A grafted peptidomimetic for EGFR heterodimerization inhibition: Implications in NSCLC models

Singh, Sitanshu S.; Mattheolabakis, George; Gu, Xia; Withers, Sita S.; Dahal, Achyut; Jois, Seetharama D.

doi:10.1016/j.ejmech.2021.113312

Cited by 15 publications

(10 citation statements)

References 56 publications

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“…The HER‐2‐positive breast and non‐small‐cell lung cancer cell lines BT‐474, Calu‐3, and A549 overexpress HER2, representing aggressive forms of breast and lung cancer (Lee‐Hoeflich et al., 2008; Mar, Vredenburgh, & Wasser, 2015; Naik et al., 2021; Takezawa et al., 2012; Wang et al., 2006). The compound SFTI‐G5 is a cyclic peptidomimetic that is known to target HER2‐overexpressing cancer cells and inhibit the dimerization of EGFR:HER2 and HER2:HER3 (Singh et al., 2021). This compound also inhibits lung tumor growth in an animal model.…”

Section: Commentarymentioning

confidence: 99%

Assessment of Antitumor and Antiproliferative Efficacy and Detection of Protein‐Protein Interactions in Cancer Cells from 3D Tumor Spheroids

et al. 2022

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When compared to two-dimensional (2D) cell cultures, 3D spheroids have been considered suitable in vitro models for drug discovery research and other studies of drug activity. Based on different 3D cell culture procedures, we describe procedures we have used to obtain 3D tumor spheroids by both the hangingdrop and ultra-low-attachment plate methods and to analyze the antiproliferative and antitumor efficacy of different chemotherapeutic agents, including a peptidomimetic. We have applied this method to breast and lung cancer cell lines such as BT-474, MCF-7, A549, and Calu-3. We also describe a proximity ligation assay of the cells from the spheroid model to detect protein-protein interactions of EGFR and HER2.

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Section: Commentarymentioning

confidence: 99%

Assessment of Antitumor and Antiproliferative Efficacy and Detection of Protein‐Protein Interactions in Cancer Cells from 3D Tumor Spheroids

et al. 2022

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“…Western blotting (WB) experiments were used to certify HER2 overexpression in the two cell lines (Fig. 2a, b) [26,27]. We found that the cells in the control group grew well (OD value showed an increasing trend over time).…”

Section: Antitumor Effect Of Sbp On the Cells Treated With Pyrotinib ...mentioning

confidence: 99%

Effects of Shenling Baizhu Powder on Pyrotinib-Induced Diarrhea: Analysis of Gut Microbiota, Metabonomics, and Network Pharmacology

Lai

Jiang

Zhuo

et al. 2022

Preprint

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Background Shenling Baizhu Powder (SBP) is a traditional Chinese medicine (TCM) prescription, which has good efficacy on gastrointestinal toxicity. In this study, we used gut microbiota analysis, metabonomics, and network pharmacology to investigate the therapeutic effect of SBP on pyrotinib-induced diarrhea. Methods 24 Rats were randomly divided into 4 groups: control group, SBP group (3.6 g/kg /bid SBP for 10 days), pyrotinib model group (80mg/kg/qd pyrotinib), and pyrotinib + SBP treatment group. A 16S rRNA sequencing was used to detect the microbiome of rat fecal bowel, metabolic profiles were collected by non-targeted metabolomics, and key metabolic pathways were identified using MetaboAnalyst 5.0. The antitumor effect of SBP on cells treated with pyrotinib was measured using a CCK-8 assay. Network pharmacology was used to predict the target and action pathway of SBP in treating pyrotinib-related diarrhea. Results In vivo study indicated that SBP could significantly alleviate pyrotinib-induced diarrhea, reaching a therapeutic effect of 66.7%. SBP could regulate pyrotinib-induced microbiota disorder. LEfSe research revealed that the SBP could potentially decrease the relative abundance of Escherichia, Helicobacter, and Enterobacteriaceae and increase the relative abundance of Lachnospiraceae, Bacilli, Lactobacillales etc. In addition, 25-Hydroxycholesterol, Guanidinosuccinic acid, 5-Hydroxyindolepyruvate, and cAMP were selected as potential biomarkers of SBP for pyrotinib-induced diarrhea. Moreover, Spearman's analysis showed a correlation between gut microbiota and metabolite: the decreased 25-hydroxycholesterol in the SBP treatment group was negatively correlated with Lachnospiraceae while positively correlated with Escherichia and Helicobacter. Meanwhile, SBP did not affect the inhibitory effect of pyrotinib on BT-474 cells and Calu-3 cells in vitro. Also, network analysis further revealed that SBP treated pyrotinib-induced diarrhea through multiple pathways, including inflammatory bowel disease, IL-17 signaling pathway, pathogenic Escherichia coli infection, and cAMP signaling pathway. Conclusions SBP could effectively relieve pyrotinib-induced diarrhea, revealing that intestinal flora and its metabolites may be involved in this process.

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“…Other approaches such as peptidomimetic approach or grafted peptides and stapled peptide approaches where peptides are stabilized for in vivo delivery should be considered. [ 76 , 125 , 126 , 127 , 128 ]…”

Section: Challenges Of Peptides As Therapeutics For Covid‐19mentioning

confidence: 99%

“…Mutated amino acid residues are shown as spheres (magenta) along with a label peptidomimetic approach or grafted peptides and stapled peptide approaches where peptides are stabilized for in vivo delivery should be considered. [76,[125][126][127][128] 7 | CONCLUSIONS AND FUTURE DIRECTIONS…”

Section: Challenges Of Peptides As Therapeutics For Covid-19mentioning

confidence: 99%

Peptides and peptidomimetics as therapeutic agents for Covid‐19

et al. 2021

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The severe acute respiratory syndrome coronavirus‐2 (SARS‐CoV‐2) Covid‐19 pandemic has caused high morbidity and mortality rates worldwide. Virus entry into cells can be blocked using several strategies, including inhibition of protein‐protein interactions (PPIs) between the viral spike glycoprotein and cellular receptors, as well as blocking of spike protein conformational changes that are required for cleavage/activation and fusogenicity. The spike‐mediated viral attachment and entry into cells via fusion of the viral envelope with cellular membranes involve PPIs mediated by short peptide fragments exhibiting particular secondary structures. Thus, peptides that can inhibit these PPIs may be used as potential antiviral agents preventing virus entry and spread. This review is focused on peptides and peptidomimetics as PPI modulators and protease inhibitors against SARS‐CoV‐2.

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A grafted peptidomimetic for EGFR heterodimerization inhibition: Implications in NSCLC models

Cited by 15 publications

References 56 publications

Assessment of Antitumor and Antiproliferative Efficacy and Detection of Protein‐Protein Interactions in Cancer Cells from 3D Tumor Spheroids

Assessment of Antitumor and Antiproliferative Efficacy and Detection of Protein‐Protein Interactions in Cancer Cells from 3D Tumor Spheroids

Effects of Shenling Baizhu Powder on Pyrotinib-Induced Diarrhea: Analysis of Gut Microbiota, Metabonomics, and Network Pharmacology

Peptides and peptidomimetics as therapeutic agents for Covid‐19

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