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Items: 18


Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2.

Ortiz Zacarías NV, van Veldhoven JPD, Portner L, van Spronsen E, Ullo S, Veenhuizen M, van der Velden WJC, Zweemer AJM, Kreekel RM, Oenema K, Lenselink EB, Heitman LH, IJzerman AP.

J Med Chem. 2018 Oct 25;61(20):9146-9161. doi: 10.1021/acs.jmedchem.8b00605. Epub 2018 Oct 11.


A two-state model for the kinetics of competitive radioligand binding.

Guo D, Peletier LA, Bridge L, Keur W, de Vries H, Zweemer A, Heitman LH, IJzerman AP.

Br J Pharmacol. 2018 May;175(10):1719-1730. doi: 10.1111/bph.14184. Epub 2018 Apr 17.


Apoptotic Bodies Elicit Gas6-Mediated Migration of AXL-Expressing Tumor Cells.

Zweemer AJM, French CB, Mesfin J, Gordonov S, Meyer AS, Lauffenburger DA.

Mol Cancer Res. 2017 Dec;15(12):1656-1666. doi: 10.1158/1541-7786.MCR-17-0012. Epub 2017 Sep 18.


The AXL Receptor is a Sensor of Ligand Spatial Heterogeneity.

Meyer AS, Zweemer AJ, Lauffenburger DA.

Cell Syst. 2015 Jul 29;1(1):25-36.


Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor.

Vilums M, Zweemer AJ, Dilanchian A, van Veldhoven JP, de Vries H, Brussee J, Saunders J, Stamos D, Heitman LH, IJzerman AP.

ChemMedChem. 2015 Jul;10(7):1249-58. doi: 10.1002/cmdc.201500058. Epub 2015 Jun 1.


Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2).

Strunz AK, Zweemer AJ, Weiss C, Schepmann D, Junker A, Heitman LH, Koch M, Wünsch B.

Bioorg Med Chem. 2015 Jul 15;23(14):4034-49. doi: 10.1016/j.bmc.2015.02.019. Epub 2015 Feb 18.


When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists.

Vilums M, Zweemer AJ, Barmare F, van der Gracht AM, Bleeker DC, Yu Z, de Vries H, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, IJzerman AP.

Eur J Med Chem. 2015 Mar 26;93:121-34. doi: 10.1016/j.ejmech.2015.01.063. Epub 2015 Feb 2.


Synthesis, binding affinity and structure-activity relationships of novel, selective and dual targeting CCR2 and CCR5 receptor antagonists.

Junker A, Kokornaczyk AK, Zweemer AJ, Frehland B, Schepmann D, Yamaguchi J, Itami K, Faust A, Hermann S, Wagner S, Schäfers M, Koch M, Weiss C, Heitman LH, Kopka K, Wünsch B.

Org Biomol Chem. 2015 Feb 28;13(8):2407-22. doi: 10.1039/c4ob02397h.


Design and synthesis of novel small molecule CCR2 antagonists: evaluation of 4-aminopiperidine derivatives.

Vilums M, Zweemer AJ, Dekkers S, Askar Y, de Vries H, Saunders J, Stamos D, Brussee J, Heitman LH, IJzerman AP.

Bioorg Med Chem Lett. 2014 Dec 1;24(23):5377-80.


Discovery and mapping of an intracellular antagonist binding site at the chemokine receptor CCR2.

Zweemer AJ, Bunnik J, Veenhuizen M, Miraglia F, Lenselink EB, Vilums M, de Vries H, Gibert A, Thiele S, Rosenkilde MM, IJzerman AP, Heitman LH.

Mol Pharmacol. 2014 Oct;86(4):358-68. doi: 10.1124/mol.114.093328. Epub 2014 Jul 14.


Bias in chemokine receptor signalling.

Zweemer AJ, Toraskar J, Heitman LH, IJzerman AP.

Trends Immunol. 2014 Jun;35(6):243-52. doi: 10.1016/ Epub 2014 Mar 26. Review.


Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.

Vilums M, Zweemer AJ, Yu Z, de Vries H, Hillger JM, Wapenaar H, Bollen IA, Barmare F, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, Ijzerman AP.

J Med Chem. 2013 Oct 10;56(19):7706-14. doi: 10.1021/jm4011737. Epub 2013 Sep 27.


Multiple binding sites for small-molecule antagonists at the CC chemokine receptor 2.

Zweemer AJ, Nederpelt I, Vrieling H, Hafith S, Doornbos ML, de Vries H, Abt J, Gross R, Stamos D, Saunders J, Smit MJ, Ijzerman AP, Heitman LH.

Mol Pharmacol. 2013 Oct;84(4):551-61. doi: 10.1124/mol.113.086850. Epub 2013 Jul 22.


Defining the molecular response to trastuzumab, pertuzumab and combination therapy in ovarian cancer.

Sims AH, Zweemer AJ, Nagumo Y, Faratian D, Muir M, Dodds M, Um I, Kay C, Hasmann M, Harrison DJ, Langdon SP.

Br J Cancer. 2012 May 22;106(11):1779-89. doi: 10.1038/bjc.2012.176. Epub 2012 May 1.


Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers.

Gao ZG, Verzijl D, Zweemer A, Ye K, Göblyös A, Ijzerman AP, Jacobson KA.

Biochem Pharmacol. 2011 Sep 15;82(6):658-68. doi: 10.1016/j.bcp.2011.06.017. Epub 2011 Jun 21.


Trastuzumab and pertuzumab produce changes in morphology and estrogen receptor signaling in ovarian cancer xenografts revealing new treatment strategies.

Faratian D, Zweemer AJ, Nagumo Y, Sims AH, Muir M, Dodds M, Mullen P, Um I, Kay C, Hasmann M, Harrison DJ, Langdon SP.

Clin Cancer Res. 2011 Jul 1;17(13):4451-61. doi: 10.1158/1078-0432.CCR-10-2461. Epub 2011 May 13.


A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.

Heitman LH, Göblyös A, Zweemer AM, Bakker R, Mulder-Krieger T, van Veldhoven JP, de Vries H, Brussee J, Ijzerman AP.

J Med Chem. 2009 Feb 26;52(4):926-31. doi: 10.1021/jm8014052.


False positives in a reporter gene assay: identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase.

Heitman LH, van Veldhoven JP, Zweemer AM, Ye K, Brussee J, IJzerman AP.

J Med Chem. 2008 Aug 14;51(15):4724-9. doi: 10.1021/jm8004509. Epub 2008 Jul 23.


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