Heitman LH - Search Results

1

3DDPDs: describing protein dynamics for proteochemometric bioactivity prediction. A case for (mutant) G protein-coupled receptors.

Gorostiola González M, van den Broek RL, Braun TGM, Chatzopoulou M, Jespers W, IJzerman AP, Heitman LH, van Westen GJP. Gorostiola González M, et al. Among authors: heitman lh. J Cheminform. 2023 Aug 28;15(1):74. doi: 10.1186/s13321-023-00745-5. J Cheminform. 2023. PMID: 37641107 Free PMC article.

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. Junker A, et al. Among authors: heitman lh. Org Biomol Chem. 2015 Feb 28;13(8):2407-22. doi: 10.1039/c4ob02397h. Org Biomol Chem. 2015. PMID: 25566983

3

The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity.

Mukhopadhyay P, Baggelaar M, Erdelyi K, Cao Z, Cinar R, Fezza F, Ignatowska-Janlowska B, Wilkerson J, van Gils N, Hansen T, Ruben M, Soethoudt M, Heitman L, Kunos G, Maccarrone M, Lichtman A, Pacher P, Van der Stelt M. Mukhopadhyay P, et al. Br J Pharmacol. 2016 Feb;173(3):446-58. doi: 10.1111/bph.13338. Epub 2016 Jan 15. Br J Pharmacol. 2016. PMID: 26398481 Free PMC article.

4

Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core.

Bonger KM, van den Berg RJ, Knijnenburg AD, Heitman LH, Ijzerman AP, Oosterom J, Timmers CM, Overkleeft HS, van der Marel GA. Bonger KM, et al. Among authors: heitman lh. Bioorg Med Chem. 2008 Apr 1;16(7):3744-58. doi: 10.1016/j.bmc.2008.01.054. Epub 2008 Feb 2. Bioorg Med Chem. 2008. PMID: 18282756

5

Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors.

van den Nieuwendijk AM, Pietra D, Heitman L, Göblyös A, IJzerman AP. van den Nieuwendijk AM, et al. J Med Chem. 2004 Jan 29;47(3):663-72. doi: 10.1021/jm030863d. J Med Chem. 2004. PMID: 14736246

6

Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist.

Heitman LH, Mulder-Krieger T, Spanjersberg RF, von Frijtag Drabbe Künzel JK, Dalpiaz A, IJzerman AP. Heitman LH, et al. Br J Pharmacol. 2006 Mar;147(5):533-41. doi: 10.1038/sj.bjp.0706655. Br J Pharmacol. 2006. PMID: 16444290 Free PMC article.

7

[3H]Org 43553, the first low-molecular-weight agonistic and allosteric radioligand for the human luteinizing hormone receptor.

Heitman LH, Oosterom J, Bonger KM, Timmers CM, Wiegerinck PH, Ijzerman AP. Heitman LH, et al. Mol Pharmacol. 2008 Feb;73(2):518-24. doi: 10.1124/mol.107.039875. Epub 2007 Nov 7. Mol Pharmacol. 2008. PMID: 17989351

8

Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor.

Heitman LH, Ye K, Oosterom J, Ijzerman AP. Heitman LH, et al. Mol Pharmacol. 2008 Jun;73(6):1808-15. doi: 10.1124/mol.107.043521. Epub 2008 Mar 14. Mol Pharmacol. 2008. PMID: 18344315

9

G protein-coupled receptors of the hypothalamic-pituitary-gonadal axis: a case for Gnrh, LH, FSH, and GPR54 receptor ligands.

Heitman LH, Ijzerman AP. Heitman LH, et al. Med Res Rev. 2008 Nov;28(6):975-1011. doi: 10.1002/med.20129. Med Res Rev. 2008. PMID: 18561294 Review.

10

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. Heitman LH, et al. J Med Chem. 2008 Aug 14;51(15):4724-9. doi: 10.1021/jm8004509. Epub 2008 Jul 23. J Med Chem. 2008. PMID: 18646744

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