A5012403736- Protein Degradation and Inhibitors
- Histone Deacetylase Inhibitors Research
- Antioxidant Activity and Oxidative Stress
- Natural product bioactivities and synthesis
- Plant biochemistry and biosynthesis
- Peptidase Inhibition and Analysis
- 3D Printing in Biomedical Research
- Tissue Engineering and Regenerative Medicine
- Ubiquitin and proteasome pathways
- Electrospun Nanofibers in Biomedical Applications
- Phytochemical compounds biological activities
- 14-3-3 protein interactions
Aristotle University of Thessaloniki
2016-2025
Tufts University
2016
Monopolar spindle 1 (Mps1, also known as TTK) and Aurora kinase (AURK) A B are critical regulators of mitosis have been linked to the progression various cancers. Here, we report design, synthesis, biological evaluation a series PROTACs (proteolysis-targeting chimeras) targeting TTK AURKs. We synthesized degrader molecules based on four different 2-aminoadenine-based ligands, recruiting either cereblon or VHL E3-ligase. Our research showed that nature linker modification ligand significantly...
Abstract Understanding the organization and mechanical function of extracellular matrix (ECM) is critical for development therapeutic strategies that regulate wound healing following disease or injury. However, these relationships are challenging to elucidate during remodeling myocardial infarction (MI) due rapid changes in cellularity an inability characterize both ECM microstructure non-destructively. In this study, we overcome those challenges through whole organ decellularization...
Abstract Despite significant progress in cancer treatment, certain cancers remain difficult to target, particularly when aberrant expression of the c-MYC protein is involved, a target considered "undruggable" due its disordered structure and lack binding sites. Efforts generate small molecule MYC inhibitors (Stellas et al 2014, Truica 2021) have been remarkable but not yet resulted into available clinician. A promising alternative approach targeting other “undruggable” targets discovery...
Although small-molecule inhibitors with moderate efficacy targeting MYC have been previously described, to this point, research efforts failed bring a suitable inhibitor the clinic. Herein, discovery of series novel degraders bearing VHL target "undruggable" is presented. The molecules are based on connecting known binder ligand or pomalidomide induce degradation in various cancer cells express MYC. Representative compounds from our work induced time- and dose-dependent manner. Selected...