ArticleBritish journal of pharmacology2018
Improving anticancer activity towards colon cancer cells with a new p53-activating agent.
Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 27 citations in OpenAlex.
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- Selenium nanoparticle-delivered MDM2 inhibitor reactivates p53 and reprograms tumor immune microenvironment in colorectal cancer.Frontiers in immunology · 2025Article
- Structure-Activity Relationship Studies of Chalcones and Diarylpentanoids with Antitumor Activity: Potency and Selectivity Optimization.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Counteracting Colon Cancer by Inhibiting Mitochondrial Respiration and Glycolysis with a Selective PKCδ Activator.International journal of molecular sciences · 2023Article
- Amaryllidaceae-Type Alkaloids fromMolecules (Basel, Switzerland) · 2022Article
- Supercritical fluid extract ofFrontiers in pharmacology · 2022Article
- BP-M345, a New Diarylpentanoid with Promising Antimitotic Activity.Molecules (Basel, Switzerland) · 2021Article
- BBIT20 inhibits homologous DNA repair with disruption of the BRCA1-BARD1 interaction in breast and ovarian cancer.British journal of pharmacology · 2021Article
- Review
- Tryptophanol-Derived Oxazolopyrrolidone Lactams as Potential Anticancer Agents against Gastric Adenocarcinoma.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Antimicrobial Peptides as New Combination Agents in Cancer Therapeutics: A Promising Protocol against HT-29 Tumoral Spheroids.International journal of molecular sciences · 2020Article
- SLMP53-2 Restores Wild-Type-Like Function to Mutant p53 through Hsp70: Promising Activity in Hepatocellular Carcinoma.Cancers · 2019Article
- Improving anticancer activity towards colon cancer cells with a new p53-activating agent.British journal of pharmacology · 2018Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeImpairment of the tumour suppressor p53 pathway is a major event in human cancers, making p53 activation one of the most attractive therapeutic strategies to halt cancer. Here, we have identified a new selective p53 activator and investigated its potential as an anticancer agent. EXPERIMENTAL APPROACH: Anti-proliferative activity of the (R)-tryptophanol-derived bicyclic lactam SYNAP was evaluated in a range of human cancer cells with different p53 status. The anticancer activity and mechanism of action of SYNAP was studied in two- and three-dimensional models of human colon adenocarcinoma HCT116 cells with wild-type p53 and corresponding p53-null isogenic derivative cells, alone and in combination with known chemotherapeutic agents. KEY
resultsSYNAP showed anti-proliferative effect in human cancer cells dependent on p53 status. In HCT116 cells, SYNAP caused p53-dependent growth inhibition, associated with cell cycle arrest and apoptosis, anti-migratory activity and regulation of the expression of p53 transcriptional targets. Data also indicated that SYNAP targeted p53, inhibiting its interaction with its endogenous inhibitors, murine double minute (MDM)2 and MDMX. Moreover, SYNAP sensitized colon cancer cells to the cytotoxic effect of known chemotherapeutic agents. SYNAP did not induce acquired or cross-resistance and re-sensitized doxorubicin-resistant colon cancer cells to chemotherapy. Additionally, SYNAP was non-genotoxic and had low cytotoxicity against normal cells. CONCLUSION AND IMPLICATIONS: SYNAP revealed encouraging anticancer activity, either alone or in combination with known chemotherapeutic agents, in colon cancer cells. Apart from its promising application in cancer therapy, SYNAP may provide a starting point for improved p53 activators.
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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.