Publications
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Antiprotozoan lead discovery by aligning dry and wet screening: Prediction, synthesis, and biological assay of novel quinoxalinones KU Leuven
Protozoan parasites have been one of the most significant public health problems for centuries and several human infections caused by them have massive global impact. Most of the current drugs used to treat these illnesses have been used for decades and have many limitations such as the emergence of drug resistance, severe side-effects, low-to-medium drug efficacy, administration routes, cost, etc. These drugs have been largely neglected as ...
Biological Assay to Determine Gonadotropin Potency: From In Vivo to In Vitro Sustainable Method KU Leuven
Various preparations of follicle-stimulating hormone (FSH) are commercially available; however, they differ in glycoforms composition and purity owing to their respective sources. Additional chemical/physical changes can also be introduced during manufacturing and can impact their biological activity (biopotency), which is routinely assessed using an in vivo bioassay (Steelman-Pohley). This study aimed to determine whether an in vitro bioassay ...
Synthesis and biological evaluation of tamoxifen fusion compounds for the optimization of MASPIT, a three-hybrid target deconvolution assay Ghent University
Synthesis and biological evaluation of small-molecule fusion compounds for the optimization of MASPIT, a three-hybrid target deconvolution assay Ghent University
Design, synthesis and biological evaluation of tamoxifen-fusion compounds for the optimization of MASPIT, a three-hybrid target deconvolution assay Ghent University
An in-vitro assay using human spermatozoa to detect toxicity of biologically active substances Ghent University
Identifying the key toxic players within an in-vivo toxic syndrome is crucial to develop targeted therapies. Here, we established a novel method that characterizes the effect of single substances by means of an ex-vivo incubation set-up. We found that primary human spermatozoa elicit a distinct motile response on a (uremic) toxic milieu. Specifically, this approach describes the influence of a bulk toxic environment (uremia) as well as single ...
Activity-based reporter assays for the screening of abused substances in biological matrices Ghent University
Repurposing High-Throughput Image Assays Enables Biological Activity Prediction for Drug Discovery KU Leuven
In both academia and the pharmaceutical industry, large-scale assays for drug discovery are expensive and often impractical, particularly for the increasingly important physiologically relevant model systems that require primary cells, organoids, whole organisms, or expensive or rare reagents. We hypothesized that data from a single high-throughput imaging assay can be repurposed to predict the biological activity of compounds in other assays, ...
Method comparison of dipeptidyl peptidase IV activity assays and their application in biological samples containing reversible inhibitors University of Antwerp
Background Dipeptidyl peptidase IV (DPPIV, DPP4) is a serine protease that releases N-terminal dipeptides. It is a validated drug target for type 2 diabetes and DPPIV inhibitors are currently evaluated for other therapeutic applications. Various assays are used for DPPIV activity measurements in biological samples. Highly sensitive methods are needed to measure also very low activities in inhibited samples. Methods Here, the three most ...