List of works - Frank J Dekker

6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site ⬇️

scientific article published on November 10, 2011

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

scientific article published on 16 March 2017

A Pathophysiological Model of Non-Alcoholic Fatty Liver Disease Using Precision-Cut Liver Slices ⬇️

scientific article published on 27 February 2019

A combinatorial approach for the discovery of drug-like inhibitors of 15-lipoxygenase-1

scientific article published on 12 April 2019

A dual inhibitor of matrix metalloproteinases and a disintegrin and metalloproteinases, [¹⁸F]FB-ML5, as a molecular probe for non-invasive MMP/ADAM-targeted imaging.

scientific article published on 15 November 2014

A functional screen implicates microRNA-138-dependent regulation of the depalmitoylation enzyme APT1 in dendritic spine morphogenesis

scientific article published on 24 May 2009

Activity-Based Probes for 15-Lipoxygenase-1.

scientific article published on 9 September 2016

Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the Syk SH2 domains with equally high affinity as the natural ligand

scientific article published in April 2003

Anacardic acid derived salicylates are inhibitors or activators of lipoxygenases

scientific article published on 21 June 2012

Antibody-Free Detection of Protein Tyrosine Nitration in Tissue Sections

scientific article published on 11 July 2011

Aqueous oxidative Heck reaction as a protein-labeling strategy

scientific article published on 20 December 2013

Basic nuclear processes affected by histone acetyltransferases and histone deacetylase inhibitors.

scientific article published on August 2013

Binding of a diphosphorylated-ITAM peptide to spleen tyrosine kinase (Syk) induces distal conformational changes: a hydrogen exchange mass spectrometry study.

scientific article published in July 2005

Catalytic asymmetric total synthesis of (S)-(-)-zearalenone, a novel lipoxygenase inhibitor

scientific article published on 20 June 2013

Characterization of a thermostable methylaspartate ammonia lyase from Carboxydothermus hydrogenoformans

scientific article published on 18 October 2011

Cyclic phosphopeptides for interference with Grb2 SH2 domain signal transduction prepared by ring-closing metathesis and phosphorylation

scientific article published on 01 October 2003

Delivery of epidrugs

scientific article published on 25 March 2014

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

scientific article published on 09 July 2016

Design of compound libraries based on natural product scaffolds and protein structure similarity clustering (PSSC).

scientific article

Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups

scientific article

Development of highly potent inhibitors of the Ras-targeting human acyl protein thioesterases based on substrate similarity design

scientific article published on 9 September 2011

Discovery of a novel activator of 5-lipoxygenase from an anacardic acid derived compound collection.

scientific article

Engineering methylaspartate ammonia lyase for the asymmetric synthesis of unnatural amino acids

scientific article

Enhancement of the enantioselectivity of carboxylesterase A by structure-based mutagenesis

scientific article published on 12 January 2012

Enrichment and Detection of Tyrosine-Nitrated Proteins

scientific article published on 01 August 2012

Enzyme kinetics and inhibition of histone acetyltransferase KAT8.

scientific article published on 22 October 2015

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.

scientific article published on 15 March 2016

Histone acetyl transferases as emerging drug targets.

scientific article published on 02 July 2009

Histone acetyltransferases are crucial regulators in NF-κB mediated inflammation.

scientific article

Histone acetyltransferases: challenges in targeting bi-substrate enzymes

scientific article

Histone deacetylase 3 (HDAC 3) as emerging drug target in NF-κB-mediated inflammation

scientific article

Identification of 6-benzyloxysalicylates as a novel class of inhibitors of 15-lipoxygenase-1.

scientific article published on 5 March 2015

Identification of Acyl Protein Thioesterases 1 and 2 as the Cellular Targets of the Ras-Signaling Modulators Palmostatin B and M

scientific article published on 09 September 2011

Identification of potential antivirulence agents by substitution-oriented screening for inhibitors of Streptococcus pyogenes sortase A

scientific article published on 15 October 2018

Improved inhibition of the histone acetyltransferase PCAF by an anacardic acid derivative

scientific article published on 3 July 2010

Increased acetylation of lysine 317/320 of p53 caused by BCR-ABL protects from cytoplasmic translocation of p53 and mitochondria-dependent apoptosis in response to DNA damage

scientific article

Inflammation, Cancer and Oxidative Lipoxygenase Activity are Intimately Linked

scientific article published on 17 July 2014

Inhibiting the palmitoylation/depalmitoylation cycle selectively reduces the growth of hematopoietic cells expressing oncogenic Nras

scientific article published on 5 December 2011

Inhibition of PCAF by anacardic acid derivative leads to apoptosis and breaks resistance to DNA damage in BCR-ABL-expressing cells

scientific article

Inhibition of the PCAF histone acetyl transferase and cell proliferation by isothiazolones.

