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Items: 26

1.

BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis.

Sanderson MP, Apgar J, Garin-Chesa P, Hofmann MH, Kessler D, Quant J, Savchenko A, Schaaf O, Treu M, Tye H, Zahn SK, Zoephel A, Haaksma E, Adolf GR, Kraut N.

Mol Cancer Ther. 2015 Dec;14(12):2762-72. doi: 10.1158/1535-7163.MCT-15-0539. Epub 2015 Oct 5.

2.

Combinatorial Consensus Scoring for Ligand-Based Virtual Fragment Screening: A Comparative Case Study for Serotonin 5-HT(3)A, Histamine H(1), and Histamine H(4) Receptors.

Schultes S, Kooistra AJ, Vischer HF, Nijmeijer S, Haaksma EE, Leurs R, de Esch IJ, de Graaf C.

J Chem Inf Model. 2015 May 26;55(5):1030-44. doi: 10.1021/ci500694c. Epub 2015 Apr 23.

PMID:
25815783
3.

Bispyrimidines as potent histamine H(4) receptor ligands: delineation of structure-activity relationships and detailed H(4) receptor binding mode.

Engelhardt H, Schultes S, de Graaf C, Nijmeijer S, Vischer HF, Zuiderveld OP, Dobler J, Stachurski K, Mayer M, Arnhof H, Scharn D, Haaksma EE, de Esch IJ, Leurs R.

J Med Chem. 2013 Jun 13;56(11):4264-76. doi: 10.1021/jm301886t. Epub 2013 May 28.

PMID:
23668417
4.

Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor.

Nijmeijer S, Engelhardt H, Schultes S, van de Stolpe AC, Lusink V, de Graaf C, Wijtmans M, Haaksma EE, de Esch IJ, Stachurski K, Vischer HF, Leurs R.

Br J Pharmacol. 2013 Sep;170(1):89-100. doi: 10.1111/bph.12113.

5.

Combining quantum mechanical ligand conformation analysis and protein modeling to elucidate GPCR-ligand binding modes.

Schultes S, Engelhardt H, Roumen L, Zuiderveld OP, Haaksma EE, de Esch IJ, Leurs R, de Graaf C.

ChemMedChem. 2013 Jan;8(1):49-53. doi: 10.1002/cmdc.201200412. Epub 2012 Nov 19.

PMID:
23161844
6.

Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker.

Solca F, Dahl G, Zoephel A, Bader G, Sanderson M, Klein C, Kraemer O, Himmelsbach F, Haaksma E, Adolf GR.

J Pharmacol Exp Ther. 2012 Nov;343(2):342-50. doi: 10.1124/jpet.112.197756. Epub 2012 Aug 10.

PMID:
22888144
7.

Detailed structure-activity relationship of indolecarboxamides as H4 receptor ligands.

Engelhardt H, de Esch IJ, Kuhn D, Smits RA, Zuiderveld OP, Dobler J, Mayer M, Lips S, Arnhof H, Scharn D, Haaksma EE, Leurs R.

Eur J Med Chem. 2012 Aug;54:660-8. doi: 10.1016/j.ejmech.2012.06.016. Epub 2012 Jun 18.

PMID:
22749391
8.

Ensemble Rule-Based Classification of Substrates of the Human ABC-Transporter ABCB1 Using Simple Physicochemical Descriptors.

Demel MA, Kraemer O, Ettmayer P, Haaksma E, Ecker GF.

Mol Inform. 2010 Mar 15;29(3):233-42. doi: 10.1002/minf.200900079. Epub 2010 Mar 9.

PMID:
27462766
9.

Predicting ligand interactions with ABC transporters in ADME.

Demel MA, Krämer O, Ettmayer P, Haaksma EE, Ecker GF.

Chem Biodivers. 2009 Nov;6(11):1960-9. doi: 10.1002/cbdv.200900138. Review.

PMID:
19937827
10.

A new generation of anti-histamines: Histamine H4 receptor antagonists on their way to the clinic.

Engelhardt H, Smits RA, Leurs R, Haaksma E, de Esch IJ.

Curr Opin Drug Discov Devel. 2009 Sep;12(5):628-43. Review.

PMID:
19736622
11.

Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.

Lim HD, Istyastono EP, van de Stolpe A, Romeo G, Gobbi S, Schepers M, Lahaye R, Menge WM, Zuiderveld OP, Jongejan A, Smits RA, Bakker RA, Haaksma EE, Leurs R, de Esch IJ.

