Liapakis George, PhD

Assistant Professor

Dept. of Pharmacology

Faculty of Medicine

University of Crete



Research Interests

My scientific interests are focused on elucidating the mode of ligand interaction with the G-protein coupled receptors (GPCRs) and particularly the beta-adrenergic and the corticotropin releasing factor (CRF) receptors, which bind the small catecholamines and the larger CRF analogues, respectively. Furthermore, I am interested in studying the activation-associated conformational changes in both receptors, including the structural changes in their intracellular loops that are responsible for their interaction with and activation of G-proteins. These studies will provide us with the information that might put the basis for the rational design of receptor-selective compounds with predetermined efficacy, among them proteolytically stable non-peptide agonists and/or antagonists.


Representative publications:

1.                  Shi L., Liapakis G, Xu R, Guarnieri F, Ballesteros JA, Javitch JA. (2002). [Shi and Liapakis contributed equally to this work]. Beta2 adrenergic receptor activation. Modulation of the proline kink in transmembrane 6 by a rotamer toggle switch. J Biol Chem., 277(43): 40989-40996

2.                  Liapakis G., Chan W.C., Papadokostaki M. and Javitch J.A. (2004). Synergistic Contributions of the Functional Groups of Epinephrine to its Affinity and Efficacy at the β2 Adrenergic Receptor. Mol Pharmacol., 65(5): 1181-1190

3.                  Gkountelias K., Tselios T., Venihaki M., Deraos G., Lazaridis I., Rassouli O., Gravanis A., Liapakis G. (2009). Alanine scanning mutagenesis of the second extracellular loop of type 1 corticotropin releasing factor receptor revealed residues critical for peptide binding. Mol. Pharmacol, 75:793800

4.                  Gkountelias K., Papadokostaki M., Javitch J.A., and Liapakis G. (2010). Exploring the binding site crevice of a family B GPCR, the type 1 corticotropin releasing factor receptor. Mol Pharmacol 78:785793

5.                  Rassouli O., Liapakis G., Lazaridis I., Sakellaris G., Gkountelias K., Gravanis A., Margioris A.N., Karalis K.P., Venihaki M. (2011). A novel role of peripheral corticotropin-releasing hormone (CRH) on dermal fibroblasts. PLoS One. 6(7):e21654. Epub 2011 Jul 13

6.                  Liapakis G., Venihaki M., Margioris A., Grigoriadis D., Gkountelias K. (2011). Members of CRF Family and their Receptors: From Past to Future. Curr Med Chem.; 18(17): 2583-600