Niklas Papenkordt
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View article: From Pharmacophore to Warhead: NAD <sup>+</sup> ‐Targeting Triazoles as Mechanism‐Based Sirtuin Inhibitors
From Pharmacophore to Warhead: NAD <sup>+</sup> ‐Targeting Triazoles as Mechanism‐Based Sirtuin Inhibitors Open
Sirtuins (SIRTs) are nicotinamide adenine dinucleotide (NAD + )‐dependent lysine deacylases linked to key physiological and disease processes. Here, we report a new class of mechanism‐based 1,2,3‐triazole inhibitors that hijack SIRT cataly…
View article: From Pharmacophore to Warhead: NAD <sup>+</sup> ‐Targeting Triazoles as Mechanism‐Based Sirtuin Inhibitors
From Pharmacophore to Warhead: NAD <sup>+</sup> ‐Targeting Triazoles as Mechanism‐Based Sirtuin Inhibitors Open
Sirtuins (SIRTs) are nicotinamide adenine dinucleotide (NAD + )‐dependent lysine deacylases linked to key physiological and disease processes. Here, we report a new class of mechanism‐based 1,2,3‐triazole inhibitors that hijack SIRT cataly…
View article: Tailored SirReal-type inhibitors enhance SIRT2 inhibition through ligand stabilization and disruption of NAD <sup>+</sup> co-factor binding
Tailored SirReal-type inhibitors enhance SIRT2 inhibition through ligand stabilization and disruption of NAD <sup>+</sup> co-factor binding Open
The duality of halogen-bonding-mediated ligand stabilization and the inteference of NAD + co-factor binding represents an effective strategy in the development of highly potent SIRT2 inhibitors.
View article: Aromatic Amino Acid Hydroxylases as Off-Targets of Histone Deacetylase Inhibitors
Aromatic Amino Acid Hydroxylases as Off-Targets of Histone Deacetylase Inhibitors Open
The aromatic amino acid hydroxylases (AAAHs) phenylalanine hydroxylase, tyrosine hydroxylase, and tryptophan hydroxylases 1 and 2 are structurally related enzymes that contain an active site iron atom and depend on tetrahydrobiopterin (BH<…
View article: Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation
Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation Open
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6 (HDAC6) has been associated with the pathogenesis of cancer and neurodegeneration, thus making these two enzymes promising targets for pharmaceutica…
View article: Extraction and Purification of a Phycocolloid from <i>Chaetomorpha aerea</i>
Extraction and Purification of a Phycocolloid from <i>Chaetomorpha aerea</i> Open
Phycocolloids are gelling polysaccharides extracted from algae that have found applications as microbiological culture media, food thickener, and cosmetic rheological modifiers. The extensive use of algae species that have not yet been dom…
View article: Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation
Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation Open
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6 (HDAC6) has been associated with the pathogenesis of cancer and neurodegeneration, thus making these two enzymes promising targets for pharmaceutica…
View article: Total synthesis and biological evaluation of histone deacetylase inhibitor WF-3161
Total synthesis and biological evaluation of histone deacetylase inhibitor WF-3161 Open
Matteson homologations and a Pd-catalysed C–H functionalisation are key steps in the synthesis of highly selective HDAC1 inhibitor WF-3161.
View article: Extraction and purification of a phycocolloid from Chaetomorpha aerea
Extraction and purification of a phycocolloid from Chaetomorpha aerea Open
Phycocolloids are gelling polysaccharides extracted from algae that have found applications as microbiological culture media, food thickener, and cosmetic rheological modifiers. The extensive use of algae species that have not been yet dom…
View article: Extraction and purification of a phycocolloid from Chaetomorpha aerea
Extraction and purification of a phycocolloid from Chaetomorpha aerea Open
Phycocolloids are gelling polysaccharides extracted from algae that have found applications as microbiological culture media, food thickener, and cosmetic rheological modifiers. The extensive use of algae species that have not been yet dom…