Cover Page
The handle http://hdl.handle.net/1887/81190 holds various files of this Leiden University dissertation.
Author: Yang, X.
Title: To bind or not to bind, that is an important question! : Development of covalent probes for adenosine receptors
To bind or not to bind,
that is an important question!
Development of covalent probes for adenosine receptors
The research described in this thesis was performed at the Division of Drug Discovery and Safety of the Leiden Academic Centre for Drug Research (LACDR), Leiden University (Leiden, The Netherlands). Printing of the thesis was financially supported by LACDR, Leiden University.
Cover design: Zhuoqun Hou Thesis lay-out: Xue Yang
Printing: Ridderprint BV | www.ridderprint.nl ISBN: 978-94-6375-676-1
© Copyright, Xue Yang, 2019
To bind or not to bind,
that is an important question!
Development of covalent probes for adenosine receptors
Proefschrift
ter verkrijging van
de graad van Doctor aan de Universiteit Leiden, op gezag van Rector Magnificus prof.mr. C.J.J.M. Stolker,
volgens besluit van het College voor Promoties te verdedigen op woensdag 4 december 2019
klokke 10.00uur
door
Xue Yang
Promotores: Prof. dr. Ad IJzerman Dr. Laura Heitman
Co-promotores: Dr. Julien Louvel (until June 2016) Dr. Daan van der Es (from June 2016)
Promotiecommissie: Prof. dr. Hubertus Irth (voorzitter) Prof. dr. Joke Bouwstra (secretaris) Prof. dr. Mario van der Stelt
Contents
Chapter 1 General Introduction ... 7
Chapter 2 Molecular Probes for the Human Adenosine Receptors ... 19
Chapter 3 A Covalent Antagonist for the Human Adenosine A2A Receptor ... 57
Chapter 4 Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A3 Receptor ... 79
Chapter 5 Design, Synthesis and Pharmacological Profiles of LUF7746, A Novel Covalent Partial Agonist for the Adenosine A1 Receptor ... 113
Chapter 6 An Affinity-based Probe for the human Adenosine A2A Receptor ... 141
Chapter 7 Conclusions and Future Perspectives ... 167
Summary ... 181
Samenvatting ... 185
List of publications ... 189
Curriculum Vitae ... 191
6
