A5065079184- Phosphodiesterase function and regulation
- Mast cells and histamine
- Click Chemistry and Applications
- Monoclonal and Polyclonal Antibodies Research
- Trypanosoma species research and implications
- Bacterial Genetics and Biotechnology
- RNA and protein synthesis mechanisms
- Research on Leishmaniasis Studies
- Peptidase Inhibition and Analysis
- Food Allergy and Anaphylaxis Research
- Chemical Synthesis and Analysis
- Ocular Surface and Contact Lens
- Oral microbiology and periodontitis research
- Enzyme Structure and Function
- Enzyme Production and Characterization
University of Antwerp
2018-2023
Increased Gram-negative bacteria resistance to antibiotics is becoming a global problem, and new classes of with novel mechanisms action are required. The caseinolytic protease subunit P (ClpP) serine conserved among that considered as an interesting drug target. ClpP function involved in protein turnover homeostasis, stress response, virulence other processes. focus this study was identify inhibitors Escherichia coli understand their mode action. A focused library based on diaryl...
Abstract Dry eye syndrome (DES), a multifactorial disorder which leads to ocular discomfort, visual disturbance and tear film instability, has rising prevalence limited treatment options. In this study, newly developed trypsin-like serine protease inhibitor (UAMC-00050) in drop formulation was evaluated treat inflammation. A surgical animal model of dry employed investigate the potential UAMC-00050 on pathology. Animals treated with displayed significant reduction surface damage after...
Activity-based probes (ABP) are molecules that bind covalently to the active form of an enzyme family, making them attractive tool for target and biomarker identification drug discovery. The present study describes synthesis biochemical characterization novel activity-based targeting trypsin-like serine proteases. We developed extensive library with “clickable” affinity tags a diaryl phosphonate warhead. A wide diversity was achieved by including natural amino acid analogs as well basic...
Human African trypanosomiasis is causing thousands of deaths every year in the rural areas Africa. In this manuscript we describe optimization a family phtalazinone derivatives. Phosphodiesterases have emerged as attractive molecular targets for novel treatment variety neglected parasitic diseases. Compound 1 resulted being potent TbrPDEB1 inhibitor with interesting activity against T. brucei phenotypic screen. Derivative was studied an acute vivo mouse disease model but unfortunately showed...