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1

The histamine H3 receptor: from gene cloning to H3 receptor drugs

Leurs, Rob, Bakker, Remko A., Timmerman, Henk, de Esch, Iwan J. P.

Journal:

Nature Reviews Drug Discovery

Année:

2005

Langue:

english

Fichier:

PDF, 317 KB

english, 2005

2

KLIFS: A Knowledge-Based Structural Database To Navigate Kinase–Ligand Interaction Space

van Linden, Oscar P. J., Kooistra, Albert J., Leurs, Rob, de Esch, Iwan J. P., de Graaf, Chris

Journal:

Journal of Medicinal Chemistry

Année:

2014

Langue:

english

Fichier:

PDF, 2.84 MB

english, 2014

3

QUASI: A Novel Method for Simultaneous Superposition of Multiple Flexible Ligands and Virtual Screening Using Partial Similarity

Todorov, Nikolay P., Alberts, Ian L., de Esch, Iwan J. P., Dean, Philip M.

Journal:

Journal of Chemical Information and Modeling

Année:

2007

Langue:

english

Fichier:

PDF, 519 KB

english, 2007

4

Surface plasmon resonance biosensor assay for the analysis of small-molecule inhibitor binding to human and parasitic phosphodiesterases

Siderius, Marco, Shanmugham, Anitha, England, Paul, van der Meer, Tiffany, Bebelman, Jan Paul, Blaazer, Antoni R., de Esch, Iwan J.P., Leurs, Rob

Journal:

Analytical Biochemistry

Année:

2016

Langue:

english

Fichier:

PDF, 1.73 MB

english, 2016

5

A Qualitative Model for the Histamine H3 Receptor Explaining Agonistic and Antagonistic Activity Simultaneously

Iwan J. P. de Esch, Henk Timmerman, Wiro M. P. B. Menge, Paul H. J. Nederkoorn

Journal:

Archiv der Pharmazie

Année:

2000

Langue:

english

Fichier:

PDF, 565 KB

english, 2000

6

Synthesis and Structure-Activity Relationships of 3H-Quinazolin-4-ones and 3H-Pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists

Stefania Storelli, Dennis Verzijl, Jawad Al-Badie, Niels Elders, Leontien Bosch, Henk Timmerman, Martine J. Smit, Iwan J. P. De Esch, Rob Leurs

Journal:

Archiv der Pharmazie

Année:

2007

Langue:

english

Fichier:

PDF, 1.06 MB

english, 2007

7

ChemInform Abstract: Development of a Pharmacophore Model for Histamine H3 Receptor Antagonists, Using the Newly Developed Molecular Modeling Program SLATE.

Iwan J. P. De Esch

Journal:

Année:

2001

Fichier:

PDF, 28 KB

2001

8

A Novel Synthetic Approach Towards 2-Guanidinomethyl-4(5)-sulfamoylimidazoles.

Steve Price, Richard Bull, Sue Cramp, Sophie Gardan, Marco van den Heuvel, David Neighbour, Susan E. Osbourn, Iwan J. P. de Esch, Christoph L. Buenemann

Journal:

Année:

2004

Fichier:

PDF, 24 KB

2004

9

Towards Small-Molecule CXCR3 Ligands with Clinical Potential

Maikel Wijtmans, Dennis Verzijl, Rob Leurs, Iwan J. P. de Esch, Martine J. Smit

Journal:

Année:

2008

Langue:

english

Fichier:

PDF, 539 KB

english, 2008

10

Discovery of a New Class of Non-imidazole Oxazoline-Based Histamine H3 Receptor (H3R) Inverse Agonists

Sylvain Célanire, Maikel Wijtmans, Bernard Christophe, Philippe Collart, Iwan de Esch, Donald Dassesse, Christel Delaunoy, Frédéric Denonne, Véronique Durieu, Edith Gelens, Michel Gillard, Bénédicte L

Journal:

Année:

2009

Langue:

english

Fichier:

