A5068968830- Peptidase Inhibition and Analysis
- Chemical Synthesis and Analysis
- Bone Metabolism and Diseases
- Nanoplatforms for cancer theranostics
- Protease and Inhibitor Mechanisms
- Advanced biosensing and bioanalysis techniques
- Nanoparticle-Based Drug Delivery
- Neuropeptides and Animal Physiology
- Cancer, Stress, Anesthesia, and Immune Response
- S100 Proteins and Annexins
- Immunotherapy and Immune Responses
- Cancer Immunotherapy and Biomarkers
- CAR-T cell therapy research
- Monoclonal and Polyclonal Antibodies Research
- Biochemical and Structural Characterization
- Inflammatory mediators and NSAID effects
- Click Chemistry and Applications
- Pharmacological Effects and Assays
- Pharmacological Receptor Mechanisms and Effects
- Protein Degradation and Inhibitors
- Histone Deacetylase Inhibitors Research
- Cell Adhesion Molecules Research
- Enzyme function and inhibition
Czech Academy of Sciences, Institute of Organic Chemistry and Biochemistry
2018-2024
Charles University
2020-2024
Czech Academy of Sciences
2024
Histone deacetylase 6 (HDAC6) is a multidomain cytosolic hydrolase acting mostly on nonhistone protein substrates. Investigations of the substrate specificity HDAC6 are confounded by presence 2 catalytically active domains (DD1 and DD2). In this study, acetylome peptide microarrays libraries were used to map DD1 DD2 human HDAC6. The results show that solely responsible for deacetylation substrates harboring acetyllysine at their C terminus, whereas exclusively deacetylates peptides with an...
Human cathepsin D (CatD), a pepsin-family aspartic protease, plays an important role in tumor progression and metastasis. Here, we report the development of biomimetic inhibitors CatD as novel tools for regulation this therapeutic target. We designed macrocyclic scaffold to mimic spatial conformation minimal pseudo-dipeptide binding motif pepstatin A, microbial oligopeptide inhibitor, active site. A library more than 30 peptidomimetic was employed optimization, mapping subsite interactions,...
The development of highly active and selective enzyme inhibitors is one the priorities medicinal chemistry. Typically, various high-throughput screening methods are used to find lead compounds from a large pool synthetic compounds, these further elaborated structurally refined achieve desired properties. In an effort streamline this complex laborious process, new selection strategies based on different principles have recently emerged as alternative. Herein, we compare three such with aim...
ABSTRACT Fluorescence-based contrast agents enable real-time detection of solid tumors and their neovasculature, making them ideal for use in image-guided surgery. Several have entered late-stage clinical trials or secured FDA approval, suggesting they are likely to become standard care cancer surgeries. One the key parameters optimize agent is molecular size, which dictates much pharmacokinetic pharmacodynamic properties agent. Here, we describe development a class protease-activated...
Fluorescence-based contrast agents enable real-time detection of solid tumors and their neovasculature, making them ideal for use in image-guided surgery. Several have entered late-stage clinical trials or secured FDA approval, suggesting they are likely to become the standard care cancer surgeries. One key parameters optimize is molecular size, which dictates much pharmacokinetic pharmacodynamic properties agent. Here, we describe development a class protease-activated quenched fluorescent...