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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: haisma hj. 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.
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: haisma hj. Sci Rep. 2017 Mar 27;7:45047. doi: 10.1038/srep45047. Sci Rep. 2017. PMID: 28344354 Free PMC article.
Histone acetyl transferases as emerging drug targets.
Dekker FJ, Haisma HJ. Dekker FJ, et al. Among authors: haisma hj. Drug Discov Today. 2009 Oct;14(19-20):942-8. doi: 10.1016/j.drudis.2009.06.008. Epub 2009 Jul 2. Drug Discov Today. 2009. PMID: 19577000 Review.
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: haisma hj. 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.
154 results