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The handle http://hdl.handle.net/1887/20128 holds various files of this Leiden University dissertation.
Author: Blad, Clara Catelijne
Title: A quest for connections : ligands for the HCA2, adenosine A3 and GPR88 receptors
Date: 2012-11-15
A quest for connections
ligands for the HCA
2,
adenosine A
3and GPR88 receptor s
Clara C. Blad
A quest for connections
ligands for the HCA
2,
adenosine A
3and GPR88 receptors
Proefschrift
ter verkrijging van
de graad van Doctor aan de Universiteit Leiden,
op gezag van Rector Magnificus prof. mr. P.F. van der Heijden, volgens besluit van het College voor Promoties
te verdedigen op donderdag 15 november 2012 klokke 13.45 uur
door
Clara Catelijne Blad geboren te Rotterdam
in 1982
Promotiecommissie Promotor: Prof. Dr. Adriaan P. IJzerman Overige leden: Prof. Dr. Theo J. van Berkel
Prof. Dr. Meindert Danhof Prof. Dr. Johan Kuiper Prof. Dr. Stefan Offermanns
The research described in this thesis was performed at the Division of Medicinal Chemistry of the Leiden/Amsterdam Center for Drug Research, Leiden University, Leiden, the Netherlands and at the Institut de Biologie Moléculaire et Cellulaire, Illkirch, France. The research performed in the Netherlands has been financially supported by TI Pharma (project number D1-105).
This thesis was printed by Wöhrmann Print Service (Zutphen, The Netherlands)
Table of contents
1. General introduction 9
2. Biological and pharmacological roles of hydroxy- carboxylic acid (HCA) receptors
35 3. Effects of pyrazole partial agonists on HCA2-mediated
flushing and VLDL-triglyceride levels in mice
63 4. Structure-activity relationships of trans-substituted-
propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A)
77 5. Novel 3,6,7-substituted pyrazolopyrimidines as positive
allosteric modulators for the hydroxy-carboxylic acid receptor 2 (GPR109A)
85 6. Putative role of the adenosine A3 receptor in the
antiproliferative action of N6-(2-isopentenyl)adenosine 7. Compound screen on orphan G protein-coupled receptor 101
GPR88
119 8. General discussion, future perspectives and conclusion 135
Summary 147
Samenvatting 151
Samenvatting voor algemeen publiek 155
Nawoord 159
Curriculum vitae 161
List of publications 163