scientific article

Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages

scientific article published on 18 May 2019

Isothiazolones; thiol-reactive inhibitors of cysteine protease cathepsin B and histone acetyltransferase PCAF

scientific article published on 25 January 2011

Light-Controlled Histone Deacetylase (HDAC) Inhibitors: Towards Photopharmacological Chemotherapy

scientific article published on 29 September 2015

Metabolic alkene labeling and in vitro detection of histone acylation via the aqueous oxidative Heck reaction

scientific article (publication date: 28 March 2015)

Novel 15-Lipoxygenase-1 Inhibitor Protects Macrophages from Lipopolysaccharide-Induced Cytotoxicity

scientific article published on 19 April 2019

Photoactivation provides a mechanistic explanation for pan-assay interference behaviour of 2-aminopyrroles in lipoxygenase inhibition

scientific article published on 24 July 2017

Protein flexibility and ligand rigidity: a thermodynamic and kinetic study of ITAM-based ligand binding to Syk tandem SH2.

scientific article

Raft protein clustering alters N-Ras membrane interactions and activation pattern.

scientific article

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

scientific article published on 2 September 2015

Reactivity of isothiazolones and isothiazolone-1-oxides in the inhibition of the PCAF histone acetyltransferase

scientific article

Replacement of an Indole Scaffold Targeting Human 15-Lipoxygenase-1 Using Combinatorial Chemistry

scientific article published on 02 May 2019

Replacement of the intervening amino acid sequence of a Syk-binding diphosphopeptide by a nonpeptide spacer with preservation of high affinity

scientific article published on 01 March 2002

Role of solution conformation and flexibility of short peptide ligands that bind to the p56(lck) SH2 domain.

scientific article

SK channel activation potentiates auranofin-induced cell death in glio- and neuroblastoma cells

scientific article published on 15 November 2019

SK channel-mediated metabolic escape to glycolysis inhibits ferroptosis and supports stress resistance in C. elegans

scientific article published on 23 April 2020

Site-specific quantification of lysine acetylation in the N-terminal tail of histone H4 using a double-labelling, targeted UHPLC MS/MS approach

scientific article (publication date: May 2016)

Small Multitarget Molecules Incorporating the Enone Moiety

scientific article published on 07 January 2019

Small molecule inhibition of protein depalmitoylation as a new approach towards downregulation of oncogenic Ras signalling

scientific article

Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases.

scientific article

Small-molecule inhibition of APT1 affects Ras localization and signaling

scientific article

Stability of energy metabolites-An often overlooked issue in metabolomics studies: A review.

scientific article published on 11 May 2015

Structure-activity relationships for binding of 4-substituted triazole-phenols to macrophage migration inhibitory factor (MIF)

scientific article published on 11 November 2019

Surface plasmon resonance thermodynamic and kinetic analysis as a strategic tool in drug design. Distinct ways for phosphopeptides to plug into Src- and Grb2 SH2 domains.

scientific article published in February 2005

Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties

scientific article published on 17 December 2019

The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors.

scientific article published on 2 March 2018

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

scientific article

Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity

scientific article published in December 2016

List of works by Frank J Dekker

6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site ⬇️

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

A Pathophysiological Model of Non-Alcoholic Fatty Liver Disease Using Precision-Cut Liver Slices ⬇️

A combinatorial approach for the discovery of drug-like inhibitors of 15-lipoxygenase-1

A dual inhibitor of matrix metalloproteinases and a disintegrin and metalloproteinases, [¹⁸F]FB-ML5, as a molecular probe for non-invasive MMP/ADAM-targeted imaging.

A functional screen implicates microRNA-138-dependent regulation of the depalmitoylation enzyme APT1 in dendritic spine morphogenesis

Activity-Based Probes for 15-Lipoxygenase-1.

Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the Syk SH2 domains with equally high affinity as the natural ligand

Anacardic acid derived salicylates are inhibitors or activators of lipoxygenases

Antibody-Free Detection of Protein Tyrosine Nitration in Tissue Sections

Aqueous oxidative Heck reaction as a protein-labeling strategy

Basic nuclear processes affected by histone acetyltransferases and histone deacetylase inhibitors.

Binding of a diphosphorylated-ITAM peptide to spleen tyrosine kinase (Syk) induces distal conformational changes: a hydrogen exchange mass spectrometry study.

