Smits RA - Search Results

1

Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.

Smits RA, Lim HD, Hanzer A, Zuiderveld OP, Guaita E, Adami M, Coruzzi G, Leurs R, de Esch IJ. Smits RA, et al. J Med Chem. 2008 Apr 24;51(8):2457-67. doi: 10.1021/jm7014217. Epub 2008 Mar 22. J Med Chem. 2008. PMID: 18357976

2

Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.

Smits RA, Lim HD, Stegink B, Bakker RA, de Esch IJ, Leurs R. Smits RA, et al. J Med Chem. 2006 Jul 27;49(15):4512-6. doi: 10.1021/jm051008s. J Med Chem. 2006. PMID: 16854056

3

The emerging role of the histamine H4 receptor in anti-inflammatory therapy.

Lim HD, Smits RA, Leurs R, De Esch IJ. Lim HD, et al. Among authors: smits ra. Curr Top Med Chem. 2006;6(13):1365-73. doi: 10.2174/15680266106061365. Curr Top Med Chem. 2006. PMID: 16918455 Review.

4

Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.

Lim HD, Smits RA, Bakker RA, van Dam CM, de Esch IJ, Leurs R. Lim HD, et al. Among authors: smits ra. J Med Chem. 2006 Nov 16;49(23):6650-1. doi: 10.1021/jm060880d. J Med Chem. 2006. PMID: 17154494

5

Delineation of agonist binding to the human histamine H4 receptor using mutational analysis, homology modeling, and ab initio calculations.

Jongejan A, Lim HD, Smits RA, de Esch IJ, Haaksma E, Leurs R. Jongejan A, et al. Among authors: smits ra. J Chem Inf Model. 2008 Jul;48(7):1455-63. doi: 10.1021/ci700474a. Epub 2008 Jun 14. J Chem Inf Model. 2008. PMID: 18553960

6

Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.

Smits RA, de Esch IJ, Zuiderveld OP, Broeker J, Sansuk K, Guaita E, Coruzzi G, Adami M, Haaksma E, Leurs R. Smits RA, et al. J Med Chem. 2008 Dec 25;51(24):7855-65. doi: 10.1021/jm800876b. J Med Chem. 2008. PMID: 19053770

7

Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430.

Lim HD, Adami M, Guaita E, Werfel T, Smits RA, de Esch IJ, Bakker RA, Gutzmer R, Coruzzi G, Leurs R. Lim HD, et al. Among authors: smits ra. Br J Pharmacol. 2009 May;157(1):34-43. doi: 10.1111/j.1476-5381.2009.00200.x. Br J Pharmacol. 2009. PMID: 19413569 Free PMC article.

8

Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.

Lim HD, Istyastono EP, van de Stolpe A, Romeo G, Gobbi S, Schepers M, Lahaye R, Menge WM, Zuiderveld OP, Jongejan A, Smits RA, Bakker RA, Haaksma EE, Leurs R, de Esch IJ. Lim HD, et al. Among authors: smits ra. Bioorg Med Chem. 2009 Jun 1;17(11):3987-94. doi: 10.1016/j.bmc.2009.04.007. Epub 2009 Apr 11. Bioorg Med Chem. 2009. PMID: 19414267

9

Major advances in the development of histamine H4 receptor ligands.

Smits RA, Leurs R, de Esch IJ. Smits RA, et al. Drug Discov Today. 2009 Aug;14(15-16):745-53. doi: 10.1016/j.drudis.2009.05.007. Epub 2009 May 27. Drug Discov Today. 2009. PMID: 19477292 Review.

10

Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists.

Smits RA, Adami M, Istyastono EP, Zuiderveld OP, van Dam CM, de Kanter FJ, Jongejan A, Coruzzi G, Leurs R, de Esch IJ. Smits RA, et al. J Med Chem. 2010 Mar 25;53(6):2390-400. doi: 10.1021/jm901379s. J Med Chem. 2010. PMID: 20192225

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