ArticleCell proliferation2018
New piperidine derivative DTPEP acts as dual-acting anti-breast cancer agent by targeting ERα and downregulating PI3K/Akt-PKCα leading to caspase-dependent apoptosis.
Article in Cell proliferation, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 23 citations in OpenAlex.
- Andrographolide Selectively Inhibits the Growth of LA7 Mammary Adenocarcinoma Cells.ACS omega · 2025Article
- Piperidine and valproic acid hybrid compound (F2S4-RSC advances · 2025Article
- Phytochemical analysis of leaf extract of Piper nigrum and investigation of its biological activities.Inflammopharmacology · 2025Article
- A New Benzo[6,7]oxepino[3,2-b] Pyridine Derivative Induces Apoptosis in Canine Mammary Cancer Cell Lines.Animals : an open access journal from MDPI · 2024Article
- Therapeutic Role of Alkaloids and Alkaloid Derivatives in Cancer Management.Molecules (Basel, Switzerland) · 2023Review
- Exploring the inhibitory potential of novel piperidine-derivatives against main protease (MJournal of molecular liquids · 2023Article
- Review
- Estrogen receptor 1 inhibits the progression of hepatocellular carcinoma via positively regulating lncRNA maternally expressed gene 3 under high glucose conditions.Journal of gastrointestinal oncology · 2022Article
- Coumarins as Fungal Metabolites with Potential Medicinal Properties.Antibiotics (Basel, Switzerland) · 2022Review
- Piperidine based 1,2,3-triazolylacetamide derivatives induce cell cycle arrest and apoptotic cell death inJournal of advanced research · 2021Article
- Anticancer Applications and Pharmacological Properties of Piperidine and Piperine: A Comprehensive Review on Molecular Mechanisms and Therapeutic Perspectives.Frontiers in pharmacology · 2021Review
- ERα, A Key Target for Cancer Therapy: A Review.OncoTargets and therapy · 2020Review
- Coptisine from Coptis chinensis exerts diverse beneficial properties: A concise review.Journal of cellular and molecular medicine · 2019Review
- PLCA8 suppresses breast cancer apoptosis by activating the PI3k/AKT/NF-κB pathway.Journal of cellular and molecular medicine · 2019Article
- New piperidine derivative DTPEP acts as dual-acting anti-breast cancer agent by targeting ERα and downregulating PI3K/Akt-PKCα leading to caspase-dependent apoptosis.Cell proliferation · 2018Article
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
objectivesIn our ongoing studies to develop ER targeting agents, we screened for dual-acting molecules with a hypothesis that a single molecule can also target both ER positive and negative groups of breast cancer. MATERIALS AND
methods1-(2-(4-(Dibenzo[b,f]thiepin-10-yl)phenoxy)ethyl)piperidine (DTPEP) was synthesized and screened in both MCF-7 (ER+ve) and MDA-MB-231 (ER-ve) cells. Assays for analysis of cell cycle, ROS, apoptosis and MMP loss were carried out using flow cytometry. Its target was investigated using western blot, transactivation assay and RT-PCR. In vivo efficacy of DTPEP was validated in LA-7 syngeneic rat mammary tumour model.
resultsHere, we report identification of dual-acting molecule DTPEP that downregualtes PI3K/Akt and PKCα expression, induces ROS and ROS-dependent apoptosis, loss of mitochondrial membrane potential, induces expression of caspase indicative of both intrinsic and extrinsic apoptosis in MCF-7 and MDA-MB-231 cells. In MCF-7 cells, DTPEP downregulates ERα expression and activation. In MDA-MB-231 cells, primary cellular target of DTPEP is not clearly known, but it downregualtes PI3K/Akt and PKCα expression. In vivo study showed regression of LA-7 syngeneic mammary tumour in SD rat.
conclusionsWe identified a new dual-acting anti-breast cancer molecules as a proof of concept which is capable of targeting both ER-positive and ER-negative breast cancer.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.