de Esch IJP - Search Results

1

Fragment-to-Lead Medicinal Chemistry Publications in 2020.

de Esch IJP, Erlanson DA, Jahnke W, Johnson CN, Walsh L. de Esch IJP, et al. J Med Chem. 2022 Jan 13;65(1):84-99. doi: 10.1021/acs.jmedchem.1c01803. Epub 2021 Dec 20. J Med Chem. 2022. PMID: 34928151 Free PMC article. Review.

2

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. Curr Top Med Chem. 2006;6(13):1365-73. doi: 10.2174/15680266106061365. Curr Top Med Chem. 2006. PMID: 16918455 Review.

3

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

4

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

5

Transforming fragments into candidates: small becomes big in medicinal chemistry.

de Kloe GE, Bailey D, Leurs R, de Esch IJ. de Kloe GE, et al. Drug Discov Today. 2009 Jul;14(13-14):630-46. doi: 10.1016/j.drudis.2009.03.009. Epub 2009 Mar 31. Drug Discov Today. 2009. PMID: 19443265 Review.

6

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

7

Surface plasmon resonance biosensor based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots (LE hot spots) by deconstruction of nicotinic acetylcholine receptor α7 ligands.

de Kloe GE, Retra K, Geitmann M, Källblad P, Nahar T, van Elk R, Smit AB, van Muijlwijk-Koezen JE, Leurs R, Irth H, Danielson UH, de Esch IJ. de Kloe GE, et al. J Med Chem. 2010 Oct 14;53(19):7192-201. doi: 10.1021/jm100834y. J Med Chem. 2010. PMID: 20828128

8

Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A.

Verheij MH, de Graaf C, de Kloe GE, Nijmeijer S, Vischer HF, Smits RA, Zuiderveld OP, Hulscher S, Silvestri L, Thompson AJ, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ. Verheij MH, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5460-4. doi: 10.1016/j.bmcl.2011.06.123. Epub 2011 Jul 2. Bioorg Med Chem Lett. 2011. PMID: 21782429 Free PMC article.

9

Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.

de Graaf C, Kooistra AJ, Vischer HF, Katritch V, Kuijer M, Shiroishi M, Iwata S, Shimamura T, Stevens RC, de Esch IJ, Leurs R. de Graaf C, et al. J Med Chem. 2011 Dec 8;54(23):8195-206. doi: 10.1021/jm2011589. Epub 2011 Nov 7. J Med Chem. 2011. PMID: 22007643 Free PMC article.

10

Fragment based lead discovery of small molecule inhibitors for the EPHA4 receptor tyrosine kinase.

van Linden OP, Farenc C, Zoutman WH, Hameetman L, Wijtmans M, Leurs R, Tensen CP, Siegal G, de Esch IJ. van Linden OP, et al. Eur J Med Chem. 2012 Jan;47(1):493-500. doi: 10.1016/j.ejmech.2011.11.020. Epub 2011 Nov 18. Eur J Med Chem. 2012. PMID: 22137457

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