PDF, 428 KB

english, 2009

11

New high affinity H3 receptor agonists without a basic side chain

Ruengwit Kitbunnadaj, Marcel Hoffmann, Silvina A. Fratantoni, Gerold Bongers, Remko A. Bakker, Kerstin Wieland, Ahmed el Jilali, Iwan J.P. De Esch, Wiro M.P.B. Menge, Henk Timmerman, Rob Leurs

Journal:

Bioorganic & Medicinal Chemistry

Année:

2005

Langue:

english

Fichier:

PDF, 281 KB

english, 2005

12

Exploring a pocket for polycycloaliphatic groups in the CXCR3 receptor with the aid of a modular synthetic strategy

Maikel Wijtmans, Dennis Verzijl, Cindy M.E. van Dam, Leontien Bosch, Martine J. Smit, Rob Leurs, Iwan J.P. de Esch

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2009

Langue:

english

Fichier:

PDF, 2.66 MB

english, 2009

13

Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28

Janneke W. Hulshof, Henry F. Vischer, Mark H.P. Verheij, Silvina A. Fratantoni, Martine J. Smit, Iwan J.P. de Esch, Rob Leurs

Journal:

Bioorganic & Medicinal Chemistry

Année:

2006

Langue:

english

Fichier:

PDF, 316 KB

english, 2006

14

Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28

Henry F. Vischer, Janneke W. Hulshof, Saskia Hulscher, Silvina A. Fratantoni, Mark H.P. Verheij, Jane Victorina, Martine J. Smit, Iwan J.P. de Esch, Rob Leurs

Journal:

Bioorganic & Medicinal Chemistry

Année:

2010

Langue:

english

Fichier:

PDF, 1.35 MB

english, 2010

15

CXCR3 antagonists: Quaternary ammonium salts equipped with biphenyl- and polycycloaliphatic-anchors

Maikel Wijtmans, Dennis Verzijl, Serge Bergmans, Michael Lai, Leontien Bosch, Martine J. Smit, Iwan J.P. de Esch, Rob Leurs

Journal:

Bioorganic & Medicinal Chemistry

Année:

2011

Langue:

english

Fichier:

PDF, 3.01 MB

english, 2011

16

Structure–activity relationships for the inhibition of recombinant human cytochromes P450 by curcumin analogues

Regina Appiah-Opong, Iwan de Esch, Jan N.M. Commandeur, Mayagustina Andarini, Nico P.E. Vermeulen

Journal:

European Journal of Medicinal Chemistry

Année:

2008

Langue:

english

Fichier:

PDF, 411 KB

english, 2008

17

A novel synthetic approach towards 2-guanidinomethyl-4(5)-sulfamoylimidazoles

Steve Price, Richard Bull, Sue Cramp, Sophie Gardan, Marco van den Heuvel, David Neighbour, Susan E. Osbourn, Iwan J.P. de Esch, Christoph L. Buenemann

Journal:

Tetrahedron Letters

Année:

2004

Langue:

english

Fichier:

PDF, 242 KB

english, 2004

18

Targeted LC–MS derivatization for aldehydes and carboxylic acids with a new derivatization agent 4-APEBA

Mark Eggink, Maikel Wijtmans, Ansgar Kretschmer, Jeroen Kool, Henk Lingeman, Iwan J. P. de Esch, Wilfried M. A. Niessen, Hubertus Irth

Journal:

Analytical and Bioanalytical Chemistry

Année:

2010

Langue:

english

Fichier:

PDF, 497 KB

english, 2010

19

Development of a microfluidic confocal fluorescence detection system for the hyphenation of nano-LC to on-line biochemical assays

Ferry Heus, Martin Giera, Gerdien E. de Kloe, Dick van Iperen, Joost Buijs, Tariq T. Nahar, August B. Smit, Henk Lingeman, Iwan J. P. de Esch, Wilfried M. A. Niessen, Hubertus Irth, Jeroen Kool

Journal:

Analytical and Bioanalytical Chemistry

Année:

2010

Langue:

english

Fichier:

PDF, 468 KB

english, 2010

20

Synthesis and structure–activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists

Nalan Terzioglu, Richard M. van Rijn, Remko A. Bakker, Iwan J.P. De Esch, Rob Leurs

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2004

Langue:

english

Fichier:

