Heitman LH - Search Results

1

Cannabinoid CB₂ receptor ligand profiling reveals biased signalling and off-target activity.

Soethoudt M, Grether U, Fingerle J, Grim TW, Fezza F, de Petrocellis L, Ullmer C, Rothenhäusler B, Perret C, van Gils N, Finlay D, MacDonald C, Chicca A, Gens MD, Stuart J, de Vries H, Mastrangelo N, Xia L, Alachouzos G, Baggelaar MP, Martella A, Mock ED, Deng H, Heitman LH, Connor M, Di Marzo V, Gertsch J, Lichtman AH, Maccarrone M, Pacher P, Glass M, van der Stelt M. Soethoudt M, et al. Among authors: heitman lh. Nat Commun. 2017 Jan 3;8:13958. doi: 10.1038/ncomms13958. Nat Commun. 2017. PMID: 28045021 Free PMC article.

2

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. Heitman LH, et al. J Med Chem. 2009 Feb 26;52(4):926-31. doi: 10.1021/jm8014052. J Med Chem. 2009. PMID: 19161279

3

Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor.

Heitman LH, Narlawar R, de Vries H, Willemsen MN, Wolfram D, Brussee J, Ijzerman AP. Heitman LH, et al. J Med Chem. 2009 Apr 9;52(7):2036-42. doi: 10.1021/jm801561h. J Med Chem. 2009. PMID: 19296599

4

Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics.

Guo D, van Dorp EJ, Mulder-Krieger T, van Veldhoven JP, Brussee J, Ijzerman AP, Heitman LH. Guo D, et al. Among authors: heitman lh. J Biomol Screen. 2013 Mar;18(3):309-20. doi: 10.1177/1087057112464776. Epub 2012 Oct 23. J Biomol Screen. 2013. PMID: 23093571

5

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. Zweemer AJ, et al. Among authors: heitman lh. Mol Pharmacol. 2013 Oct;84(4):551-61. doi: 10.1124/mol.113.086850. Epub 2013 Jul 22. Mol Pharmacol. 2013. PMID: 23877010

6

Binding kinetics of ZM241385 derivatives at the human adenosine A2A receptor.

Guo D, Xia L, van Veldhoven JP, Hazeu M, Mocking T, Brussee J, Ijzerman AP, Heitman LH. Guo D, et al. Among authors: heitman lh. ChemMedChem. 2014 Apr;9(4):752-61. doi: 10.1002/cmdc.201300474. Epub 2014 Mar 3. ChemMedChem. 2014. PMID: 24591302

7

Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines.

Louvel J, Guo D, Agliardi M, Mocking TA, Kars R, Pham TP, Xia L, de Vries H, Brussee J, Heitman LH, Ijzerman AP. Louvel J, et al. Among authors: heitman lh. J Med Chem. 2014 Apr 24;57(8):3213-22. doi: 10.1021/jm401643m. Epub 2014 Apr 3. J Med Chem. 2014. PMID: 24669958

8

Bias in chemokine receptor signalling.

Zweemer AJ, Toraskar J, Heitman LH, IJzerman AP. Zweemer AJ, et al. Among authors: heitman lh. 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.

9

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. Zweemer AJ, et al. Among authors: heitman lh. Mol Pharmacol. 2014 Oct;86(4):358-68. doi: 10.1124/mol.114.093328. Epub 2014 Jul 14. Mol Pharmacol. 2014. PMID: 25024169

10

Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.

Louvel J, Guo D, Soethoudt M, Mocking TA, Lenselink EB, Mulder-Krieger T, Heitman LH, IJzerman AP. Louvel J, et al. Among authors: heitman lh. Eur J Med Chem. 2015 Aug 28;101:681-91. doi: 10.1016/j.ejmech.2015.07.023. Epub 2015 Jul 15. Eur J Med Chem. 2015. PMID: 26210506

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