[HTML][HTML] Sirtuin functions and modulation: from chemistry to the clinic

V Carafa, D Rotili, M Forgione, F Cuomo… - Clinical …, 2016 - Springer
Sirtuins are NAD+-dependent histone deacetylases regulating important metabolic
pathways in prokaryotes and eukaryotes and are involved in many biological processes …

[HTML][HTML] SIRT1 and SIRT2 activity control in neurodegenerative diseases

R Manjula, K Anuja, FJ Alcain - Frontiers in pharmacology, 2021 - frontiersin.org
Sirtuins are NAD+ dependent histone deacetylases (HDAC) that play a pivotal role in
neuroprotection and cellular senescence. SIRT1-7 are different homologs from sirtuins. They …

Chemically induced degradation of sirtuin 2 (Sirt2) by a proteolysis targeting chimera (PROTAC) based on sirtuin rearranging ligands (SirReals)

M Schiedel, D Herp, S Hammelmann… - Journal of medicinal …, 2018 - ACS Publications
Here we report the development of a proteolysis targeting chimera (PROTAC) based on the
combination of the unique features of the sirtuin rearranging ligands (SirReals) as highly …

An overview of Sirtuins as potential therapeutic target: Structure, function and modulators

Y Wang, J He, M Liao, M Hu, W Li, H Ouyang… - European journal of …, 2019 - Elsevier
Abstract Sirtuin (Yeast Silent Information RegulatorsⅡ, Sir2) was first discovered in the
1970s. Because of its function by removing acetylated groups from histones in the presence …

[HTML][HTML] Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

SR Alizadeh, SM Hashemi - Medicinal Chemistry Research, 2021 - Springer
Currently, the development of anticancer drug resistance is significantly restricted the clinical
efficacy of the most commonly prescribed anticancer drug. Malignant disease is widely …

The Current State of NAD+‐Dependent Histone Deacetylases (Sirtuins) as Novel Therapeutic Targets

M Schiedel, D Robaa, T Rumpf… - Medicinal research …, 2018 - Wiley Online Library
Sirtuins are NAD+‐dependent protein deacylases that cleave off acetyl, as well as other acyl
groups, from the ε‐amino group of lysines in histones and other substrate proteins. Seven …

Development of first-in-class dual Sirt2/HDAC6 inhibitors as molecular tools for dual inhibition of tubulin deacetylation

L Sinatra, A Vogelmann, F Friedrich… - Journal of medicinal …, 2023 - ACS Publications
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6
(HDAC6) has been associated with the pathogenesis of cancer and neurodegeneration …

Synthesis, in-vitro α-glucosidase inhibition and molecular docking studies of 1, 3, 4-thiadiazole-5, 6-diphenyl-1, 2, 4-triazine hybrids: potential leads in the search of …

H Kumar, M Dhameja, S Kurella, A Uma… - Journal of Molecular …, 2023 - Elsevier
Abstract A series of 1, 3, 4-thiadiazole-5, 6-diphenyl-triazine hybrids 7a-l have been
designed, synthesized and investigated for the α-glucosidase inhibitory activities. All the …

Further insight into the dual COX-2 and 15-LOX anti-inflammatory activity of 1, 3, 4-thiadiazole-thiazolidinone hybrids: The contribution of the substituents at 5th …

YM Omar, SG Abdel-Moty, HHM Abdu-Allah - Bioorganic Chemistry, 2020 - Elsevier
Herin we report the design, synthesis, full characterization and biological investigation of
new 15-LOX/COX dual inhibitors based on 1, 3-thiazolidin-4-one (15-lipoxygenase …

Versatile role of sirtuins in metabolic disorders: From modulation of mitochondrial function to therapeutic interventions

A Afzaal, K Rehman, S Kamal… - Journal of biochemical …, 2022 - Wiley Online Library
Abstract Sirtuins (SIRT1–7) are distinct histone deacetylases (HDACs) whose activity is
determined by cellular metabolic status andnicotinamide adenine dinucleotide (NAD+) …