sirt-1 inhibitor  (ASINEX Inc)

Journal: Molecules

Article Title: Virtual Screening in the Identification of Sirtuins’ Activity Modulators

doi: 10.3390/molecules27175641

Figure Lengend Snippet: Perspective of the computational studies leading to the identification of selective and/or pan-Sirtuins modulators (shown in green). The chemical structure and the explored biological activity of the discovered hit compounds are reported. The applied virtual screening (VS) strategy is specified as structure-based (SBVS) or ligand-based (LBVS) methodology. The results are listed based on the sirtuin type (alternatively in gray and cyan), according to SBVS followed by LBVS and combined SB-LB approaches, as chronological order. Data about parasitic sirtuins (depicted in coral) are also detailed, referring to the Leishmania (Lm-Sirt), Trypanosoma cruzi (Tc-Sirt) and Schistosoma mansoni (Sm-Sirt) sirtuins.

Article Snippet: 2021 , [ ] , Screening of SIRT-6 inhibitors and activators: A novel activator has an impact on breast cancer cells , 6 , LB-SB , LB: pharmacophore, similarity based , 1,2 , YES , ENAMINE (4 103 115), Chembridge (1 022 400), in house library of 1,4-dihydropyridine derivatives (∼100) , MOE (pharmacophore, similarity, docking), Glide/Maestro/ Schrodinger (docking) , 4H-chromen analogs (A), 1,4-dihydropyridine (I) , A, I , 80 μM (EC 50 , activator) 60% @200 μM (IC 50 , inhibitor).

Techniques: Activity Assay, Biomarker Discovery, Software, Inhibition, In Silico, Functional Assay, In Vitro, Sequencing, Generated, Histone Deacetylase Assay, Binding Assay, Analogues, Drug discovery, Purification, Modification, Activation Assay, Derivative Assay

Journal: Food Science & Nutrition

Article Title: Nobiletin Ameliorates Skeletal Muscle Performance in D‐Galactose‐Induced Aging Mice by Boosting Aerobic Metabolism

doi: 10.1002/fsn3.71416

Figure Lengend Snippet: Nob improved the antioxidant capacity of skeletal muscle in D‐gal‐induced aging mice. (A) ROS content, n = 3 mice/group; (B) SOD activity, n = 4 mice/group; (C) MDA content, n = 4 mice/group; (E–G) Western blot analysis of SIRT1, PGC‐1α, Nrf2, and GAPDH in D‐gal‐induced C2C12 cells treated with vehicle and Nob, n = 3. ** p < 0.01, *** p < 0.001, **** p < 0.0001.

Article Snippet: SIRT‐1 inhibitor (EX‐527, HY‐15452) was obtained from MedChemExpress (Shanghai, China).

Techniques: Activity Assay, Western Blot

Journal: International Journal of Molecular Sciences

Article Title: Acetylation of Steroidogenic Acute Regulatory Protein Sensitizes 17β-Estradiol Regulation in Hormone-Sensitive Breast Cancer Cells

doi: 10.3390/ijms25168732

Figure Lengend Snippet: Acetylated StAR lysine residues (highlighted in red) under basal (DMSO, dimethyl sulfoxide) and Panobinostat (PANO)-, SAHA-, IV-, and VII-treated conditions in MCF7 cells.

Article Snippet: A number of key reagents were utilized in this study, as follows: Panobinostat (LBH589) was obtained from APExBIO (Houston, TX, USA); Vorinostat (SAHA) and SIRT 1 Inhibitors IV and VII were purchased from Millipore-Sigma (St. Louis, MO, USA); anti-StAR antibodies (Abs) (ab180804 or ab96637) were obtained from Abcam (Boston, MA, USA); and an ELISA kit for E2 was purchased from Cayman Chemical Co. (Ann Arbor, MI, USA) [ , ].

Techniques: