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  • Open Access

    ARTICLE

    An ISSA-RF Algorithm for Prediction Model of Drug Compound Molecules Antagonizing ERα Gene Activity

    Minxi Rong1, Yong Li1,*, Xiaoli Guo1,*, Tao Zong2, Zhiyuan Ma2, Penglei Li2

    Oncologie, Vol.24, No.2, pp. 309-327, 2022, DOI:10.32604/oncologie.2022.021256

    Abstract Objectives: The ERα biological activity prediction model is constructed by the compound molecular data of the anti-breast cancer therapeutic target ERα and its biological activity data, which improves the screening efficiency of anti-breast cancer drug candidates and saves the time and cost of drug development. Methods: In this paper, Ridge model is used to screen out molecular descriptors with a high degree of influence on the biological activity of Erα and divide datasets with different numbers of the molecular descriptors by screening results. Random Forest (RF) is trained by Root Mean Square Error (RMSE) and Coefficient of determination (R2) to… More >

  • Open Access

    ARTICLE

    Cyclic biaxial tensile strain enhances osteogenic differentiation in rat bone marrow-derived mesenchymal stem cells via activating ERα-Wnt3a/β-catenin pathway

    MIN TANG1,#, XUELING HE1,2,#, XINGHONG YAO1, JIRUI WEN1, MINGYUE BAO1, LIANG LI1,*

    BIOCELL, Vol.46, No.6, pp. 1465-1472, 2022, DOI:10.32604/biocell.2022.018967

    Abstract The present study was designed to investigate the role of estrogen receptor α (ERα) in biaxial tensile strain (BTS) regulated osteogenic differentiation of rat bone marrow-derived mesenchymal stem cells (rBMSCs). rBMSCs were derived from rats and overexpressed ERα. The rBMSCs were subjected to BTS at 1 Hz with a strain of 2% for 4 h per day, 3 days, with or without ERα inhibitor ICI 182,780 (ICI). Then, bone mineralization was performed by Alizarin Red Staining. The markers of osteogenic differentiation and downstream Wnt3a/β-catenin signaling were detected by western blotting. Results showed that BTS enhanced the osteogenic differentiation of rBMSCs,… More >

  • Open Access

    ARTICLE

    Chaperone-mediated autophagy targeting chimeras (CMATAC) for the degradation of ERα in breast cancer

    JUN ZHANG, YEHONG HUANG, WENZHUO LIU, LULU LI, LIMING CHEN*

    BIOCELL, Vol.44, No.4, pp. 591-595, 2020, DOI:10.32604/biocell.2020.011642

    Abstract Estrogen receptor alpha (ERα/ESR1) is overexpressed in over half of all breast cancers and is considered a valuable therapeutic target in ERα positive breast cancer. Here, we designed a membrane-permeant Chaperonemediated Autophagy Targeting Chimeras (CMATAC) peptide to knockdown endogenous ERα protein through chaperone-mediated autophagy. The peptide contains a cell membrane-penetrating peptide (TAT) that allows the peptide to by-pass the plasma membrane, an αI peptide as a protein-binding peptide (PBD) that binds specifically to ERα, and CMA-targeting peptide (CTM) that targeting chaperone-mediated autophagy. We validated that ERα targeting peptide was able to target and degrade ERα to reduce the viability of… More >

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