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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: High Affinity Inhibitors of the Macrophage Infectivity Potentiator Protein from <i>Trypanosoma cruzi</i>, <i>Burkholderia pseudomallei</i>, and <i>Legionella pneumophila</i>─A Comparison
High Affinity Inhibitors of the Macrophage Infectivity Potentiator Protein from <i>Trypanosoma cruzi</i>, <i>Burkholderia pseudomallei</i>, and <i>Legionella pneumophila</i>─A Comparison Open
Since Chagas disease, melioidosis, and Legionnaires' disease are all potentially life-threatening infections, there is an urgent need for new treatment strategies. All causative agents, Trypanosoma cruzi, Burkholderia pseudomalle…
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: 1,4‐Pyrazolyl‐Containing SAFit‐Analogues are Selective FKBP51 Inhibitors With Improved Ligand Efficiency and Drug‐Like Profile
1,4‐Pyrazolyl‐Containing SAFit‐Analogues are Selective FKBP51 Inhibitors With Improved Ligand Efficiency and Drug‐Like Profile Open
The FK506 binding protein 51 (FKBP51) is an appealing drug target due to its role in several diseases such as depression, anxiety, chronic pain and obesity. Towards this, selectivity versus the close homolog FKBP52 is essential. However, c…
View article: Improvement of Inhibitors of the Macrophage Infectivity Potentiator Protein from Trypanosoma cruzi, Burkholderia pseudomallei, and Legionella pneumophila – a Comparison
Improvement of Inhibitors of the Macrophage Infectivity Potentiator Protein from Trypanosoma cruzi, Burkholderia pseudomallei, and Legionella pneumophila – a Comparison Open
The treatment of Chagas disease and infections with Gram-negative bacteria is limited to a low number of antibiotics. Due to the development of resistance and partially severe side effects, there is an urgent need for new treatment strateg…
View article: Discovery of a Potent Proteolysis Targeting Chimera Enables Targeting the Scaffolding Functions of FK506‐Binding Protein 51 (FKBP51)
Discovery of a Potent Proteolysis Targeting Chimera Enables Targeting the Scaffolding Functions of FK506‐Binding Protein 51 (FKBP51) Open
The FK506‐binding protein 51 (FKBP51) is a promising target in a variety of disorders including depression, chronic pain, and obesity. Previous FKBP51‐targeting strategies were restricted to occupation of the FK506‐binding site, which does…
View article: Deconstructing Protein Binding of Sulfonamides and Sulfonamide Analogues
Deconstructing Protein Binding of Sulfonamides and Sulfonamide Analogues Open
Sulfonamides are one of the most important pharmacophores in medicinal chemistry, and sulfonamide analogues have gained substantial interest in recent years. However, the protein interactions of sulfonamides and especially of their analogu…
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…
View article: [4.3.1]Bicyclic FKBP Ligands Inhibit <i>Legionella Pneumophila</i> Infection by <i>Lp</i> Mip‐Dependent and <i>Lp</i> Mip‐Independent Mechanisms**
[4.3.1]Bicyclic FKBP Ligands Inhibit <i>Legionella Pneumophila</i> Infection by <i>Lp</i> Mip‐Dependent and <i>Lp</i> Mip‐Independent Mechanisms** Open
Legionella pneumophila is the causative agent of Legionnaires’ disease, a serious form of pneumonia. Its macrophage infectivity potentiator (Mip), a member of a highly conserved family of FK506‐binding proteins (FKBPs), plays a major role …
View article: Structure-Based Discovery of a New Selectivity-Enabling Motif for the FK506-Binding Protein 51
Structure-Based Discovery of a New Selectivity-Enabling Motif for the FK506-Binding Protein 51 Open
In recent years, the selective inhibition of FKBP51 has emerged as a possible treatment for chronic pain, obesity-induced diabetes, or depression. All currently known advanced FKBP51-selective inhibitors, including the widely used SAFit2, …
View article: Structure-Based Design of High-Affinity Macrocyclic FKBP51 Inhibitors
Structure-Based Design of High-Affinity Macrocyclic FKBP51 Inhibitors Open
The FK506-binding protein 51 (FKBP51) emerged as a key player in several diseases like stress-related disorders, chronic pain, and obesity. Linear analogues of FK506 called SAFit were shown to be highly selective for FKBP51 over its closes…
View article: Switching the Switch: Ligand Induced Disulfide Formation in HDAC8
Switching the Switch: Ligand Induced Disulfide Formation in HDAC8 Open
Human histone deacetylase 8 is a well‐recognized target for T‐cell lymphoma and particularly childhood neuroblastoma. PD‐404,182 was shown to be a selective covalent inhibitor of HDAC8 that forms mixed disulfides with several cysteine resi…
View article: Synthesis and structure activity relationship of 1, 3-benzo-thiazine-2-thiones as selective HDAC8 inhibitors
Synthesis and structure activity relationship of 1, 3-benzo-thiazine-2-thiones as selective HDAC8 inhibitors Open