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CC chemokine receptor 2 is allosterically modulated by sodium ions and amiloride derivatives through a distinct sodium ion binding site.
den Hollander LS, Zweemer AJM, Béquignon OJM, Hammerl DM, Bleijs BTM, Veenhuizen M, Lantsheer WJF, Chau B, van Westen GJP, IJzerman AP, Heitman LH. den Hollander LS, et al. Among authors: zweemer ajm. Biochem Pharmacol. 2024 Nov;229:116464. doi: 10.1016/j.bcp.2024.116464. Epub 2024 Aug 5. Biochem Pharmacol. 2024. PMID: 39111604
Bias in chemokine receptor signalling.
Zweemer AJ, Toraskar J, Heitman LH, IJzerman AP. Zweemer AJ, et al. Trends Immunol. 2014 Jun;35(6):243-52. doi: 10.1016/j.it.2014.02.004. Epub 2014 Mar 26. Trends Immunol. 2014. PMID: 24679437 Review.
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. Ortiz Zacarías NV, et al. Among authors: zweemer ajm. J Med Chem. 2018 Oct 25;61(20):9146-9161. doi: 10.1021/acs.jmedchem.8b00605. Epub 2018 Oct 11. J Med Chem. 2018. PMID: 30256641 Free PMC article.
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. Vilums M, et al. J Med Chem. 2013 Oct 10;56(19):7706-14. doi: 10.1021/jm4011737. Epub 2013 Sep 27. J Med Chem. 2013. PMID: 24028535
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. Vilums M, et al. Eur J Med Chem. 2015 Mar 26;93:121-34. doi: 10.1016/j.ejmech.2015.01.063. Epub 2015 Feb 2. Eur J Med Chem. 2015. PMID: 25666912
22 results