Class I histone deacetylases (HDAC1–3) are histone lysine delactylases

C Moreno-Yruela, D Zhang, W Wei, M Bæk, W Liu… - Science …, 2022 - science.org
Lysine L-lactylation [K (L-la)] is a newly discovered histone mark stimulated under conditions
of high glycolysis, such as the Warburg effect. K (L-la) is associated with functions that are …

Mechanism-based inhibitors of SIRT2: structure–activity relationship, X-ray structures, target engagement, regulation of α-tubulin acetylation and inhibition of breast …

AL Nielsen, N Rajabi, N Kudo, K Lundø… - RSC Chemical …, 2021 - pubs.rsc.org
Sirtuin 2 (SIRT2) is a protein deacylase enzyme that removes acetyl groups and longer
chain acyl groups from post-translationally modified lysine residues. It affects diverse …

Substrates and Cyclic Peptide Inhibitors of the Oligonucleotide‐Activated Sirtuin 7

JE Bolding, AL Nielsen, I Jensen… - Angewandte Chemie …, 2023 - Wiley Online Library
The sirtuins are NAD+‐dependent lysine deacylases, comprising seven isoforms (SIRT1–7)
in humans, which are involved in the regulation of a plethora of biological processes …

Dethioacylation by sirtuins 1–3: considerations for drug design using mechanism-based sirtuin inhibition

N Rajabi, AL Nielsen, CA Olsen - ACS Medicinal Chemistry …, 2020 - ACS Publications
The sirtuin enzymes are potential drug targets for intervention in a series of diseases. Efforts
to inhibit enzymes of this class with thioamide-and thiourea-containing, substrate-mimicking …

Kinetic characterization of inhibitors of histone deacetylases (HDACs) and sirtuins

C Moreno-Yruela, AS Madsen, CA Olsen - 2019 - researchsquare.com
Histone deacetylase (HDAC) inhibitors are employed for the treatment of lymphoma and are
under development against multiple other types of cancer and neurodegenerative diseases …

Fluorogenic Substrates and Cyclic Peptide Inhibitors of the Oligonucleotide Activated SIRT7

JE Bolding, AL Nielsen, I Jensen, LA Ryberg… - bioRxiv, 2023 - biorxiv.org
The sirtuins are NAD+-dependent lysine deacylases, comprising seven isoforms (SIRT1–7)
in humans, which are involved in the regulation of a plethora of biology, including gene …

[PDF][PDF] Selective inhibitors of SIRT2 regulate perinuclear α-tubulin acetylation, migration, and invasion of breast cancer cells

AL Nielsen, N Rajabi, N Kudo, K Lundø… - bioRxiv 2020.03 …, 2020 - scholar.archive.org
ABSTRACT Sirtuin 2 (SIRT2) is a protein deacylase enzyme that has been reported to
remove both acetyl groups and longer chain acyl groups from lysine residues in post …