This seminar will describe how neuroactive peptides are converted into drug-like compounds. To accelerate discovery and optimization of analgesic conotoxins, I will present efforts to improve oxidative folding of disulfide-rich peptides using selenocysteines. To deliver neuroactive peptides into the brain, I will present studies on engineering galanin analogs that suppress seizures and are currently in preclinical development for the treatment of epilepsy.