PDF, 303 KB

english, 2004

21

Synthesis and structure–activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists

Stefania Storelli, Pauline Verdijk, Dennis Verzijl, Henk Timmerman, Andrea C. van de Stolpe, Cornelis P. Tensen, Martine J. Smit, Iwan J.P. De Esch, Rob Leurs

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2005

Langue:

english

Fichier:

PDF, 214 KB

english, 2005

22

Synthesis and histamine H3 receptor activity of 4-(n-alkyl)-1H-imidazoles and 4-(ω-phenylalkyl)-1H-imidazoles

Iwan J.P De Esch, Aziz Gaffar, Wiro M.P.B Menge, Henk Timmerman

Journal:

Bioorganic & Medicinal Chemistry

Année:

1999

Langue:

english

Fichier:

PDF, 169 KB

english, 1999

23

Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430

Herman D Lim, Maristella Adami, Elena Guaita, Thomas Werfel, Rogier A Smits, Iwan JP De Esch, Remko A Bakker, Ralf Gutzmer, Gabriella Coruzzi, Rob Leurs

Journal:

British Journal of Pharmacology

Année:

2009

Langue:

english

Fichier:

PDF, 759 KB

english, 2009

24

Molecular and biochemical pharmacology of the histamine H4 receptor

Rob Leurs, Paul L Chazot, Fiona C Shenton, Herman D Lim, Iwan JP De Esch

Journal:

British Journal of Pharmacology

Année:

2009

Langue:

english

Fichier:

PDF, 392 KB

english, 2009

25

Strain-dependent effects of the histamine H4 receptor antagonist JNJ7777120 in a murine model of acute skin inflammation

Gabriella Coruzzi, Cristina Pozzoli, Maristella Adami, Daniela Grandi, Nicoletta Guido, Rogier Smits, Iwan de Esch, Rob Leurs

Journal:

Experimental Dermatology

Année:

2012

Langue:

english

Fichier:

PDF, 440 KB

english, 2012

26

A medicinal chemistry perspective on melting point: matched molecular pair analysis of the effects of simple descriptors on the melting point of drug-like compounds

de Graaf, Chris, Berger, Helmut, Mayer, Moriz, Steffen, Andreas, Haaksma, Eric E. J., Schultes, Sabine, de Esch, Iwan J. P., Leurs, Rob, Krämer, Oliver

Journal:

Année:

2012

Langue:

english

Fichier:

PDF, 430 KB

english, 2012

27

Diazepam-bound GABAA receptor models identify new benzodiazepine binding-site ligands

Richter, Lars, de Graaf, Chris, Sieghart, Werner, Varagic, Zdravko, Mörzinger, Martina, de Esch, Iwan J P, Ecker, Gerhard F, Ernst, Margot

Journal:

Nature Chemical Biology

Année:

2012

Langue:

english

Fichier:

PDF, 2.07 MB

english, 2012

28

Acetylcholine binding protein (AChBP) as template for hierarchical in silico screening procedures to identify structurally novel ligands for the nicotinic receptors

Atilla Akdemir, Prakash Rucktooa, Aldo Jongejan, Rene van Elk, Sonia Bertrand, Titia K. Sixma, Daniel Bertrand, August B. Smit, Rob Leurs, Chris de Graaf, Iwan J.P. de Esch

Journal:

Bioorganic & Medicinal Chemistry

Année:

2011

Langue:

english

Fichier:

PDF, 1022 KB

english, 2011

29

Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics

Rogier A. Smits, Herman D. Lim, Tiffany van der Meer, Sebastiaan Kuhne, Karin Bessembinder, Obbe P. Zuiderveld, Maikel Wijtmans, Iwan J.P. de Esch, Rob Leurs

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2012

Langue:

english

Fichier:

PDF, 1.58 MB

english, 2012

30

Structure-based design, synthesis and structure–activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein

Ewald Edink, Atilla Akdemir, Chimed Jansen, René van Elk, Obbe Zuiderveld, Frans J.J. de Kanter, Jacqueline E. van Muijlwijk-Koezen, August B. Smit, Rob Leurs, Iwan J.P. de Esch

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2012

Langue:

english

Fichier:

