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Terpenoids: The Biological Key Molecules
Published in Dijendra Nath Roy, Terpenoids Against Human Diseases, 2019
Moumita Majumdar, Dijendra Nath Roy
The ErbB, or HER, pathway is regulated by terpenoids in an interactive manner. ErbB proteins are, in nature, tyrosine kinases comprising four receptors structurally analogous to epidermal growth factor receptor (EGFR). In the human body, these include Her1 (EGFR, ErbB1), Her2 (Neu, ErbB2), Her3 (ErbB3) and Her4 (ErbB4). With the overexpression of genes, this pathway causes uncontrolled cell proliferation, leading to cancer development (Cho and Leahy 2002). After conformational changes, phosphorylated tyrosine residues of the receptor proteins act as binding sites for the RAS-rapidly accelerated fibrosarcoma-MAPK (RAS-Raf-MAPK) pathway, which inhibits apoptosis (Herbst 2004).
Aptamers as Tools for Targeted Drug Delivery
Published in Rakesh N. Veedu, Aptamers, 2017
The ErbB-2 receptor belongs to the epidermal growth factor-related protein family of receptor tyrosine kinases and is overex-pressed in many cancers. The anticancerous activity of a trimeric version of ErbB-2 receptor was tested both in vitro and in vivo (Fig. 8.2) [53]. The antiproliferative studies were conducted in human gastric cancer N87 cancer cells and in female CD-1 nude mice intradermally inoculated with N87 cells. The aptamer multimerization helped the avidity of binding to the ErbB-2 receptor and in crosslinking the receptor on the cell surface. The authors suggest that higher oligomers of the aptamer may have increased effectiveness and are not limited to trimers [53]. A nuclease-resistant therapeutic aptamer that binds specifically to the epidermal growth factor receptor (EGFR) was selected by SELEX, and the activity was studied in EGFR-positive cancer cells [29]. The results indicate that the aptamer CL4 was successful in inducing apoptosis in the cells that were resistant to commonly used therapeutic EGFR inhibitors. When co-administered with cetuximab, synergistic effect in the therapeutic effect was observed, both in vitro and in vivo [29]. The chemically modified Adipo8 aptamer was tested for its selectivity in binding to white adipose tissues, the accumulation of which leads to obesity [19]. The aptamer was modified by introducing phosphorothioate linkage (PS linkage) and conjugating with PEG. The modified aptamers could selectively identify the white adipose tissue compared to other types of adipose and pre-adipose tissues. Adipo8 inhibited adipogenic differentiation of adipose tissue and holds great promise for the development of therapeutic strategies against obesity [19].
Small-Molecule Inhibitors Targeting Receptor Tyrosine Kinases in Cancer
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2020
Mohammad Hojjat-Farsangi, Gholamreza Khamisipour
EGFR or ErbB family have four members with similar structure, including EGFR (ErbB1), HER2/neu (ErbB2), HER3 (ErbB3), and HER4 (ErbB4). Members of this family are important for the regulation of normal cell proliferation, differentiation, and survival. In normal situations, EGFR ligand (EGF) binds to the extracellular part of EGFR and induce EGFR homo/heterodimerization with other members of this family and leads to phosphorylation at specific tyrosine amino acids within the kinase domain (Ono and Kuwano, 2006).
Expression profiles of long non-coding RNA in mouse lung tissue exposed to radon
Published in Journal of Toxicology and Environmental Health, Part A, 2019
Jihua Nie, Jing Wu, Zhihai Chen, Yang Jiao, Jie Zhang, Hailin Tian, Jianxiang Li, Jian Tong
ErbB pathway plays an important role in the regulation of cellular proliferation, cell survival and differentiation. Dysregulation of this pathway is linked to various types of cancers (Brizzolara et al. 2017; Glogowska et al. 2017). Notch signaling pathway is involved in dysregulated cell growth, proliferation and carcinogenesis (Lee et al. 2016; Lobry et al. 2014). Functional analysis via bioinformatics in this study suggested that the genes involved in ErbB and Notch signaling pathways were upregulated. The results from our study revealed increased ErbB2 and k-Ras protein expression in lung tissue of mice exposed to radon compared to controls. It is of interest that Lu and Zeng (2017) also observed that enhanced k-Ras and p53 protein expressions to be associated with pancreatic adenocarcinoma. These observations suggested that the involvement of k-Ras and p53 protein elevation might be associated with radon-induced mouse pulmonary injury. In summary, radon exposure enriched several lncRNAs which were implicated in the regulation of mRNA expression of transcription factors may be involved in radon-induced lung carcinogenesis. However, further investigations are required to verify the network alterations between lncRNA and coding genes.
A new Ho(III) dinuclear complex: treatment activity and cure values on mania by reducing the expression of the ErbB4 on the noradrenergic neurons
Published in Inorganic and Nano-Metal Chemistry, 2021
Yong-Hua Chen, Yan Xu, Hao Wu, Xiao-Yi Li, Ming-Jun Zhang
ErbB4 is a ubiquitously expressed member of the ErbB family of receptor tyrosine kinases that is essential for normal development of the mammary gland, nervous system, and heart. To explain the experimental results that the Ho metal complex may exhibit activities to the ErbB4 kinase, the molecular docking has been performed for the Ho metal complex in contacting with 3BCE receptor.