Niek G Leus

Niek G J Leus

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Niek G Leus

Niek G J Leus

Publications by authors named "Niek G J Leus"

16Publications

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1PubMed Central Citations

The relevance of K calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor.

Eur J Med Chem 2017 Aug 5;136:480-486. Epub 2017 May 5.

University of Groningen, Groningen Research Institute of Pharmacy, Department of Chemical and Pharmaceutical Biology, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2017.05.015DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5720340PMC
August 2017

A 6-alkylsalicylate histone acetyltransferase inhibitor inhibits histone acetylation and pro-inflammatory gene expression in murine precision-cut lung slices.

Pulm Pharmacol Ther 2017 06 16;44:88-95. Epub 2017 Mar 16.

Chemical and Pharmaceutical Biology, Groningen Research Institute of Pharmacy, University of Groningen, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.pupt.2017.03.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5447808PMC
June 2017

Design of a novel thiophene inhibitor of 15-lipoxygenase-1 with both anti-inflammatory and neuroprotective properties.

Eur J Med Chem 2016 Oct 9;122:786-801. Epub 2016 Jul 9.

Department of Chemical and Pharmaceutical Biology, Groningen Research Institute of Pharmacy, University of Groningen, Groningen, 9713 AV, The Netherlands.

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http://dx.doi.org/10.1016/j.ejmech.2016.07.010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5010146PMC
October 2016

Activity-Based Probes for 15-Lipoxygenase-1.

Angew Chem Int Ed Engl 2016 09 9;55(40):12300-5. Epub 2016 Sep 9.

Department of Chemical and Pharmaceutical Biology, Groningen Research Institute of Pharmacy, University of Groningen, Antonius Deusinglaan 1, 9713 AV, Groningen, The Netherlands.

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http://dx.doi.org/10.1002/anie.201606876DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5218545PMC
September 2016

The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases.

Biochem Pharmacol 2016 Feb 21;102:130-140. Epub 2015 Dec 21.

Pharmaceutical Gene Modulation, Groningen Research Institute of Pharmacy, University of Groningen, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.bcp.2015.12.010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4871277PMC
February 2016

Rational Development of a Potent 15-Lipoxygenase-1 Inhibitor with in Vitro and ex Vivo Anti-inflammatory Properties.

J Med Chem 2015 Oct 16;58(19):7850-62. Epub 2015 Sep 16.

Department of Pharmaceutical Gene Modulation, ‡Department of Drug Design, Groningen Research Institute of Pharmacy, University of Groningen , Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.

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http://dx.doi.org/10.1021/acs.jmedchem.5b01121DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4872822PMC
October 2015

SAINT-liposome-polycation particles, a new carrier for improved delivery of siRNAs to inflamed endothelial cells.

Eur J Pharm Biopharm 2015 Jan 25;89:40-7. Epub 2014 Nov 25.

University of Groningen, University Medical Center Groningen, Dept. of Pathology & Medical Biology, Medical Biology Section, Groningen, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.ejpb.2014.11.015DOI Listing
January 2015

VCAM-1 specific PEGylated SAINT-based lipoplexes deliver siRNA to activated endothelium in vivo but do not attenuate target gene expression.

Int J Pharm 2014 Jul 18;469(1):121-31. Epub 2014 Apr 18.

University of Groningen, University Medical Center Groningen, Department of Pathology & Medical Biology, Medical Biology section, Laboratory for Endothelial Biomedicine & Vascular Drug Targeting Research, Groningen, the Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.ijpharm.2014.04.041DOI Listing
July 2014

ATM increases activation-induced cytidine deaminase activity at downstream S regions during class-switch recombination.

J Immunol 2014 May 11;192(10):4887-96. Epub 2014 Apr 11.

Department of Microbiology and Physiological Systems, University of Massachusetts Medical School, Worcester, MA 01605.

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http://dx.doi.org/10.4049/jimmunol.1303481DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4049217PMC
May 2014

Anti-VCAM-1 SAINT-O-Somes enable endothelial-specific delivery of siRNA and downregulation of inflammatory genes in activated endothelium in vivo.

J Control Release 2014 Feb 3;176:64-75. Epub 2014 Jan 3.

University of Groningen, University Medical Center Groningen, Dept. of Pathology & Medical Biology, Medical Biology Section, Laboratory for Endothelial Biomedicine & Vascular Drug Targeting Research, Groningen, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.jconrel.2013.12.029DOI Listing
February 2014

Effective siRNA delivery to inflamed primary vascular endothelial cells by anti-E-selectin and anti-VCAM-1 PEGylated SAINT-based lipoplexes.

Int J Pharm 2014 Jan 12;459(1-2):40-50. Epub 2013 Nov 12.

University of Groningen, University Medical Center Groningen, Department of Pathology & Medical Biology, Medical Biology Section, Laboratory for Endothelial Biomedicine & Vascular Drug Targeting Research, Groningen, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.ijpharm.2013.11.008DOI Listing
January 2014

Anti-VCAM-1 and anti-E-selectin SAINT-O-Somes for selective delivery of siRNA into inflammation-activated primary endothelial cells.

Mol Pharm 2013 Aug 12;10(8):3033-44. Epub 2013 Jul 12.

Department of Pathology & Medical Biology, Medical Biology Section, Laboratory for Endothelial Biomedicine & Vascular Drug Targeting Research, University Medical Center Groningen, University of Groningen , Groningen, The Netherlands.

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http://dx.doi.org/10.1021/mp4001124DOI Listing
August 2013

Targeted siRNA delivery to diseased microvascular endothelial cells: cellular and molecular concepts.

IUBMB Life 2011 Aug 15;63(8):648-58. Epub 2011 Jul 15.

Department of Pathology & Medical Biology, Medical Biology section, Laboratory for Endothelial Biomedicine & Vascular Drug Targeting Research, University Medical Center, University of Groningen, The Netherlands.

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http://dx.doi.org/10.1002/iub.487DOI Listing
August 2011

Reassessment of the role of Mut S homolog 5 in Ig class switch recombination shows lack of involvement in cis- and trans-switching.

J Immunol 2008 Dec;181(12):8450-9

Department of Molecular Genetics and Microbiology, Program in Immunology and Virology, University of Massachusetts Medical School, Worcester, MA 01655, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2656362PMC
http://dx.doi.org/10.4049/jimmunol.181.12.8450DOI Listing
December 2008