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    SIRT2 deacetylates and decreases the expression of FOXM1 in colon cancer
    (Wiley, 2024) Yildiz, Baris; Demirel, Ramazan; Staudacher, Jonas J.; Beseren, Hatice; Yildiz, Gulden; Akpinar, Ali Emre; Park, Seong-Hoon
    New FOXM1-specific inhibitors with the potential to be used for therapeutic purposes are under extensive research. We hypothesized that deacetylation of FOXM1 would decrease protein expression, thus providing novel therapeutic management of colon cancers. Immunostaining was used to determine FOXM1 and SIRT2 expressions in human colon cancer tissue microarrays (n = 90) from Stage I to Stage IV. SIRT2-FOXM1 interaction was evaluated in colon cancer cells using immunoprecipitation. Deacetylation of FOXM1 via SIRT2 was determined using in vitro deacetylation assays. FOXM1 could be hyper-acetylated when p300 and pCAF histone acetyltransferases were administered alongside deacetylase inhibitors. We detected that SIRT2 and FOXM1 physically interacted, and SIRT2 deacetylated FOXM1 in vitro. SIRT2 overexpression led to a significant decrease while knockdown of SIRT2 increased the FOXM1 expression in HCT116 human colon carcinoma cells. In the analysis of 90 human colorectal cancer samples, high SIRT2 expression was observed in about 49% of colorectal cancer, intermediate in 29%, and low or no staining in 22%. Strong SIRT2 expression was found to be negatively associated with the FOXM1 staining in our clinical cohort. This study reveals a molecular interaction and association between SIRT2 and FOXM1 expression in colon cancer cell lines and human colon cancer samples, and suggests that targeting SIRT2 activity using small molecule modulators may be a promising therapeutic approach for colorectal cancer. SIRT2-FOXM1 interaction in colon cancer. SIRT2 and FOXM1 physically interacted and SIRT2 deacetylated FOXM1 in vitro. Strong SIRT2 expression was negatively associated with FOXM1 staining in a human colon carcinoma tissue microarray. Resveratrol, berberine, and quercetin reduced FOXM1 expression in colon cancer cells.image Upregulation of FOXM1 may be an early molecular signal required for cancer SIRT2 and FOXM1 physically interacted, and SIRT2 deacetylated FOXM1 in vitro Strong SIRT2 expression was negatively associated with the FOXM1 staining in the TMA Resveratrol, berberine and quercetin decreased FOXM1 expression in colorectal cancer cells
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    Synthesis and characterization of some benzidine-based azomethine derivatives with molecular docking studies and anticancer activities
    (Springer Int Publ Ag, 2023) Erdogan, Musa; Yesildag, Ali; Yildiz, Baris; Tuzun, Burak; Ozden, Ozkan
    In this study, a benzidine-based azomethine derivate 2 with a proposed new mechanism and its two derivatives 4a-b have been designed, synthesized and characterized by 1H, 13C NMR, FT-IR, and HRMS spectroscopic techniques, and their anticancer properties were investigated. The target compounds 2, 4a-b were obtained with excellent yields (91% and above) by condensation of benzidine (1) with three different aldehyde derivatives (formaldehyde, benzaldehyde 3a orp-nitrobenzaldehyde 3b) in refluxing EtOH. Surprisingly, treatment of benzidine (1) with formaldehyde afforded N-4,N-4,N-4',N-4'-tetrakis(ethoxymethyl)-[1,1'-biphenyl]-4,4'-diamine (2). The anticancer properties of these benzidine derivatives 2, 4a-b against two cell lines (MDA-MB-231 human breast adenocarcinoma and DLD1 human colorectal adenocarcinoma cell lines) were investigated with a colorimetric assay using the tetrazolium salt WST-8 (2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium, monosodium salts). The obtained results showed that the benzidine-based azomethine derivatives 2, 4a-b had a significant effect on the human breast cancer cell line (MDA-MB-231). Then, molecular docking calculations were made to compare the biological activities of benzidine-based azomethine derivatives 2, 4a-b against cancer proteins. ADME/T analysis was performed to examine the drug properties of benzidine-based azomethine derivatives 2, 4a-b. The compounds 2, 4a-b are promising as potential anticancer drug candidates.{GRAPHIACAL ABSTRACT}