• No results found

Cover Page The handle

N/A
N/A
Protected

Academic year: 2021

Share "Cover Page The handle"

Copied!
9
0
0

Bezig met laden.... (Bekijk nu de volledige tekst)

Hele tekst

(1)

Cover Page

The handle http://hdl.handle.net/1887/19038 holds various files of this Leiden University dissertation.

Author: Horst, Eelke van der

Title: Drugs, structures, fragments : substructure-based approaches to GPCR drug discovery and design

Date: 2012-05-31

(2)

Drugs, Structures, Fragments

Substructure-based approaches to GPCR drug discovery and design

(3)
(4)

Drugs, Structures, Fragments

Substructure-based approaches to GPCR drug discovery and design

P ROEFSCHRIFT

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 31 mei 2012

klokke 16:15 uur

door

Eelke van der Horst

geboren te Voorburg in 1976

(5)

Promotiecommissie

Promotor: Prof. Dr. A. P. IJzerman Copromotor: Dr. A. Bender

Overige leden: Prof. Dr. H. van Vlijmen Prof. Dr. T. Hankemeier Prof. Dr. J. de Vlieg Prof. Dr. M. Danhof

.

Cidrux Pharminformatics B.V. is gratefully acknowledged for financially supporting the printing of this thesis.

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). This research was conducted as part of the GPCR forum of the Dutch Top Institute Pharma (project number D1-105).

This thesis was printed by Wöhrmann Print Service (Zutphen, The Netherlands)

(6)

千里之行, 始于足下 Qiān lĭ zhī xíng, shĭ yú zú xià (The journey of a thousand miles begins with a single step)

Lao-tzu, The Way of Lao-tzu Chinese philosopher (604 BC - 531 BC)

(7)
(8)

Contents

7

Contents

Chapter 1. General Introduction 9

Chapter 2. Substructure-Based Approaches to GPCR Drug Discovery and

Design 25

Chapter 3. Substructure Mining of GPCR Ligands Reveals Activity-Class

Specific Functional Groups in an Unbiased Manner 65 Chapter 4. A novel chemogenomics analysis of G protein-coupled

receptors (GPCRs) and their ligands: a potential strategy for

receptor de-orphanization 113

Chapter 5. Substructure-Based Virtual Screening for Adenosine A

2A

Receptor Ligands 145

Chapter 6. Multi-Objective Evolutionary Design of Adenosine Receptor

Ligands 175

Chapter 7. General Conclusion and Perspectives 215

Summary 227

Samenvatting 230

List of publications 235

Curriculum Vitae 237

Nawoord 239

Abbreviations 241

(9)

Referenties

GERELATEERDE DOCUMENTEN

The research described in this thesis was performed at the Division of Analytical Biosciences of the Leiden/Amsterdam Center for Drug Research, Leiden University, the Netherlands,

The studies described in this thesis were performed at the division of Medical Pharmaco- logy of the Leiden / Amsterdam Center for Drug Research and Leiden University Medical

The studies described in the thesis have been performed at the Division of Medical Pharmacology, Leiden/Amsterdam Center for Drug Research (LACDR) and Leiden University Medical

The research described in this thesis was performed at the division of Medical Pharmacology of the Leiden/ Amsterdam Center for Drug Research and the Leiden University Medical

The research described in this thesis was performed at the Division of Analyt- ical Biosciences of the Leiden/Amsterdam Center for Drug Research, Leiden University, Leiden,

The research described in this thesis was performed at the department of Medicinal Chemistry of the Leiden Academic Centre for Drug Research (LACDR), Leiden University (Leiden,

The investigations described in this thesis were performed at the Division of Toxicology of the Leiden/Amsterdam Center for Drug Research, Leiden University, Leiden, The

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,