Semi-high-throughput screening platform for 5 alpha-reductase inhibitors
A screening platform using radio-labeled substrates and HPLC to identify inhibitors of 5 alpha-reductase enzymes (SRD5A1 and SRD5A2). Supports drug discovery for conditions such as benign prostatic hyperplasia, androgenetic alopecia, and androgen-dependent cancers.
Overview
This offering provides a semi-high-throughput in vitro screening platform for identifying inhibitors of 5 alpha-reductase enzymes (SRD5A1 and SRD5A2). The platform leverages radio-labeled substrates combined with HPLC separation and on-line beta-counting to measure enzyme activity and inhibition. It builds on the laboratory's extensive experience in steroid metabolizing enzyme research and inhibitor screening, supporting drug discovery efforts targeting androgen-related conditions such as benign prostatic hyperplasia, androgenetic alopecia, and androgen-dependent cancers including prostate cancer.
Technical specifications
Screening approach:
- Uses tritium-labeled substrates incubated with recombinant SRD5A1 or SRD5A2 protein, test compound, and cofactor
- Substrate and product separation via HPLC with on-line beta-counter and automatic peak integration
- Alternative cell-based format using stable cell lines, enabling simultaneous preliminary in vitro toxicity assessment
- Semi-high-throughput capability through HPLC autosampler, allowing overnight unattended operation
- Applicable to both purified enzyme assays and tissue homogenate or cell line testing
Key advantages:
- Established methodology built on prior validation of HSD17B enzyme screening platforms
- Flexibility to test compounds in both recombinant and cell-based formats
- Potential for parallel toxicity screening in the cell-based configuration
Technology readiness level
The underlying screening methodology has been extensively validated for HSD17B enzyme activity and inhibition in cell lines and tissue homogenates. The proposed extension to SRD5A1 and SRD5A2 builds directly on this proven platform. Future validation will focus on adapting the radio-labeled substrate HPLC approach to recombinant SRD5A proteins and stable cell lines, establishing reproducible screening conditions and compound response profiles. The platform is positioned for collaborative refinement and pilot screening campaigns with industrial partners.
About University of Turku
The University of Turku is a comprehensive public research university in southwest Finland with a broad academic profile. Integration with Turku University Hospital enables co‑located clinical research and national imaging capabilities, including the jointly operated Turku PET Centre. Campus adjacency to Turku Science Park and the Health Campus Turku network links faculty to hundreds of companies and public partners for R&D and scale‑up. Research draws competitive support from the Research Council of Finland, Business Finland and EU programmes, and a dedicated Technology Transfer Office manages IP, licensing and spinouts for partners.
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