A quest for connections : ligands for the HCA2, adenosine A3 and GPR88 receptors

Leiden Repository

A quest for connections : ligands for the HCA2, adenosine A3 and GPR88 receptors

Title: A quest for connections : ligands for the HCA2, adenosine A3 and GPR88 receptors
Author: Blad, Clara Catelijne
Publisher: Division of Medicinal Chemistry of the Leiden/Amsterdam Center for Drug Research, Faculty of Science, Leiden University
Issue Date: 2012-11-15
Keywords: Adenosine
Allosteric modulator
Atherosclerosis
G protein-coupled receptor
GPR109A
GPR88
Isopentenyl adenosine
Medicinal chemistry
Nicotinic acid
Orphan receptor
Abstract: In this thesis, several orthosteric and allosteric agonists are presented for the newly discovered hydroxy-carboxylic acid (HCA) receptor 2, and their in vivo activity or in vitro structure-activity relationships are described. The literature on HCA receptors was also thoroughly reviewed, providing some insight into the future of this receptor family as drug targets. The anti-cancer drug N6-(2-isopentenyl)adenosine (IPA) was shown to be a specific ligand for the adenosine A3 receptor, and its antiproliferative effect seems to be mediated by this receptor at low concentrations. A ligand discovery screen for orphan receptor GPR88 was performed, in which over 4000 compounds were tested.
Description: Promotor: Adriaan P. IJzerman
With summary in Dutch
Faculty: Faculteit der Wiskunde en Natuurwetenschappen
Citation: Blad, C.C., 2012, Doctoral thesis, Leiden University
Sponsor: TI-Pharma, project D1-105
Handle: http://hdl.handle.net/1887/20128
 

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application/pdf Title page_Table of contents 212.8Kb View/Open
application/pdf Chapter 1 General introduction 1.445Mb View/Open
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application/pdf Chapter 8 Gener ... on and future perspectives 480.5Kb View/Open
application/pdf Summary 188.3Kb View/Open
application/pdf Summary in Dutch 189.5Kb View/Open
application/pdf Summary for general audience 451.4Kb View/Open
application/pdf Afterword_Curriculum Vitae_List of publications 234.0Kb View/Open
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