In vitro screening of steroid 5-alpha reductase inhibitors using purified enzyme and LC-MS/MS quantification
BioNotus offers a contract research service for screening 5-alpha reductase inhibitors using purified human enzyme combined with a validated LC-MS/MS dihydrotestosterone quantification assay. The platform delivers reproducible, high-throughput results in 384-well format for drug discovery and preclinical development programs targeting steroid-related disorders.
Overview
This service provides an integrated in vitro screening platform for identifying and characterizing inhibitors of human steroid 5-alpha reductase, the enzyme responsible for converting testosterone into the more potent androgen dihydrotestosterone (DHT). Inhibition of this enzyme is a validated therapeutic strategy for conditions such as benign prostatic hyperplasia, androgenetic alopecia, and certain hormone-dependent disorders.
BioNotus addresses a longstanding gap in life science research by offering screening with purified, fully characterized 5-alpha reductase enzyme rather than crude cell or tissue homogenates, where enzyme concentration is unknown and inter-experiment comparisons are unreliable. The service combines proprietary enzyme production with a sensitive, in-house LC-MS/MS assay for DHT quantification, delivering high-quality, reproducible data suitable for hit identification, lead optimization, and structure-activity relationship studies.
Technical specifications
- Purified enzyme system: Recombinant expression of full-length wild-type human 5-alpha reductase (type I and type II), optimized for expression efficiency, stabilization, purification, and full biochemical characterization including concentration and activity.
- Validated LC-MS/MS DHT assay: In-house developed and validated liquid chromatography tandem mass spectrometry method for sensitive and selective quantification of dihydrotestosterone, leveraging BioNotus's established expertise in steroid, bile acid, and cholesterol-derived metabolite bioanalysis.
- High-throughput screening format: 384-well plate assay with optimized protocols to minimize reagent consumption while maximizing throughput.
- GLP-certified laboratory: Work performed under Good Laboratory Practice standards to support regulatory-grade data generation.
- Scalable workflow: Enzyme production and screening can be scaled to accommodate varying project sizes and compound library depths.
Technology readiness level
The underlying expression system has been previously validated for multiple proteins widely used in drug discovery and enzyme screening, reducing technical risk for enzyme production. The LC-MS/MS assay development builds directly on BioNotus's established track record with steroid-like analytes. The complete screening workflow, from purified enzyme to high-throughput inhibitor evaluation with quantitative DHT readout, is positioned as a ready-to-engage contract research offering suitable for pharmaceutical, biotech, and academic partners seeking reliable in vitro 5-alpha reductase inhibitor screening.
About BioNotus
BioNotus is a GLP-certified contract research organization based in Niel, Belgium, that specializes in providing integrated solutions for drug discovery and development. Founded in 2017, the company offers a unique, combined portfolio of services encompassing bioanalysis, pharmacometrics, and discovery ADMET profiling. Its laboratory is equipped for LC-MS/MS-based bioanalysis to quantify drugs, metabolites, and biomarkers in diverse biological matrices, while its pharmacometrics division utilizes computational modeling and simulation, including population and physiology-based pharmacokinetic (PBPK) approaches, to guide clinical study design and dosing strategies. By offering both laboratory and consulting capabilities under one roof, BioNotus aims to enhance project efficiency and data-driven decision-making for its clients.
The company serves a wide range of partners, including university hospitals, academic researchers, and small-to-medium-sized pharmaceutical and biotech firms. By converting complex experimental data into actionable insights, BioNotus helps clients navigate regulatory requirements, optimize dosing in special populations, and improve the success rates of preclinical and clinical trials. Their approach emphasizes fit-for-purpose solutions and iterative integration of bioanalytical data with predictive modeling, providing customers with affordable, high-quality support that spans the entire lifecycle of drug development from early discovery stages to late-stage clinical evaluation.
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