Research

Novel Ligands for GPCRs

This is a collaborative project where new ligands for GPCRs are designed and optimized using the molecular modeling of the group of Dr. Patricia Reggio at UNCG. Targeted libraries of compounds are then synthesized in my group. The syntheses are designed to be convergent so that a large number of analogs can be synthesized in a minimal number of steps. The compounds are then sent to Temple University where the groupof Dr. Mary Abood determines their ability to agonize or antagonize the different GPCRs. This information is then used to modify the modeling data which enables the iterative optimization cycle to continue. Funding for this project has been provided by the National Institute of Health in the form of R01 (DA023204) and an R21 (NS077347) grants. This support is gratefully acknowledged.

Selected Publications:

“Identification of the GPR55 Antagonist Binding Site Using a Novel Set of High-Potency GPR55 Selective Ligands”
Evangelia Kotsikorou, Haleli Sharir, Derek M Shore, Dow P. Hurst, Diane L. Lynch, Karla E. Madrigal, Susanne Heynen-Genel, Loribelle B. Milan, Thomas D.Y. Chung, Herbert H. Seltzman, Yushi Bai, Marc G. Caron, Lawrence S. Barak, Mitchell P Croatt, Mary E Abood, and Patricia H. Reggio
Biochemistry 2013, 52, 9456-9469.
http://pubs.acs.org/doi/abs/10.1021/bi4008885