Junior Group Leader Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences Prague, Czech Republic
Neurosteroids are endogenous compounds synthesized in the brain. They modulate a variety of ligand-gated ion channels and G protein-coupled receptors. The clinical potential of neurosteroids has been demonstrated by the recent FDA approval of allopregnanolone, ganaxolone and zuranolone. The development of novel neurosteroids offers great potential for the treatment of unmet medical needs such as neuropathic pain, epilepsy, autism spectrum disorder, or depression. However, development is challenging in terms of structural design, synthesis, ADME properties, and bioavailability. Our novel medicinal approach using QSAR models for neurosteroid ligands of ɣ-gamma-aminobutyric acid receptors and (ii) in vitro model using dark quencher probes for the design of novel ligands for G protein-coupled receptors will be presented. Finally, our novel nanoformulation delivery approach will be described.
Learning Objectives:
Upon completion, the participant will understand the difference between steroidal hormones and neurosteroids.
Upon completion, the participant will remember recently FDA approved neurosteroids and their indication.
Upon completion, the participant will be able to discuss the therapeutic potential of neurosteroids and their mechanism of action.
Upon completion, the participant will be able to discuss crucial topics in the development of novel neurosteroids.
