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Items: 9

1.

Allosteric modulation of G protein-coupled receptors by amiloride and its derivatives. Perspectives for drug discovery?

Massink A, Amelia T, Karamychev A, IJzerman AP.

Med Res Rev. 2020 Mar;40(2):683-708. doi: 10.1002/med.21633. Epub 2019 Sep 8. Review.

2.

In search of novel ligands using a structure-based approach: a case study on the adenosine A2A receptor.

Lenselink EB, Beuming T, van Veen C, Massink A, Sherman W, van Vlijmen HW, IJzerman AP.

J Comput Aided Mol Des. 2016 Oct;30(10):863-874. Epub 2016 Sep 15.

3.

5'-Substituted Amiloride Derivatives as Allosteric Modulators Binding in the Sodium Ion Pocket of the Adenosine A2A Receptor.

Massink A, Louvel J, Adlere I, van Veen C, Huisman BJ, Dijksteel GS, Guo D, Lenselink EB, Buckley BJ, Matthews H, Ranson M, Kelso M, IJzerman AP.

J Med Chem. 2016 May 26;59(10):4769-77. doi: 10.1021/acs.jmedchem.6b00142. Epub 2016 May 10.

PMID:
27124340
4.

Mass spectrometry-based ligand binding assays on adenosine A1 and A2A receptors.

Massink A, Holzheimer M, Hölscher A, Louvel J, Guo D, Spijksma G, Hankemeier T, IJzerman AP.

Purinergic Signal. 2015 Dec;11(4):581-94. doi: 10.1007/s11302-015-9477-0. Epub 2015 Oct 19.

5.

Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study.

Romagnoli R, Baraldi PG, Lopez-Cara C, Cruz-Lopez O, Moorman AR, Massink A, IJzerman AP, Vincenzi F, Borea PA, Varani K.

Eur J Med Chem. 2015 Aug 28;101:185-204. doi: 10.1016/j.ejmech.2015.06.041. Epub 2015 Jun 24.

PMID:
26141910
6.

Sodium ion binding pocket mutations and adenosine A2A receptor function.

Massink A, Gutiérrez-de-Terán H, Lenselink EB, Ortiz Zacarías NV, Xia L, Heitman LH, Katritch V, Stevens RC, IJzerman AP.

Mol Pharmacol. 2015 Feb;87(2):305-13. doi: 10.1124/mol.114.095737. Epub 2014 Dec 3. Erratum in: Mol Pharmacol. 2019 Apr;95(4):462.

7.

Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene.

Romagnoli R, Baraldi PG, IJzerman AP, Massink A, Cruz-Lopez O, Lopez-Cara LC, Saponaro G, Preti D, Aghazadeh Tabrizi M, Baraldi S, Moorman AR, Vincenzi F, Borea PA, Varani K.

J Med Chem. 2014 Sep 25;57(18):7673-86. doi: 10.1021/jm5008853. Epub 2014 Sep 12.

PMID:
25181013
8.

Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor.

Guo D, Venhorst SN, Massink A, van Veldhoven JP, Vauquelin G, IJzerman AP, Heitman LH.

Br J Pharmacol. 2014 Dec;171(23):5295-312. doi: 10.1111/bph.12836. Epub 2014 Sep 5.

9.

The role of a sodium ion binding site in the allosteric modulation of the A(2A) adenosine G protein-coupled receptor.

Gutiérrez-de-Terán H, Massink A, Rodríguez D, Liu W, Han GW, Joseph JS, Katritch I, Heitman LH, Xia L, Ijzerman AP, Cherezov V, Katritch V, Stevens RC.

Structure. 2013 Dec 3;21(12):2175-85. doi: 10.1016/j.str.2013.09.020. Epub 2013 Nov 7.

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