PDF, 1.42 MB

english, 2012

31

Transforming fragments into candidates: small becomes big in medicinal chemistry

Gerdien E. de Kloe, David Bailey, Rob Leurs, Iwan J.P. de Esch

Journal:

Drug Discovery Today

Année:

2009

Langue:

english

Fichier:

PDF, 1.28 MB

english, 2009

32

Major advances in the development of histamine H4 receptor ligands

Rogier A. Smits, Rob Leurs, Iwan J.P. de Esch

Journal:

Drug Discovery Today

Année:

2009

Langue:

english

Fichier:

PDF, 621 KB

english, 2009

33

Fragment based lead discovery of small molecule inhibitors for the EPHA4 receptor tyrosine kinase

Oscar P.J. van Linden, Carine Farenc, Willem H. Zoutman, Liesbeth Hameetman, Maikel Wijtmans, Rob Leurs, Cornelis P. Tensen, Gregg Siegal, Iwan J.P. de Esch

Journal:

European Journal of Medicinal Chemistry

Année:

2012

Langue:

english

Fichier:

PDF, 1.48 MB

english, 2012

34

Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation

Gabriella Coruzzi, Maristella Adami, Elena Guaita, Iwan J.P. de Esch, Rob Leurs

Journal:

European Journal of Pharmacology

Année:

2007

Langue:

english

Fichier:

PDF, 498 KB

english, 2007

35

Inhibition of brain [3H]cimetidine binding by improgan-like antinociceptive drugs

Rebecca Stadel, Amanda B. Carpenter, Julia W. Nalwalk, Iwan J.P. de Esch, Elwin Janssen, Lindsay B. Hough

Journal:

European Journal of Pharmacology

Année:

2010

Langue:

english

Fichier:

PDF, 250 KB

english, 2010

36

Selective histamine H3 and H4 receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach

Gabriella Coruzzi, Maristella Adami, Cristina Pozzoli, Iwan J.P. de Esch, Rogier Smits, Rob Leurs

Journal:

European Journal of Pharmacology

Année:

2011

Langue:

english

Fichier:

PDF, 600 KB

english, 2011

37

Crystal structure of the EphA4 protein tyrosine kinase domain in the apo- and dasatinib-bound state

Carine Farenc, Patrick H.N. Celie, Cornelis P. Tensen, Iwan J.P. de Esch, Gregg Siegal

Journal:

Année:

2011

Langue:

english

Fichier:

PDF, 1.67 MB

english, 2011

38

Keynote review: Histamine H3 receptor antagonists reach out for the clinic

Sylvain Celanire, Maikel Wijtmans, Patrice Talaga, Rob Leurs, Iwan J.P. de Esch

Journal:

Drug Discovery Today

Année:

2005

Langue:

english

Fichier:

PDF, 353 KB

english, 2005

39

Crystal Structure-Based Virtual Screening for Fragment-like Ligands of the Human Histamine H1 Receptor

Kooistra, Albert J., Vischer, Henry F., Katritch, Vsevolod, Kuijer, Martien, Shiroishi, Mitsunori, Iwata, So, Shimamura, Tatsuro, Stevens, Raymond C., de Esch, Iwan J. P., de Graaf, Chris

Journal:

Journal of Medicinal Chemistry

Année:

2011

Langue:

english

Fichier:

PDF, 4.26 MB

english, 2011

40

Identification of a Novel Scaffold for Allosteric Inhibition of Wild Type and Drug Resistant HIV-1 Reverse Transcriptase by Fragment Library Screening

Geitmann, Matthis, Elinder, Malin, Seeger, Christian, Brandt, Peter, de Esch, Iwan J. P., Danielson, U. Helena

Journal:

Journal of Medicinal Chemistry

Année:

2011

Langue:

english

Fichier:

PDF, 1.51 MB

english, 2011

41

Delineation of Agonist Binding to the Human Histamine H4 Receptor Using Mutational Analysis, Homology Modeling, and ab Initio Calculations

Jongejan, Aldo, Lim, Herman D., Smits, Rogier A., de Esch, Iwan J. P., Haaksma, Eric, Leurs, Rob

Journal:

Journal of Chemical Information and Modeling

Année:

2008

Langue:

english

Fichier:

PDF, 410 KB

english, 2008

42

Design, Synthesis, and Structure–Activity Relationships of Highly Potent 5-HT 3 Receptor Ligands

Verheij, Mark H. P., Thompson, Andrew J., van Muijlwijk-Koezen, Jacqueline E., Lummis, Sarah C. R., Leurs, Rob, de Esch, Iwan J. P.

