Evaluation of peptidomimetic inhibitors
Christopher Lenz, Krishna Saxena, Stefan Knapp
The paper evaluates peptidomimetic inhibitors using a set of complementary assays to support drug discovery.
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Goethe University FrankfurtORCID 0000-0002-2237-5378Unclaimed ORCID profile · follow to get notified of new preprints
5 papers
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Christopher Lenz, Krishna Saxena, Stefan Knapp
The paper evaluates peptidomimetic inhibitors using a set of complementary assays to support drug discovery.
Christopher Lenz, Lewis Elson, Johannes Dopfer…·Stefan Knapp
This study develops peptide-based tracers for SPSB2 E3 ligase by conjugating cell-penetrating peptides to degrons, enabling efficient cellular delivery and target engagement assessment.
Martina Dettenhöfer, Laura Nadine Tandara, Jennifer Alisa Amrhein…·Thomas Hanke
The paper describes the optimization of a macrocyclic scaffold to develop a selective STK10 inhibitor with nanomolar activity and good kinome selectivity.
Joshua Gerninghaus, Rezart Zhubi, Andreas Krämer…·Thomas Hanke
The paper optimizes a 2-aminopyrimidine-based macrocycle to create a dual EPHA2/GAK kinase inhibitor with antiviral activity against dengue virus.
Martin P. Schwalm, Andreas Krämer, Anja Dölle…·Stefan Knapp
This paper develops cell-based assays to monitor PROTAC degradation kinetics and ternary complex formation, revealing that ternary complex stability is critical for PROTAC efficiency.