Project summary
The synthesis and analytical characterization of novel inhibitor candidates are coordinated through the consortium's medicinal chemistry platform. It ensures the continuous synthesis, analytical characterization, and provision of novel low-molecular-weight CatSper and Slo3 inhibitors. The optimisation of these compounds is carried out using computational and structure-based approaches in cooperation with the respective subprojects, based on analyses of structure–activity relationships. The aim is not only to develop CatSper and Slo3 inhibitors for oral or vaginal administration, but also to provide new tools for the structural analysis of CatSper in human sperm.
Workflow for the identification of men with CatSper- or Slo3-related infertility by functional testing and comprehensive phenotypic characterisation (WP1) and exome/genome sequencing to elucidate the genetic/molecular causes (WP2).
Physiological and inhibited sperm ion channel function. From blockade of CatSper and Slo3 ion channels by small molecules preventing the hyperactivated sperm motility to inhibiting the fertilization process and providing contraception.
