Drug-target residence time : a case for the adenosine A1 and A2A receptors

Guo, D. (2014)

Doctoral Thesis

Ligand-receptor binding kinetics is increasingly recognized to play a pivotal role in the early phase of drug design and discovery. In this thesis ligand-receptor binding kinetics, particularly residence time, at the adenosine A1 and A2A receptors was extensively investigated. Several case studies at these two prototypical GPCRs demonstrate that binding kinetics as an emerging paradigm can provide additional information of drug-target interactions at the molecular level. This thesis will contribute to stipulating the importance of kientics-based drug design and discovery in the future.

• Binding kinetics
• Residence time
• GPCR
• Adenosine receptor
• Kinetic assay

• All authors: Guo, D.
• Supervisor: IJzerman, A.P.
• Co-supervisor: Heitman, L.H.
• Committee: Graaf, P.H. van der; Water, B. van de; Danhof, M.; Vauquelin, G.
• Qualification: Doctor (dr.)
• Awarding Institution: Leiden Academic Center for Drug Research (LACDR), Faculty of Science, Leiden University
• Date: 2014-06-25
• ISBN (print): 9789461086976