Publications by authors named "M Zengerle"
Understanding the chemical and electronic properties of point defects in two-dimensional materials, as well as their generation and passivation, is essential for the development of functional systems, spanning from next-generation optoelectronic devices to advanced catalysis. Here, we use synchrotron-based X-ray photoelectron spectroscopy (XPS) with submicron spatial resolution to create sulfur vacancies (SVs) in monolayer MoS and monitor their chemical and electronic properties during the defect creation process. X-ray irradiation leads to the emergence of a distinct Mo 3d spectral feature associated with undercoordinated Mo atoms.
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- PROTACs are specialized molecules designed to selectively target and degrade specific proteins by recruiting an E3 ligase, which leads to the protein's destruction by the proteasome.
- Many PROTACs fall outside the typical chemical structures of common drugs, and there is still limited understanding of how their structures affect their ability to pass through membranes.
- The study introduces a method that combines two assays to evaluate the permeability of VH032-based PROTACs, providing valuable insights into how structural changes can influence their effectiveness and guiding the development of better drugs.
Allele-specific chemical genetics enables selective inhibition within families of highly-conserved proteins. The four BET (bromodomain & extra-terminal domain) proteins - BRD2, BRD3, BRD4 and BRDT bind acetylated chromatin their bromodomains and regulate processes such as cell proliferation and inflammation. BET bromodomains are of particular interest, as they are attractive therapeutic targets but existing inhibitors are pan-selective.
View Article and Find Full Text PDFThe 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 derivatizing two different BET bromodomain inhibitors, triazolodiazepine JQ1 and the more potent tetrahydroquinoline I-BET726, via distinct exit vectors, using different polyethylene glycol linkers to VHL ligand VH032.
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- Pluripotent stem cells (PSCs) can develop into specialized tissues like the pancreas and heart, but how they transition from pluripotency to specific lineages is not fully understood.
- Researchers conducted a small molecule screen to uncover new regulators of the Smad2 signaling network, which is crucial for determining the fate of PSCs.
- They found that BET family proteins play a key role in activating Smad2 through Nodal gene regulatory elements, with Brd4 primarily maintaining pluripotency and Brd2 facilitating differentiation, highlighting how these proteins help manage the transition from pluripotent cells to specialized ones.