Vanessa Buffa
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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: 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: Analysis of the Selective Antagonist SAFit2 as a Chemical Probe for the FK506-Binding Protein 51
Analysis of the Selective Antagonist SAFit2 as a Chemical Probe for the FK506-Binding Protein 51 Open
The FK506-binding protein 51 (FKBP51) has emerged as an important regulator of the mammalian stress response and is involved in persistent pain states and metabolic pathways. The FK506 analog SAFit2 (short for selective antagonist of FKBP5…