Michael Zengerle
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View article: Understanding and Improving the Membrane Permeability of VH032-Based PROTACs
Understanding and Improving the Membrane Permeability of VH032-Based PROTACs Open
Proteolysis targeting chimeras (PROTACs) are catalytic heterobifunctional molecules that can selectively degrade a protein of interest by recruiting a ubiquitin E3 ligase to the target, leading to its ubiquitylation and degradation by the …
View article: Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition
Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition Open
Allele-specific chemical genetics enables selective inhibition within families of highly-conserved proteins.
View article: Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds Open
The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 ubiquitin ligase ligand via a linker. Here we examined the impact of…
View article: Brd4‐Brd2 isoform switching coordinates pluripotent exit and Smad2‐dependent lineage specification
Brd4‐Brd2 isoform switching coordinates pluripotent exit and Smad2‐dependent lineage specification Open
Pluripotent stem cells ( PSC s) hold great clinical potential, as they possess the capacity to differentiate into fully specialised tissues such as pancreas, liver, neurons and cardiac muscle. However, the molecular mechanisms that coordin…
View article: Chemical genetics approaches for selective intervention in epigenetics
Chemical genetics approaches for selective intervention in epigenetics Open
Chemical genetics is the use of biologically active small molecules (chemical probes) to investigate the functions of gene products, through the modulation of protein activity. Recent years have seen significant progress in the application…
View article: New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition
New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition Open
We describe new synthetic routes developed toward a range of substituted analogues of bromo and extra-terminal (BET) bromodomain inhibitors I-BET762/JQ1 based on the triazolo-benzodiazepine scaffold. These new routes allow for the derivati…
View article: Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4 Open
The Bromo- and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET selective bromodomain inhibitor JQ1. However, the lack of intra-BE…