Professor Ken Feldman of The Pennsylvania State University is developing efficient methods to prepare human hormone receptor binding agents to serve as potential drug candidates. This project is funded by the Chemical Synthesis program of the Chemistry Division at the National Science Foundation. These methods are based upon preliminary discoveries in Dr. Feldman's laboratory involving new approaches to stitch together small pieces of molecules in order to form larger chemical structures with control over molecular shape. These product molecules will aid in understanding the structural features that contribute to selective association with one hormone receptor over another. The funded research also includes studies on marine water remediation techniques, and the broader impacts of this latter work might include improvements in the quality of husbandry for marine ornamentals.
The chemistry features a new approach to forming indolidenes, reactive indole-derived species that engage in bond formation to append either five-membered rings or seven-membered rings onto the indole framework. Since indoles with appended rings constitute important targets for drug discovery, this chemistry may impact several areas of pharmaceutical science. More specifically, preliminary reports ascribe a remarkable selectivity for activating the human progesterone receptor over other hormone receptors by a five-membered ring appended indole called lecanindole D, a naturally occurring fungal-derived material. The investigation of the structural basis for this selectivity is a major thrust of the funded research.