Journal:

Journal of Medicinal Chemistry

Année:

2012

Langue:

english

Fichier:

PDF, 576 KB

english, 2012

43

Antinociceptive activity of chemical congeners of improgan: Optimization of side chain length leads to the discovery of a new, potent, non-opioid analgesic

Lindsay B. Hough, Iwan J.P. de Esch, Elwin Janssen, James Phillips, Konstantina Svokos, Brian Kern, Jennifer Trachler, Mary E. Abood, Rob Leurs, Julia W. Nalwalk

Journal:

Neuropharmacology

Année:

2006

Langue:

english

Fichier:

PDF, 413 KB

english, 2006

44

Constitutive activity of H3 autoreceptors modulates histamine synthesis in rat brain through the cAMP/PKA pathway

David Moreno-Delgado, Anna Torrent, Jordi Gómez-Ramírez, Iwan de Esch, Isaac Blanco, Jordi Ortiz

Journal:

Neuropharmacology

Année:

2006

Langue:

english

Fichier:

PDF, 302 KB

english, 2006

45

CC12, a high-affinity ligand for [3H]cimetidine binding, is an improgan antagonist

Lindsay B. Hough, Julia W. Nalwalk, James G. Phillips, Brian Kern, Zhixing Shan, Mark P. Wentland, Iwan J.P. de Esch, Elwin Janssen, Travis Barr, Rebecca Stadel

Journal:

Neuropharmacology

Année:

2007

Langue:

english

Fichier:

PDF, 565 KB

english, 2007

46

The histamine H4 receptor as a new therapeutic target for inflammation

Iwan J.P. de Esch, Robin L. Thurmond, Aldo Jongejan, Rob Leurs

Journal:

Trends in Pharmacological Sciences

Année:

2005

Langue:

english

Fichier:

PDF, 333 KB

english, 2005

47

En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family

Rob Leurs, Henry F. Vischer, Maikel Wijtmans, Iwan J.P. de Esch

Journal:

Trends in Pharmacological Sciences

Année:

2011

Langue:

english

Fichier:

PDF, 325 KB

english, 2011

48

Erratum to “En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family” [Trends Pharmacol. Sci. 32 (4) (2011) 250–257]

Rob Leurs, Henry F. Vischer, Maikel Wijtmans, Iwan J.P. de Esch

Journal:

Trends in Pharmacological Sciences

Année:

2012

Langue:

english

Fichier:

PDF, 55 KB

english, 2012

49

Chemical Insights in the Concept of Hybrid Drugs: The Antitumor Effect of Nitric Oxide-Donating Aspirin Involves A Quinone Methide but Not Nitric Oxide nor Aspirin

Hulsman, Niels, Medema, Jan Paul, Bos, Carina, Jongejan, Aldo, Leurs, Rob, Smit, Martine J., de Esch, Iwan J. P., Richel, Dick, Wijtmans, Maikel

Journal:

Journal of Medicinal Chemistry

Année:

2007

Langue:

english

Fichier:

PDF, 396 KB

english, 2007

50

Virtual Fragment Screening: Discovery of Histamine H 3 Receptor Ligands Using Ligand-Based and Protein-Based Molecular Fingerprints

Sirci, Francesco, Istyastono, Enade P., Vischer, Henry F., Kooistra, Albert J., Nijmeijer, Saskia, Kuijer, Martien, Wijtmans, Maikel, Mannhold, Raimund, Leurs, Rob, de Esch, Iwan J. P., de Graaf, Chri

Journal:

Journal of Chemical Information and Modeling

Année:

2012

Langue:

english

Fichier:

PDF, 7.27 MB

english, 2012