Catalytic asymmetric total synthesis of (S)-(-)-zearalenone, a novel lipoxygenase inhibitor

Characterization of a thermostable methylaspartate ammonia lyase from Carboxydothermus hydrogenoformans

Cyclic phosphopeptides for interference with Grb2 SH2 domain signal transduction prepared by ring-closing metathesis and phosphorylation

Delivery of epidrugs

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

Design of compound libraries based on natural product scaffolds and protein structure similarity clustering (PSSC).

Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups

Development of highly potent inhibitors of the Ras-targeting human acyl protein thioesterases based on substrate similarity design

Discovery of a novel activator of 5-lipoxygenase from an anacardic acid derived compound collection.

Engineering methylaspartate ammonia lyase for the asymmetric synthesis of unnatural amino acids

Enhancement of the enantioselectivity of carboxylesterase A by structure-based mutagenesis

Enrichment and Detection of Tyrosine-Nitrated Proteins

Enzyme kinetics and inhibition of histone acetyltransferase KAT8.

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.

Histone acetyl transferases as emerging drug targets.

Histone acetyltransferases are crucial regulators in NF-κB mediated inflammation.

Histone acetyltransferases: challenges in targeting bi-substrate enzymes

Histone deacetylase 3 (HDAC 3) as emerging drug target in NF-κB-mediated inflammation

Identification of 6-benzyloxysalicylates as a novel class of inhibitors of 15-lipoxygenase-1.

Identification of Acyl Protein Thioesterases 1 and 2 as the Cellular Targets of the Ras-Signaling Modulators Palmostatin B and M

Identification of potential antivirulence agents by substitution-oriented screening for inhibitors of Streptococcus pyogenes sortase A

Improved inhibition of the histone acetyltransferase PCAF by an anacardic acid derivative

Increased acetylation of lysine 317/320 of p53 caused by BCR-ABL protects from cytoplasmic translocation of p53 and mitochondria-dependent apoptosis in response to DNA damage

Inflammation, Cancer and Oxidative Lipoxygenase Activity are Intimately Linked

Inhibiting the palmitoylation/depalmitoylation cycle selectively reduces the growth of hematopoietic cells expressing oncogenic Nras

Inhibition of PCAF by anacardic acid derivative leads to apoptosis and breaks resistance to DNA damage in BCR-ABL-expressing cells

Inhibition of the PCAF histone acetyl transferase and cell proliferation by isothiazolones.

Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages

Isothiazolones; thiol-reactive inhibitors of cysteine protease cathepsin B and histone acetyltransferase PCAF

Light-Controlled Histone Deacetylase (HDAC) Inhibitors: Towards Photopharmacological Chemotherapy

Metabolic alkene labeling and in vitro detection of histone acylation via the aqueous oxidative Heck reaction

Novel 15-Lipoxygenase-1 Inhibitor Protects Macrophages from Lipopolysaccharide-Induced Cytotoxicity

Photoactivation provides a mechanistic explanation for pan-assay interference behaviour of 2-aminopyrroles in lipoxygenase inhibition

Protein flexibility and ligand rigidity: a thermodynamic and kinetic study of ITAM-based ligand binding to Syk tandem SH2.

Raft protein clustering alters N-Ras membrane interactions and activation pattern.

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

Reactivity of isothiazolones and isothiazolone-1-oxides in the inhibition of the PCAF histone acetyltransferase

Replacement of an Indole Scaffold Targeting Human 15-Lipoxygenase-1 Using Combinatorial Chemistry

Replacement of the intervening amino acid sequence of a Syk-binding diphosphopeptide by a nonpeptide spacer with preservation of high affinity

Role of solution conformation and flexibility of short peptide ligands that bind to the p56(lck) SH2 domain.

SK channel activation potentiates auranofin-induced cell death in glio- and neuroblastoma cells

SK channel-mediated metabolic escape to glycolysis inhibits ferroptosis and supports stress resistance in C. elegans

Site-specific quantification of lysine acetylation in the N-terminal tail of histone H4 using a double-labelling, targeted UHPLC MS/MS approach

Small Multitarget Molecules Incorporating the Enone Moiety

Small molecule inhibition of protein depalmitoylation as a new approach towards downregulation of oncogenic Ras signalling

Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases.

Small-molecule inhibition of APT1 affects Ras localization and signaling

Stability of energy metabolites-An often overlooked issue in metabolomics studies: A review.

Structure-activity relationships for binding of 4-substituted triazole-phenols to macrophage migration inhibitory factor (MIF)

Surface plasmon resonance thermodynamic and kinetic analysis as a strategic tool in drug design. Distinct ways for phosphopeptides to plug into Src- and Grb2 SH2 domains.

Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties

The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors.

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

Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity