A phenotypic screening platform utilising human spermatozoa identifies new compounds with contraceptive activity [article]

Christopher LR Barratt, Paul Andrews, Franz Gruber
2019 bioRxiv   pre-print
There is an urgent need to develop new methods for male contraception, however a major barrier to drug discovery has been the lack of validated targets and the absence of an effective high-throughput phenotypic screening system. To address this deficit, we developed a fully-automated robotic screening platform that provided quantitative evaluation of compound activity against two key attributes of human sperm function: motility and acrosome reaction. In order to accelerate contraceptive
more » ... ent, we screened the comprehensive collection of 12,000 molecules that make up the ReFRAME repurposing library, comprising nearly all the small molecules that have been approved or have undergone clinical development, or have significant preclinical profiling. We identified compounds that potently inhibit motility representing either novel drug candidates or routes to target identification. This platform will allow for major drug discovery programmes that address the critical gap in the contraceptive portfolio as well as uncover novel human sperm biology.
doi:10.1101/808105 fatcat:46abz77afbejlb3wkmetyxpheq