A5051208114- Sirtuins and Resveratrol in Medicine
- Toxin Mechanisms and Immunotoxins
- Autophagy in Disease and Therapy
- Histone Deacetylase Inhibitors Research
- Cholinesterase and Neurodegenerative Diseases
- Peptidase Inhibition and Analysis
- Global Public Health Policies and Epidemiology
- Phenothiazines and Benzothiazines Synthesis and Activities
- Quinazolinone synthesis and applications
- Natural product bioactivities and synthesis
- Global Healthcare and Medical Tourism
- Business and Economic Development
- Biochemical and Molecular Research
- Protein Degradation and Inhibitors
- Computational Drug Discovery Methods
- Crystallization and Solubility Studies
- Medicinal Plants and Neuroprotection
- Andrographolide Research and Applications
- X-ray Diffraction in Crystallography
- PARP inhibition in cancer therapy
- Synthesis and biological activity
- Tensor decomposition and applications
Martin Luther University Halle-Wittenberg
2015-2024
Biruni University
2018
Sirtuins are NAD+-dependent protein lysine deacylases implicated in aging-related diseases. Mammalian Sirtuin 4 (Sirt4) is located mitochondria and a potential therapeutic target for cancer metabolic diseases, but no potent selective Sirt4 inhibitors have been reported. Here, we describe the identification of Sirt4-specific small-molecule inhibitors. Testing hits from target-based virtual screen revealed 12 active compounds. A focused based on two top compounds, followed by...
Sirtuins are protein deacylases that regulate metabolism and stress responses implicated in aging-related diseases. Modulators of the human sirtuins Sirt1–7 sought as chemical tools potential therapeutics, e.g., for cancer. Selective potent inhibitors available Sirt2, but selective Sirt5 with Ki values low nanomolar range lacking. We synthesized screened 3-arylthiosuccinylated 3-benzylthiosuccinylated peptide derivatives yielding low-nanomolar values. A biotinylated derivative this scaffold...
Sirtuin 1 (Sirt1) is a NAD+ dependent lysine deacetylase associated with the pathogenesis of various diseases including cancer. In many cancer types Sirt1 expression increased. Higher levels have been metastasis and poor prognosis. However, tumor suppressing properties also observed in some instances even dual role for same type has reported. Increased activity linked to life span extension cells respectively organisms by promoting DNA repair processes downregulation suppressor proteins....
Sirtuins are nicotinamide adenine dinucleotide (NAD+)-dependent class III histone deacetylases, which have been linked to the pathogenesis of numerous diseases, including HIV, metabolic disorders, neurodegeneration and cancer. Docking virtual pan-African natural products library (p-ANAPL), followed by in vitro testing, resulted identification two inhibitors sirtuin 1, 2 3 (sirt1–3). Two bichalcones, known as rhuschalcone IV (8) an analogue I (9), previously isolated from medicinal plant Rhus...
Nonpolar derivatives of heterocyclic aromatic screening hits like the non‐selective sirtuin inhibitor splitomicin tend to be poorly soluble in biological fluids. Unlike sp 3 ‐rich natural products, flat compounds are prone stacking and often difficult optimize into leads with activity cellular systems. The aim this work was identify anchor points for introduction fragments polar functional groups newly discovered active (IC 50 = 5 μM) but nonpolar scaffold 1,2‐dihydro‐3 H ‐naphth[1,2‐ e...
Sirtuins are nicotinamide adenine dinucleotide (NAD+)-dependent class III histone deacetylases and have been linked to the pathogenesis of numerous diseases such as HIV, metabolic disorders, neurodegeneration cancer. Docking virtual pan-African natural products library (p-ANAPL), followed by in vitro testing, resulted identification two inhibitors sirtuin 1, 2 3 (sirt1-3). Two bichalcones; rhuschalcone IV (8) I (9), previously isolated from medicinal plant Rhus pyroides, were shown be active...