to nirmatrelvir (PF-07321332)
Main protease mutants of SARS-CoV-2 variants remain susceptible to nirmatrelvir (PF-07321332) Open
The COVID-19 pandemic continues to be a public health threat. Multiple mutations in the spike protein of emerging variants of SARS-CoV-2 appear to impact on the effectiveness of available vaccines. Specific antiviral agents are keenly anti…
View article: Discovery of Antiviral Cyclic Peptides Targeting the Main Protease of SARS-CoV-2 <i>via</i> mRNA Display
Discovery of Antiviral Cyclic Peptides Targeting the Main Protease of SARS-CoV-2 <i>via</i> mRNA Display Open
Antivirals that specifically target SARS-CoV-2 are needed to control the COVID-19 pandemic. The main protease (M pro ) is essential for SARS-CoV-2 replication and is an attractive target for antiviral development. Here we report the use of…
View article: Challenges of short substrate analogues as SARS-CoV-2 main protease inhibitors
Challenges of short substrate analogues as SARS-CoV-2 main protease inhibitors Open
View article: The SARS-CoV-2 main protease as drug target
The SARS-CoV-2 main protease as drug target Open