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Small and colorful stones make beautiful mosaics: fragment-based chemogenomics.
de Graaf C, Vischer HF, de Kloe GE, Kooistra AJ, Nijmeijer S, Kuijer M, Verheij MH, England PJ, van Muijlwijk-Koezen JE, Leurs R, de Esch IJ. de Graaf C, et al. Among authors: verheij mh. Drug Discov Today. 2013 Apr;18(7-8):323-30. doi: 10.1016/j.drudis.2012.12.003. Epub 2012 Dec 22. Drug Discov Today. 2013. PMID: 23266367
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.
Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines.
Spurny R, Ramerstorfer J, Price K, Brams M, Ernst M, Nury H, Verheij M, Legrand P, Bertrand D, Bertrand S, Dougherty DA, de Esch IJ, Corringer PJ, Sieghart W, Lummis SC, Ulens C. Spurny R, et al. Proc Natl Acad Sci U S A. 2012 Oct 30;109(44):E3028-34. doi: 10.1073/pnas.1208208109. Epub 2012 Oct 3. Proc Natl Acad Sci U S A. 2012. PMID: 23035248 Free PMC article.
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