ArticleOncotarget2017
A new HDAC inhibitor cinnamoylphenazine shows antitumor activity in association with intensive macropinocytosis.
Article in Oncotarget, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 18 citations in OpenAlex.
- Coreceptor AXL Facilitates African Swine Fever Virus Entry via Apoptotic Mimicry.Journal of virology · 2023Article
- Amplified CaInternational journal of cancer · 2022Article
- Novel Regulators of Macropinocytosis-Dependent Growth Revealed by Informer Set Library Screening in Pancreatic Cancer Cells.Metabolites · 2022Article
- The Role and Therapeutic Potential of Macropinocytosis in Cancer.Frontiers in pharmacology · 2022Review
- Contribution of Histone Deacetylases in Prognosis and Therapeutic Management of Cholangiocarcinoma.Molecular diagnosis & therapy · 2020Review
- The pervasiveness of macropinocytosis in oncological malignancies.Philosophical transactions of the Royal Society of London. Series B, Biological sciences · 2019Review
- Meridianin C inhibits the growth of YD-10B human tongue cancer cells through macropinocytosis and the down-regulation of Dickkopf-related protein-3.Journal of cellular and molecular medicine · 2018Article
- Concept of histone deacetylases in cancer: Reflections on esophageal carcinogenesis and treatment.World journal of gastroenterology · 2018Review
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Previous studies have shown that intensive macropinocytosis occurs in cancer cells and neutral red (NR) is noted for its capability to enter into the cell massively through a process mimetic to macropinocytosis. In addition, trans-cinnamic acid (tCA) has been found to be an inhibitor of histone deacetylase (HDAC). In the present study, cinnamoylphenazine (CA-PZ) that consists of NR and tCA moieties was synthesized and evaluated. As shown, CA-PZ massively entered into colon carcinoma HT-29 cells and pancreatic carcinoma MIA PaCa-2 cells and this entry was blocked by 5-(N-ethyl-N-isopropyl) amiloride (EIPA, an inhibitor of macropinocytosis), indicating a macropinocytosis-mediated uptake. Furthermore, CA-PZ markedly increased the protein expression levels of acetyl-H3, acetyl-H4 and p21 in HT-29 cells and MIA PaCa-2 cells. CA-PZ significantly inhibited the growth of colon carcinoma HT-29 and pancreatic carcinoma MIA PaCa-2 xenografts. By in vivo imaging, CA-PZ displayed prominent accumulation in the tumor xenografts. The study indicates that the newly synthesized CA-PZ acts as an HDAC inhibitor in association with intensive macropinocytosis-mediated intracellular delivery in cancer cells. The use of neutral red for preparation of chimeric molecules with the attribute of macropinocytosis-mediated intracellular delivery might open an alternative way for development of HDAC inhibitors.
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