Bioorg Med Chem. 2009 Jun 1;17(11):3987-94. doi: 10.1016/j.bmc.2009.04.007. Epub 2009 Apr 11.

PMID:
19414267
12.

Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.

Smits RA, de Esch IJ, Zuiderveld OP, Broeker J, Sansuk K, Guaita E, Coruzzi G, Adami M, Haaksma E, Leurs R.

J Med Chem. 2008 Dec 25;51(24):7855-65. doi: 10.1021/jm800876b.

PMID:
19053770
13.

In silico prediction of substrate properties for ABC-multidrug transporters.

Demel MA, Schwaha R, Krämer O, Ettmayer P, Haaksma EE, Ecker GF.

Expert Opin Drug Metab Toxicol. 2008 Sep;4(9):1167-80. doi: 10.1517/17425255.4.9.1167 . Review.

PMID:
18721111
14.

Phenylalanine 169 in the second extracellular loop of the human histamine H4 receptor is responsible for the difference in agonist binding between human and mouse H4 receptors.

Lim HD, Jongejan A, Bakker RA, Haaksma E, de Esch IJ, Leurs R.

J Pharmacol Exp Ther. 2008 Oct;327(1):88-96. doi: 10.1124/jpet.108.140343. Epub 2008 Jul 17.

PMID:
18635748
15.

Delineation of agonist binding to the human histamine H4 receptor using mutational analysis, homology modeling, and ab initio calculations.

Jongejan A, Lim HD, Smits RA, de Esch IJ, Haaksma E, Leurs R.

J Chem Inf Model. 2008 Jul;48(7):1455-63. doi: 10.1021/ci700474a. Epub 2008 Jun 14.

PMID:
18553960
16.

Linking agonist binding to histamine H1 receptor activation.

Jongejan A, Bruysters M, Ballesteros JA, Haaksma E, Bakker RA, Pardo L, Leurs R.

Nat Chem Biol. 2005 Jul;1(2):98-103. Epub 2005 Jun 19.

PMID:
16408006
17.

Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.

Ries UJ, Priepke HW, Hauel NH, Haaksma EE, Stassen JM, Wienen W, Nar H.

Bioorg Med Chem Lett. 2003 Jul 21;13(14):2291-5.

PMID:
12824020
18.

Serine and threonine residues bend alpha-helices in the chi(1) = g(-) conformation.

Ballesteros JA, Deupi X, Olivella M, Haaksma EE, Pardo L.

Biophys J. 2000 Nov;79(5):2754-60.

19.

GRID/CPCA: a new computational tool to design selective ligands.

Kastenholz MA, Pastor M, Cruciani G, Haaksma EE, Fox T.

J Med Chem. 2000 Aug 10;43(16):3033-44.

PMID:
10956211
20.

Factor Xa: simulation studies with an eye to inhibitor design.

Daura X, Haaksma E, van Gunsteren WF.

J Comput Aided Mol Des. 2000 Aug;14(6):507-29.

PMID:
10921769
21.
22.

A theoretical study concerning the mode of interaction of the histamine H2-agonist dimaprit.

Haaksma EE, Donné-Op den Kelder GM, Vernooijs P, Timmerman H.

J Mol Graph. 1992 Jun;10(2):79-87.

PMID:
1386250
23.

Theoretical analysis of the activity of dimaprit derivatives on the H2-receptor.

Haaksma EE, Donné- op den Kelder GM, Timmerman H, Weinstein H.

Agents Actions Suppl. 1991;33:315-24. No abstract available.

PMID:
1647130
24.

Histamine receptors: subclasses and specific ligands.

Haaksma EE, Leurs R, Timmerman H.

Pharmacol Ther. 1990;47(1):73-104. Review.

PMID:
2195558
25.

Comparison of the interaction of the histamine H2-agonists [correction of H2-antagonists] histamine and dimaprit.

Haaksma EE, Donné-Op den Kelder GM, Timmerman H, Vernooijs P, Ravenek W.

Prog Clin Biol Res. 1989;289:361-70. No abstract available.

PMID:
2524839
26.

Studies on the active molecular species of the H2 receptor antagonists cimetidine and mifentidine.

Haaksma EE, Rademaker B, Kramer K, Eriks JC, Bast A, Timmerman H.

J Med Chem. 1987 Jan;30(1):208-11.

PMID:
3806596

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