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View article: Heterobifunctional Protein Binders Enable Cell Type-Specific Killing Through In-cell Enrichment
Heterobifunctional Protein Binders Enable Cell Type-Specific Killing Through In-cell Enrichment Open
Non-catalytic heterobifunctional molecules promise to expand the range of therapeutic options by establishing complexes between key target proteins and accessory presenter proteins equipped with additional properties. Here, we systematical…
View article: Nondegradative Synthetic Molecular Glues Enter the Clinic
Nondegradative Synthetic Molecular Glues Enter the Clinic Open
Molecular glues are small molecules that can induce or stabilize protein–protein interactions between proteins inside cells. Unlike classical small molecule drugs, molecular glues can target challenging disease‐causing proteins lacking wel…
View article: Frontispiece: Conformational Plasticity and Binding Affinity Enhancement Controlled by Linker Derivatization in Macrocycles
Frontispiece: Conformational Plasticity and Binding Affinity Enhancement Controlled by Linker Derivatization in Macrocycles Open
View article: Conformational Plasticity and Binding Affinity Enhancement Controlled by Linker Derivatization in Macrocycles
Conformational Plasticity and Binding Affinity Enhancement Controlled by Linker Derivatization in Macrocycles Open
Macrocycles are abundantly used by nature to enable cell‐permeable bioactive molecules. Synthetic non‐peptidic macrocycles are also increasingly considered as modalities for difficult‐to‐bind proteins but guidelines for macrocyclization ar…
View article: Entwicklung Konformationsbeschränkter Makrozyklen als Verbesserte FKBP51‐Inhibitoren durch Systematische Linker‐Derivatisierung
Entwicklung Konformationsbeschränkter Makrozyklen als Verbesserte FKBP51‐Inhibitoren durch Systematische Linker‐Derivatisierung Open
Makrozyklen werden zunehmend als vielversprechende Strukturklasse zur Bindung für mit herkömmlichen Arzneistoffen schwer erreichbare intrazelluläre Proteine angesehen. Jedoch sind Strategien, bioaktive azyklische Moleküle zu Makrozyklen mi…
View article: Conformationally Restricted Macrocycles as Improved FKBP51 Inhibitors Enabled by Systematic Linker Derivatization
Conformationally Restricted Macrocycles as Improved FKBP51 Inhibitors Enabled by Systematic Linker Derivatization Open
Macrocycles are increasingly considered as promising modalities to target challenging intracellular proteins. However, strategies for transitioning from active linear starting points to improved macrocycles are still underdeveloped. Here w…
View article: Konformationsplastizität und Steigerung der Bindungsaffinität durch Linker‐Derivatisierung in Makrozyklen
Konformationsplastizität und Steigerung der Bindungsaffinität durch Linker‐Derivatisierung in Makrozyklen Open
In der Natur finden Makrozyklen häufig Anwendung, um die Zellpermeabilität von bioaktiven Molekülen zu ermöglichen. Synthetische, nicht‐peptidische Makrozyklen werden zunehmend als Modalitäten für Proteine in Betracht gezogen, die schwer z…
View article: Discovery of fully synthetic FKBP12-mTOR molecular glues
Discovery of fully synthetic FKBP12-mTOR molecular glues Open
We discovered a fully synthetic non-degradative molecular glue for the ternary complex between FKBP12 and the FRB domain of mTOR by screening a library of FKBP12 ligands. Solving the ternary complex structure allowed significant potency en…
View article: Discovery of fully synthetic FKBP12-mTOR molecular glues
Discovery of fully synthetic FKBP12-mTOR molecular glues Open
Molecular glues are a class of drug modalities with the potential to engage otherwise undruggable targets. However, the rational discovery of molecular glues for desired targets is a major challenge and most known molecular glues have been…
View article: Discovery of fully synthetic FKBP12-mTOR molecular glues
Discovery of fully synthetic FKBP12-mTOR molecular glues Open
Molecular glues are a class of drug modalities with the potential to engage otherwise undruggable targets. However, the rational discovery of molecular glues for desired targets is a major challenge and most known molecular glues have ther…