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HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity.
Leus NG, van der Wouden PE, van den Bosch T, Hooghiemstra WTR, Ourailidou ME, Kistemaker LE, Bischoff R, Gosens R, Haisma HJ, Dekker FJ. Leus NG, et al. Among authors: van den bosch t, van der wouden pe. Biochem Pharmacol. 2016 May 15;108:58-74. doi: 10.1016/j.bcp.2016.03.010. Epub 2016 Mar 16. Biochem Pharmacol. 2016. PMID: 26993378 Free PMC article.
Enzyme kinetics and inhibition of histone acetyltransferase KAT8.
Wapenaar H, van der Wouden PE, Groves MR, Rotili D, Mai A, Dekker FJ. Wapenaar H, et al. Among authors: van der wouden pe. Eur J Med Chem. 2015 Nov 13;105:289-96. doi: 10.1016/j.ejmech.2015.10.016. Epub 2015 Oct 22. Eur J Med Chem. 2015. PMID: 26505788 Free PMC article.
HDAC1-3 inhibitor MS-275 enhances IL10 expression in RAW264.7 macrophages and reduces cigarette smoke-induced airway inflammation in mice.
Leus NG, van den Bosch T, van der Wouden PE, Krist K, Ourailidou ME, Eleftheriadis N, Kistemaker LE, Bos S, Gjaltema RA, Mekonnen SA, Bischoff R, Gosens R, Haisma HJ, Dekker FJ. Leus NG, et al. Among authors: van den bosch t, van der wouden pe. Sci Rep. 2017 Mar 27;7:45047. doi: 10.1038/srep45047. Sci Rep. 2017. PMID: 28344354 Free PMC article.
The relevance of Ki calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor.
Wapenaar H, van den Bosch T, Leus NGJ, van der Wouden PE, Eleftheriadis N, Hermans J, Hailu GS, Rotili D, Mai A, Dömling A, Bischoff R, Haisma HJ, Dekker FJ. Wapenaar H, et al. Among authors: van den bosch t, van der wouden pe. Eur J Med Chem. 2017 Aug 18;136:480-486. doi: 10.1016/j.ejmech.2017.05.015. Epub 2017 May 5. Eur J Med Chem. 2017. PMID: 28527406 Free PMC article.
Light-controlled inhibition of BRAFV600E kinase.
Hoorens MWH, Ourailidou ME, Rodat T, van der Wouden PE, Kobauri P, Kriegs M, Peifer C, Feringa BL, Dekker FJ, Szymanski W. Hoorens MWH, et al. Among authors: van der wouden pe. Eur J Med Chem. 2019 Oct 1;179:133-146. doi: 10.1016/j.ejmech.2019.06.042. Epub 2019 Jun 18. Eur J Med Chem. 2019. PMID: 31252305
7-Hydroxycoumarins Are Affinity-Based Fluorescent Probes for Competitive Binding Studies of Macrophage Migration Inhibitory Factor.
Xiao Z, Chen D, Song S, van der Vlag R, van der Wouden PE, van Merkerk R, Cool RH, Hirsch AKH, Melgert BN, Quax WJ, Poelarends GJ, Dekker FJ. Xiao Z, et al. Among authors: van der wouden pe. J Med Chem. 2020 Oct 22;63(20):11920-11933. doi: 10.1021/acs.jmedchem.0c01160. Epub 2020 Oct 13. J Med Chem. 2020. PMID: 32940040 Free PMC article.
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